Farnesoid X receptor (FXR): Structures and ligands

[Display omitted] Farnesoid X receptor (FXR) is a bile acid activated nuclear receptor (BAR) and is mainly expressed in the liver and intestine. Upon ligand binding, FXR regulates key genes involved in the metabolic process of bile acid synthesis, transport and reabsorption and is also involved in t...

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Published in:Computational and structural biotechnology journal Vol. 19; pp. 2148 - 2159
Main Authors: Jiang, Longying, Zhang, Huajun, Xiao, Desheng, Wei, Hudie, Chen, Yongheng
Format: Journal Article
Language:English
Published: Netherlands Elsevier B.V 01.01.2021
Research Network of Computational and Structural Biotechnology
Elsevier
Subjects:
Agonists
Antagonists
bile
bile acids
biotechnology
domain
drugs
Farnesoid X receptor
intestines
Ligand binding domain
ligands
liver
metabolism
resorption
Review
Structure
therapeutics
Farnesoid X receptor
Agonists
Antagonists
Structure
Ligand binding domain
ISSN:2001-0370, 2001-0370
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Abstract [Display omitted] Farnesoid X receptor (FXR) is a bile acid activated nuclear receptor (BAR) and is mainly expressed in the liver and intestine. Upon ligand binding, FXR regulates key genes involved in the metabolic process of bile acid synthesis, transport and reabsorption and is also involved in the metabolism of carbohydrates and lipids. Because of its important functions, FXR is considered as a promising drug target for the therapy of bile acid-related liver diseases. With the approval of obeticholic acid (OCA) as the first small molecule to target FXR, many other small molecules are being evaluated in clinical trials. This review summarizes the structures of FXR, especially its ligand binding domain, and the development of small molecules (including agonists and antagonists) targeting FXR.
AbstractList Farnesoid X receptor (FXR) is a bile acid activated nuclear receptor (BAR) and is mainly expressed in the liver and intestine. Upon ligand binding, FXR regulates key genes involved in the metabolic process of bile acid synthesis, transport and reabsorption and is also involved in the metabolism of carbohydrates and lipids. Because of its important functions, FXR is considered as a promising drug target for the therapy of bile acid-related liver diseases. With the approval of obeticholic acid (OCA) as the first small molecule to target FXR, many other small molecules are being evaluated in clinical trials. This review summarizes the structures of FXR, especially its ligand binding domain, and the development of small molecules (including agonists and antagonists) targeting FXR.Farnesoid X receptor (FXR) is a bile acid activated nuclear receptor (BAR) and is mainly expressed in the liver and intestine. Upon ligand binding, FXR regulates key genes involved in the metabolic process of bile acid synthesis, transport and reabsorption and is also involved in the metabolism of carbohydrates and lipids. Because of its important functions, FXR is considered as a promising drug target for the therapy of bile acid-related liver diseases. With the approval of obeticholic acid (OCA) as the first small molecule to target FXR, many other small molecules are being evaluated in clinical trials. This review summarizes the structures of FXR, especially its ligand binding domain, and the development of small molecules (including agonists and antagonists) targeting FXR.
Farnesoid X receptor (FXR) is a bile acid activated nuclear receptor (BAR) and is mainly expressed in the liver and intestine. Upon ligand binding, FXR regulates key genes involved in the metabolic process of bile acid synthesis, transport and reabsorption and is also involved in the metabolism of carbohydrates and lipids. Because of its important functions, FXR is considered as a promising drug target for the therapy of bile acid-related liver diseases. With the approval of obeticholic acid (OCA) as the first small molecule to target FXR, many other small molecules are being evaluated in clinical trials. This review summarizes the structures of FXR, especially its ligand binding domain, and the development of small molecules (including agonists and antagonists) targeting FXR.
[Display omitted] Farnesoid X receptor (FXR) is a bile acid activated nuclear receptor (BAR) and is mainly expressed in the liver and intestine. Upon ligand binding, FXR regulates key genes involved in the metabolic process of bile acid synthesis, transport and reabsorption and is also involved in the metabolism of carbohydrates and lipids. Because of its important functions, FXR is considered as a promising drug target for the therapy of bile acid-related liver diseases. With the approval of obeticholic acid (OCA) as the first small molecule to target FXR, many other small molecules are being evaluated in clinical trials. This review summarizes the structures of FXR, especially its ligand binding domain, and the development of small molecules (including agonists and antagonists) targeting FXR.
Author Jiang, Longying
Xiao, Desheng
Chen, Yongheng
Zhang, Huajun
Wei, Hudie
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  surname: Wei
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  surname: Chen
  fullname: Chen, Yongheng
  email: yonghenc@163.com
  organization: Department of Pathology, NHC Key Laboratory of Cancer Proteomics, Laboratory of Structural Biology, National Clinical Research Center for Geriatric Disorders, Xiangya Hospital, Central South University, Changsha, Hunan 410008, China
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Cites_doi 10.1074/jbc.RA118.004652
10.1016/S0168-8278(18)31427-2
10.1016/j.jhep.2007.09.015
10.1016/j.bmc.2018.07.017
10.1016/j.tibs.2006.08.002
10.1002/hep.30509
10.1016/j.bbadis.2017.08.016
10.1074/jbc.M209323200
10.1021/acsmedchemlett.8b00534
10.1080/13543784.2020.1763302
10.1002/hep.22661
10.3389/fphar.2020.01247
10.1021/acsmedchemlett.0c00647
10.1074/jbc.275.15.10918
10.1002/cbic.201700059
10.1053/j.gastro.2014.08.042
10.1021/acs.jmedchem.5b00342
10.1016/j.jhep.2016.01.016
10.1016/j.cct.2019.105889
10.1016/j.tiv.2016.11.014
10.1124/mol.110.064501
10.1002/hep.23450
10.1021/np100489u
10.1002/hep.31205
10.1021/acs.jmedchem.5b01161
10.1093/emboj/cdg569
10.1038/s41586-020-2569-1
10.1016/S0092-8674(00)00062-3
10.1007/s10620-016-4143-0
10.1002/hep4.1193
10.1021/jm8014124
10.1126/science.1072891
10.1084/jem.20171965
10.1074/jbc.275.14.10638
10.1002/hep.24537
10.1007/164_2019_227
10.1038/srep42801
10.1016/j.ejphar.2013.10.048
10.1053/j.gastro.2013.05.042
10.2174/1568026614666141112103516
10.1016/j.bbrc.2020.10.039
10.1039/C9MD00264B
10.1021/jm3002718
10.1152/ajpgi.00356.2017
10.1021/acs.jmedchem.7b00907
10.1172/JCI0214505
10.1371/journal.pone.0105930
10.3390/nu11051132
10.1016/S1097-2765(03)00104-7
10.3390/ijms17040536
10.1002/pro.3496
10.1093/molbev/msm251
10.3390/cancers11101478
10.1111/jcmm.16083
10.1021/acsmedchemlett.0c00640
10.3389/fchem.2018.00140
10.1021/ci300459k
10.1021/acs.jmedchem.9b01621
10.1186/s13046-018-0781-8
10.1074/jbc.M114.630475
10.1016/S0140-6736(19)33041-7
10.1016/j.aquatox.2010.02.020
10.1371/journal.pone.0115028
10.1007/164_2019_232
10.1016/j.bmc.2014.04.014
10.1016/j.cmet.2005.09.001
10.1016/S1097-2765(00)00051-4
10.1016/j.metabol.2018.03.016
10.1016/S0140-6736(14)61933-4
10.1002/minf.200900009
10.1016/S1097-2765(00)80348-2
10.1074/jbc.M011610200
10.1358/dot.2016.52.12.2571703
10.1016/j.bbapap.2014.06.007
10.1073/pnas.0710981105
10.1016/j.cell.2019.01.036
10.1007/s40265-016-0616-x
10.1111/joim.12140
10.1074/jbc.RA118.004188
10.1053/j.gastro.2014.12.005
10.1016/j.jhep.2017.01.013
10.1186/s12929-018-0475-8
10.1002/hep.30661
10.1016/j.bmcl.2008.06.073
10.1038/s41467-019-10853-2
10.1016/S1097-2765(03)00112-6
10.1016/j.bbadis.2010.11.011
10.1038/378681a0
10.1016/j.bioorg.2019.103511
10.1681/ASN.2017020222
10.1080/07391102.2018.1462735
10.1074/jbc.M209505200
10.1007/164_2019_233
10.1038/s41598-017-12629-4
10.1021/jm7015864
10.1002/hep.29569
10.1016/j.cmet.2013.01.003
10.1016/j.tibs.2014.10.011
10.1002/cpdd.762
10.1177/0960327118817862
10.1002/cphy.c120023
10.1371/journal.pone.0030443
10.1002/mnfr.201900608
10.1371/journal.pone.0129866
10.1021/jm501273r
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Keywords Farnesoid X receptor
Agonists
Antagonists
Structure
Ligand binding domain
Language English
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  text: 2021-01-01
  day: 01
PublicationDecade 2020
PublicationPlace Netherlands
PublicationPlace_xml – name: Netherlands
PublicationTitle Computational and structural biotechnology journal
PublicationTitleAlternate Comput Struct Biotechnol J
PublicationYear 2021
Publisher Elsevier B.V
Research Network of Computational and Structural Biotechnology
Elsevier
Publisher_xml – name: Elsevier B.V
– name: Research Network of Computational and Structural Biotechnology
– name: Elsevier
References Chen, Yang, Lai, Kang, Gan (b0390) 2016; 17
Tully, Rucker, Chianelli, Williams, Vidal (b0295) 2017; 60
Chen, Wu, Hsu, Liou, Chang (b0095) 2018; 25
Zhan, Liu, Fang, Kong, He (b0155) 2014; 9
Festa, Finamore, Marchianò, Di Leva, Carino (b0490) 2019; 10
Goodwin, Jones, Price, Watson, McKee (b0040) 2000; 6
Kowdley, Luketic, Chapman, Hirschfield, Poupon (b0530) 2018; 67
Downes, Verdecia, Roecker, Hughes, Hogenesch (b0165) 2003; 11
Sayin, Wahlström, Felin, Jäntti, Marschall (b0310) 2013; 17
Gomez-Ospina, Potter, Xiao, Manickam, Kim (b0090) 2016; 7
Kemper (b0025) 2011; 8
Yang, Broderick, Jiang, Hsu, Maier (b0205) 2014; 1844
Jin, Feng, Rong, Pan, Inaba (b0220) 2013; 4
Huang, Yu, Gao, Zhang, Li (b0470) 2012; 55
Cui, Martin, Jin, Liu, Pandit (b0100) 2018; 37
Jiang, Xie, Lv, Li, Krausz (b0500) 2015; 6
Fu, Coulter, Yoshihara, Oh, Fang (b0030) 2019; 176
Al-Aqil, Monte, Peleteiro-Vigil, Briz, Rosales (b0045) 2018; 9
Fiorucci, Biagioli, Sepe, Zampella, Distrutti (b0230) 2020; 29
Zheng, Lu, Tian, Ma, Wei (b0170) 2018; 293
Ijssennagger, Janssen, Milona, Ramos Pittol, Hollman (b0065) 2016; 64
Ahmad, Sanderson, Dickerson, Adda (b0330) 2018; 68
Li, Yang, Wang, Qi, Yang (b0430) 2020; 11
Teno, Iguchi, Oda, Yamashita, Masuda (b0510) 2021; 12
Inagaki, Choi, Moschetta, Peng, Cummins (b0050) 2005; 2
Yu, Lin, Forman, Chen (b0485) 2014; 22
Lieu, Jayaweera, Zhao, Poole, Jensen (b0340) 2014; 147
Baghdasaryan, Claudel, Gumhold, Silbert, Adorini (b0550) 2011; 54
Mi, Devarakonda, Harp, Han, Pellicciari (b0175) 2003; 11
Yang, Mao, Guo, Lin, Ming (b0555) 2020; 587
Li, Fu, Cheng, Zheng, Zhang (b0355) 2012; 52
Rastinejad, Ollendorff, Polikarpov (b0200) 2015; 40
Shapiro, Kolodziejczyk, Halstuch, Elinav (b0055) 2018; 215
Hoeke, Plass, Heegsma, Geuken, van Rijsbergen (b0060) 2009; 49
Festa, Renga, D'Amore, Sepe, Finamore (b0420) 2014; 57
Gege, Hambruch, Hambruch, Kinzel, Kremoser (b0360) 2019; 256
Attia, Tawfiq, Ali, Elmazar (b0110) 2017; 7
Loomba, Noureddin, Kowdley, Kohli, Sheikh (b0290) 2020; 10
Cao, Xiao, Zhou, Yan, Wang (b0085) 2019; 317
Schmidt, Schierle, Gellrich, Kaiser, Merk (b0480) 2018; 26
Xu (b0460) 2016; 59
Akwabi-Ameyaw, Bass, Caldwell, Caravella, Chen (b0270) 2008; 18
Gautam, Paudel, Abidin, Bhandari (b0440) 2019; 38
Xu, Liu, Zhu, Chen, Fu (b0225) 2015; 290
Soisson, Parthasarathy, Adams, Sahoo, Sitlani (b0545) 2008; 105
Künnemann K, The Liver Meeting 2016 - American Association for the Study of Liver Diseases, 67th Annual Meeting (November 11-15, 2016 - Boston, Massachusetts, USA): Drugs Today (Barc). 2016 Dec;52(12):673-680. DOI:10.1358/dot.2016.52.12.2571703.
Genin, Bueno, Agejas Francisco, Manninen, Bocchinfuso (b0275) 2015; 58
Patel, Harrison, Elkhashab, Trotter, Herring (b0285) 2020; 72
Urizar, Liverman, Dodds, Silva, Ordentlich (b0465) 2002; 296
Flatt, Martin, Wang, Mahaney, Murphy (b0280) 2009; 52
Younossi, Ratziu, Loomba, Rinella, Anstee (b0255) 2019; 394
Pedrosa, Seyedkazemi, Francque, Sanyal, Rinella (b0300) 2020; 88
Merk, Sreeramulu, Kudlinzki, Saxena, Linhard (b0190) 2019; 10
Renaud, Rochel, Ruff, Vivat, Chambon (b0195) 1995; 378
Chiang, Kimmel, Weinberger, Stroup (b0035) 2000; 275
Zhang, Cayting, Weinstock, Gerstein (b0010) 2008; 25
Amano, Shimada, Miura, Adachi, Tozawa (b0475) 2014; 723
Trauner, Gulamhusein, Hameed, Caldwell, Shiffman (b0365) 2019; 70
Wang, Chen, Hollister, Sowers, Forman (b0235) 1999; 3
Laffitte, Kast, Nguyen, Zavacki, Moore (b0145) 2000; 275
Verbeke L, Nevens F and Laleman W, Steroidal or non-steroidal FXR agonists - Is that the question? Vol. 66(4). 2017: J Hepatol. 680-681.
Weikum, Liu, Ortlund (b0125) 2018; 27
Helmstädter, Vietor, Sommer, Schierle, Willems (b0375) 2021; 12
Zheng, Lu, Lin, Wang, Qiu (b0215) 2017; 18
Kumar, Singh, Tali, Dheer, Shankar (b0515) 2020; 95
Li, Xu, Guo, Zheng, Sun (b0105) 2020; 24
van Zutphen, Bertolini, de Vries, Bloks, de Boer (b0240) 2019; 256
Neuschwander-Tetri, Loomba, Sanyal, Lavine, Van Natta (b0260) 2015; 385
Chianelli, Rucker, Roland, Tully, Nelson (b0305) 2020; 63
Carino, Cipriani, Marchianò, Biagioli, Santorelli (b0400) 2017; 7
Devarakonda, Harp, Kim, Ozyhar, Rastinejad (b0135) 2003; 22
Mudaliar, Henry, Sanyal, Morrow, Marschall (b0250) 2013; 145
Lee, Lee, Hubbert, Edwards, Zhang (b0005) 2006; 31
Wang, Wang, Luo, Myakala, Dobrinskikh (b0395) 2018; 29
Ovadia, Perdones-Montero, Spagou, Smith, Sarafian (b0080) 2019; 70
Carino, Marchianò, Biagioli, Fiorucci, Zampella (b0410) 2019; 11
Zhang, Kast-Woelbern, Edwards (b0020) 2003; 278
Claudel, Sturm, Duez, Torra, Sirvent (b0150) 2002; 109
Rizzo, Passeri, De Franco, Ciaccioli, Donadio (b0405) 2010; 78
Boesjes, Bloks, Hageman, Bos, van Dijk (b0015) 2014; 9
Fiorucci, Di Giorgio, Distrutti (b0345) 2019; 256
Leo, Therachiyil, Siveen, Uddin, Kulinski (b0435) 2019; 11
Sherif, Saeed, Ghavimi, Nouraie, Laiyemo (b0535) 2016; 61
Steri, Schneider, Klenner, Rupp, Kriegl (b0380) 2010; 29
Passeri, Carotti, Pittol, Ciaccioli, Pellicciari (b0315) 2019; 10
Wang, Zou, Xu, Zhang, Liu (b0140) 2018; 293
Diao, Jiang, Zhang, Li, Shan (b0180) 2018; 6
Howarth, Hagey, Law, Ai, Krasowski (b0130) 2010; 98
Sato, Macchiarulo, Thomas, Gioiello, Une (b0540) 2008; 51
Ananthanarayanan, Balasubramanian, Makishima, Mangelsdorf, Suchy (b0070) 2001; 276
Lamers, Schubert-Zsilavecz, Merk (b0385) 2014; 14
Erstad, Farrar, Ghoshal, Masia, Ferreira (b0265) 2018; 2
Choi, Hwang, Chin, Kim, Lee (b0520) 2011; 74
Xu, Shi, Chen, Zhou, Wang (b0450) 2018; 85
Hu, Bonde, Eggertsen, Rudling (b0495) 2014; 275
Markham, Keam (b0120) 2016; 76
Hui, Liu, Chen, Wang, Lang (b0455) 2019; 63
Jiang, Xiao, Li, Dai, Qu (b0185) 2021; 534
Sinal, Tohkin, Miyata, Ward, Lambert (b0350) 2000; 102
Du, Qiu, Guo, Yao (b0425) 2019; 37
Dash, Figler, Blackman, Marukian, Collado (b0075) 2017; 39
Hirschfield, Mason, Luketic, Lindor, Gordon (b0525) 2015; 148
Erice, Labiano, Arbelaiz, Santos-Laso, Munoz-Garrido (b0115) 2018; 1864
Chiang (b0245) 2013; 3
Badman, Chen, Desai, Vaidya, Neelakantham (b0370) 2020; 9
Gaieb, Liu, Gathiaka, Chiu, Yang (b0210) 2018; 34
Scholtes, Diaz, Icard, Kaul, Bartenschlager (b0320) 2008; 48
Renga, Mencarelli, D'Amore, Cipriani, D'Auria (b0445) 2012; 7
Cipriani, Renga, D'Amore, Simonetti, De Tursi (b0415) 2015; 10
Cui, Huang, Zhao, Lew, Yu (b0505) 2003; 278
Thomas, Hart, Kong, Fang, Zhong (b0160) 2010; 51
Wang (10.1016/j.csbj.2021.04.029_b0140) 2018; 293
Yang (10.1016/j.csbj.2021.04.029_b0205) 2014; 1844
Li (10.1016/j.csbj.2021.04.029_b0105) 2020; 24
Passeri (10.1016/j.csbj.2021.04.029_b0315) 2019; 10
Flatt (10.1016/j.csbj.2021.04.029_b0280) 2009; 52
Hu (10.1016/j.csbj.2021.04.029_b0495) 2014; 275
Lamers (10.1016/j.csbj.2021.04.029_b0385) 2014; 14
Fu (10.1016/j.csbj.2021.04.029_b0030) 2019; 176
Boesjes (10.1016/j.csbj.2021.04.029_b0015) 2014; 9
Dash (10.1016/j.csbj.2021.04.029_b0075) 2017; 39
Festa (10.1016/j.csbj.2021.04.029_b0490) 2019; 10
Devarakonda (10.1016/j.csbj.2021.04.029_b0135) 2003; 22
Ananthanarayanan (10.1016/j.csbj.2021.04.029_b0070) 2001; 276
Sinal (10.1016/j.csbj.2021.04.029_b0350) 2000; 102
Chianelli (10.1016/j.csbj.2021.04.029_b0305) 2020; 63
Merk (10.1016/j.csbj.2021.04.029_b0190) 2019; 10
Helmstädter (10.1016/j.csbj.2021.04.029_b0375) 2021; 12
Leo (10.1016/j.csbj.2021.04.029_b0435) 2019; 11
Jiang (10.1016/j.csbj.2021.04.029_b0500) 2015; 6
Ovadia (10.1016/j.csbj.2021.04.029_b0080) 2019; 70
Mudaliar (10.1016/j.csbj.2021.04.029_b0250) 2013; 145
Lieu (10.1016/j.csbj.2021.04.029_b0340) 2014; 147
Zheng (10.1016/j.csbj.2021.04.029_b0215) 2017; 18
Baghdasaryan (10.1016/j.csbj.2021.04.029_b0550) 2011; 54
Hui (10.1016/j.csbj.2021.04.029_b0455) 2019; 63
Genin (10.1016/j.csbj.2021.04.029_b0275) 2015; 58
10.1016/j.csbj.2021.04.029_b0335
Markham (10.1016/j.csbj.2021.04.029_b0120) 2016; 76
Chen (10.1016/j.csbj.2021.04.029_b0390) 2016; 17
Shapiro (10.1016/j.csbj.2021.04.029_b0055) 2018; 215
Teno (10.1016/j.csbj.2021.04.029_b0510) 2021; 12
Fiorucci (10.1016/j.csbj.2021.04.029_b0345) 2019; 256
Xu (10.1016/j.csbj.2021.04.029_b0450) 2018; 85
Carino (10.1016/j.csbj.2021.04.029_b0400) 2017; 7
Al-Aqil (10.1016/j.csbj.2021.04.029_b0045) 2018; 9
Cui (10.1016/j.csbj.2021.04.029_b0100) 2018; 37
Sato (10.1016/j.csbj.2021.04.029_b0540) 2008; 51
Mi (10.1016/j.csbj.2021.04.029_b0175) 2003; 11
Erice (10.1016/j.csbj.2021.04.029_b0115) 2018; 1864
Neuschwander-Tetri (10.1016/j.csbj.2021.04.029_b0260) 2015; 385
Goodwin (10.1016/j.csbj.2021.04.029_b0040) 2000; 6
Downes (10.1016/j.csbj.2021.04.029_b0165) 2003; 11
Festa (10.1016/j.csbj.2021.04.029_b0420) 2014; 57
Renaud (10.1016/j.csbj.2021.04.029_b0195) 1995; 378
Schmidt (10.1016/j.csbj.2021.04.029_b0480) 2018; 26
Li (10.1016/j.csbj.2021.04.029_b0355) 2012; 52
Hirschfield (10.1016/j.csbj.2021.04.029_b0525) 2015; 148
Huang (10.1016/j.csbj.2021.04.029_b0470) 2012; 55
Cui (10.1016/j.csbj.2021.04.029_b0505) 2003; 278
Ahmad (10.1016/j.csbj.2021.04.029_b0330) 2018; 68
Tully (10.1016/j.csbj.2021.04.029_b0295) 2017; 60
Sherif (10.1016/j.csbj.2021.04.029_b0535) 2016; 61
Jiang (10.1016/j.csbj.2021.04.029_b0185) 2021; 534
Chiang (10.1016/j.csbj.2021.04.029_b0245) 2013; 3
Badman (10.1016/j.csbj.2021.04.029_b0370) 2020; 9
Gege (10.1016/j.csbj.2021.04.029_b0360) 2019; 256
Carino (10.1016/j.csbj.2021.04.029_b0410) 2019; 11
Xu (10.1016/j.csbj.2021.04.029_b0225) 2015; 290
Kumar (10.1016/j.csbj.2021.04.029_b0515) 2020; 95
Zhan (10.1016/j.csbj.2021.04.029_b0155) 2014; 9
Gautam (10.1016/j.csbj.2021.04.029_b0440) 2019; 38
Li (10.1016/j.csbj.2021.04.029_b0430) 2020; 11
Cao (10.1016/j.csbj.2021.04.029_b0085) 2019; 317
Pedrosa (10.1016/j.csbj.2021.04.029_b0300) 2020; 88
Attia (10.1016/j.csbj.2021.04.029_b0110) 2017; 7
Cipriani (10.1016/j.csbj.2021.04.029_b0415) 2015; 10
Zheng (10.1016/j.csbj.2021.04.029_b0170) 2018; 293
Jin (10.1016/j.csbj.2021.04.029_b0220) 2013; 4
Trauner (10.1016/j.csbj.2021.04.029_b0365) 2019; 70
10.1016/j.csbj.2021.04.029_b0325
Choi (10.1016/j.csbj.2021.04.029_b0520) 2011; 74
Inagaki (10.1016/j.csbj.2021.04.029_b0050) 2005; 2
Thomas (10.1016/j.csbj.2021.04.029_b0160) 2010; 51
Rastinejad (10.1016/j.csbj.2021.04.029_b0200) 2015; 40
Erstad (10.1016/j.csbj.2021.04.029_b0265) 2018; 2
Akwabi-Ameyaw (10.1016/j.csbj.2021.04.029_b0270) 2008; 18
Rizzo (10.1016/j.csbj.2021.04.029_b0405) 2010; 78
Hoeke (10.1016/j.csbj.2021.04.029_b0060) 2009; 49
Howarth (10.1016/j.csbj.2021.04.029_b0130) 2010; 98
Gomez-Ospina (10.1016/j.csbj.2021.04.029_b0090) 2016; 7
van Zutphen (10.1016/j.csbj.2021.04.029_b0240) 2019; 256
Weikum (10.1016/j.csbj.2021.04.029_b0125) 2018; 27
Claudel (10.1016/j.csbj.2021.04.029_b0150) 2002; 109
Gaieb (10.1016/j.csbj.2021.04.029_b0210) 2018; 34
Xu (10.1016/j.csbj.2021.04.029_b0460) 2016; 59
Du (10.1016/j.csbj.2021.04.029_b0425) 2019; 37
Ijssennagger (10.1016/j.csbj.2021.04.029_b0065) 2016; 64
Zhang (10.1016/j.csbj.2021.04.029_b0020) 2003; 278
Zhang (10.1016/j.csbj.2021.04.029_b0010) 2008; 25
Kowdley (10.1016/j.csbj.2021.04.029_b0530) 2018; 67
Scholtes (10.1016/j.csbj.2021.04.029_b0320) 2008; 48
Laffitte (10.1016/j.csbj.2021.04.029_b0145) 2000; 275
Yu (10.1016/j.csbj.2021.04.029_b0485) 2014; 22
Wang (10.1016/j.csbj.2021.04.029_b0235) 1999; 3
Soisson (10.1016/j.csbj.2021.04.029_b0545) 2008; 105
Renga (10.1016/j.csbj.2021.04.029_b0445) 2012; 7
Younossi (10.1016/j.csbj.2021.04.029_b0255) 2019; 394
Sayin (10.1016/j.csbj.2021.04.029_b0310) 2013; 17
Chiang (10.1016/j.csbj.2021.04.029_b0035) 2000; 275
Steri (10.1016/j.csbj.2021.04.029_b0380) 2010; 29
Loomba (10.1016/j.csbj.2021.04.029_b0290) 2020; 10
Chen (10.1016/j.csbj.2021.04.029_b0095) 2018; 25
Lee (10.1016/j.csbj.2021.04.029_b0005) 2006; 31
Patel (10.1016/j.csbj.2021.04.029_b0285) 2020; 72
Urizar (10.1016/j.csbj.2021.04.029_b0465) 2002; 296
Amano (10.1016/j.csbj.2021.04.029_b0475) 2014; 723
Kemper (10.1016/j.csbj.2021.04.029_b0025) 2011; 8
Diao (10.1016/j.csbj.2021.04.029_b0180) 2018; 6
Wang (10.1016/j.csbj.2021.04.029_b0395) 2018; 29
Yang (10.1016/j.csbj.2021.04.029_b0555) 2020; 587
Fiorucci (10.1016/j.csbj.2021.04.029_b0230) 2020; 29
35317235 - Comput Struct Biotechnol J. 2022 Mar 01;20:1227-1228. doi: 10.1016/j.csbj.2022.02.029
References_xml – volume: 18
  start-page: 4339
  year: 2008
  end-page: 4343
  ident: b0270
  article-title: Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064
  publication-title: Bioorg Med Chem Lett
– volume: 54
  start-page: 1303
  year: 2011
  end-page: 1312
  ident: b0550
  article-title: Dual farnesoid X receptor/TGR5 agonist INT-767 reduces liver injury in the Mdr2-/- (Abcb4-/-) mouse cholangiopathy model by promoting biliary HCO
  publication-title: Hepatology
– volume: 29
  start-page: 287
  year: 2010
  end-page: 292
  ident: b0380
  article-title: Target profile prediction: cross-activation of peroxisome proliferator-activated receptor (PPAR) and farnesoid X receptor (FXR)
  publication-title: Mol Inform
– volume: 11
  start-page: 1247
  year: 2020
  ident: b0430
  article-title: Farnesoid X receptor agonists as therapeutic target for cardiometabolic diseases
  publication-title: Front Pharmacol
– volume: 98
  start-page: 245
  year: 2010
  end-page: 255
  ident: b0130
  article-title: Two farnesoid X receptor alpha isoforms in Japanese medaka (Oryzias latipes) are differentially activated in vitro
  publication-title: Aquat Toxicol
– volume: 61
  start-page: 1214
  year: 2016
  end-page: 1225
  ident: b0535
  article-title: Global epidemiology of nonalcoholic fatty liver disease and perspectives on US minority populations
  publication-title: Dig Dis Sci
– volume: 68
  start-page: S584
  year: 2018
  ident: b0330
  article-title: Pharmacokinetics, pharmacodynamics, and safety of EDP-305, in healthy and presumptive NAFLD subjects
  publication-title: J Hepatol
– volume: 293
  start-page: 18180
  year: 2018
  end-page: 18191
  ident: b0140
  article-title: Ligand binding and heterodimerization with retinoid X receptor α (RXRα) induce farnesoid X receptor (FXR) conformational changes affecting coactivator binding
  publication-title: J Biol Chem
– volume: 215
  start-page: 383
  year: 2018
  end-page: 396
  ident: b0055
  article-title: Bile acids in glucose metabolism in health and disease
  publication-title: J Exp Med
– volume: 22
  start-page: 5827
  year: 2003
  end-page: 5840
  ident: b0135
  article-title: Structure of the heterodimeric ecdysone receptor DNA-binding complex
  publication-title: Embo J
– volume: 3
  start-page: 543
  year: 1999
  end-page: 553
  ident: b0235
  article-title: Endogenous bile acids are ligands for the nuclear receptor FXR/BAR
  publication-title: Mol Cell
– volume: 25
  start-page: 75
  year: 2018
  ident: b0095
  article-title: Jaundice revisited: recent advances in the diagnosis and treatment of inherited cholestatic liver diseases
  publication-title: J Biomed Sci
– volume: 1844
  start-page: 1684
  year: 2014
  end-page: 1693
  ident: b0205
  article-title: Conformational dynamics of human FXR-LBD ligand interactions studied by hydrogen/deuterium exchange mass spectrometry: insights into the antagonism of the hypolipidemic agent Z-guggulsterone
  publication-title: Biochim Biophys Acta
– volume: 14
  start-page: 2188
  year: 2014
  end-page: 2205
  ident: b0385
  article-title: Medicinal chemistry and pharmacological effects of Farnesoid X Receptor (FXR) antagonists
  publication-title: Curr Top Med Chem
– volume: 70
  start-page: 788
  year: 2019
  end-page: 801
  ident: b0365
  article-title: The nonsteroidal farnesoid X receptor agonist cilofexor (GS-9674) improves markers of cholestasis and liver injury in patients with primary sclerosing cholangitis
  publication-title: Hepatology
– volume: 275
  start-page: 10918
  year: 2000
  end-page: 10924
  ident: b0035
  article-title: Farnesoid X receptor responds to bile acids and represses cholesterol 7alpha-hydroxylase gene (CYP7A1) transcription
  publication-title: J Biol Chem
– volume: 385
  start-page: 956
  year: 2015
  end-page: 965
  ident: b0260
  article-title: Farnesoid X nuclear receptor ligand obeticholic acid for non-cirrhotic, non-alcoholic steatohepatitis (FLINT): a multicentre, randomised, placebo-controlled trial
  publication-title: Lancet
– volume: 95
  year: 2020
  ident: b0515
  article-title: Andrographolide: chemical modification and its effect on biological activities
  publication-title: Bioorg Chem
– volume: 278
  start-page: 104
  year: 2003
  end-page: 110
  ident: b0020
  article-title: Natural structural variants of the nuclear receptor farnesoid X receptor affect transcriptional activation
  publication-title: J Biol Chem
– volume: 57
  start-page: 8477
  year: 2014
  end-page: 8495
  ident: b0420
  article-title: Exploitation of cholane scaffold for the discovery of potent and selective farnesoid X receptor (FXR) and G-protein coupled bile acid receptor 1 (GP-BAR1) ligands
  publication-title: J Med Chem
– volume: 256
  start-page: 167
  year: 2019
  end-page: 205
  ident: b0360
  article-title: Nonsteroidal FXR ligands: current status and clinical applications
  publication-title: Handb Exp Pharmacol
– volume: 37
  start-page: 136
  year: 2018
  ident: b0100
  article-title: Up-regulation of FGF15/19 signaling promotes hepatocellular carcinoma in the background of fatty liver
  publication-title: J Exp Clin Cancer Res
– volume: 147
  start-page: 1417
  year: 2014
  end-page: 1428
  ident: b0340
  article-title: The bile acid receptor TGR5 activates the TRPA1 channel to induce itch in mice
  publication-title: Gastroenterology
– volume: 85
  start-page: 126
  year: 2018
  end-page: 138
  ident: b0450
  article-title: HS218 as an FXR antagonist suppresses gluconeogenesis by inhibiting FXR binding to PGC-1α promoter
  publication-title: Metabolism
– volume: 2
  start-page: 217
  year: 2005
  end-page: 225
  ident: b0050
  article-title: Fibroblast growth factor 15 functions as an enterohepatic signal to regulate bile acid homeostasis
  publication-title: Cell Metab
– volume: 63
  start-page: 25
  year: 2019
  ident: b0455
  article-title: Capsaicin improves glucose tolerance and insulin sensitivity through modulation of the gut microbiota-bile acid-FXR axis in type 2 diabetic db/db Mice
  publication-title: Mol Nutr Food Res
– volume: 9
  year: 2014
  ident: b0015
  article-title: Hepatic farnesoid X-receptor isoforms α2 and α4 differentially modulate bile salt and lipoprotein metabolism in mice
  publication-title: PLoS One
– volume: 394
  start-page: 2184
  year: 2019
  end-page: 2196
  ident: b0255
  article-title: Obeticholic acid for the treatment of non-alcoholic steatohepatitis: interim analysis from a multicentre, randomised, placebo-controlled phase 3 trial
  publication-title: Lancet
– volume: 6
  year: 2015
  ident: b0500
  article-title: Intestine-selective farnesoid X receptor inhibition improves obesity-related metabolic dysfunction
  publication-title: Nat Commun
– volume: 105
  start-page: 5337
  year: 2008
  end-page: 5342
  ident: b0545
  article-title: Identification of a potent synthetic FXR agonist with an unexpected mode of binding and activation
  publication-title: Proc Natl Acad Sci U S A
– volume: 6
  start-page: 140
  year: 2018
  ident: b0180
  article-title: Discovery of natural products as novel and potent FXR antagonists by virtual screening
  publication-title: Front Chem
– volume: 88
  year: 2020
  ident: b0300
  article-title: A randomized, double-blind, multicenter, phase 2b study to evaluate the safety and efficacy of a combination of tropifexor and cenicriviroc in patients with nonalcoholic steatohepatitis and liver fibrosis: study design of the TANDEM trial
  publication-title: Contemp Clin Trials
– volume: 49
  start-page: 151
  year: 2009
  end-page: 159
  ident: b0060
  article-title: Low retinol levels differentially modulate bile salt-induced expression of human and mouse hepatic bile salt transporters
  publication-title: Hepatology
– volume: 10
  start-page: 31622
  year: 2020
  ident: b0290
  article-title: Combination therapies including cilofexor and firsocostat for bridging fibrosis and cirrhosis due to NASH
  publication-title: Hepatology
– volume: 7
  year: 2016
  ident: b0090
  article-title: Mutations in the nuclear bile acid receptor FXR cause progressive familial intrahepatic cholestasis
  publication-title: Nat Commun
– volume: 31
  start-page: 572
  year: 2006
  end-page: 580
  ident: b0005
  article-title: FXR, a multipurpose nuclear receptor
  publication-title: Trends Biochem Sci
– volume: 72
  start-page: 58
  year: 2020
  end-page: 71
  ident: b0285
  article-title: Cilofexor, a nonsteroidal FXR agonist, in patients with noncirrhotic NASH: a phase 2 randomized controlled trial
  publication-title: Hepatology
– volume: 18
  start-page: 721
  year: 2017
  end-page: 725
  ident: b0215
  article-title: A novel class of natural FXR modulators with a unique mode of selective co-regulator assembly
  publication-title: ChemBioChem
– volume: 290
  start-page: 19888
  year: 2015
  end-page: 19899
  ident: b0225
  article-title: Structural basis for small molecule NDB (N-Benzyl-N-(3-(tert-butyl)-4-hydroxyphenyl)-2,6-dichloro-4-(dimethylamino) Benzamide) as a selective antagonist of farnesoid X receptor α (FXRα) in stabilizing the homodimerization of the receptor
  publication-title: J Biol Chem
– volume: 11
  start-page: 1079
  year: 2003
  end-page: 1092
  ident: b0165
  article-title: A chemical, genetic, and structural analysis of the nuclear bile acid receptor FXR
  publication-title: Mol Cell
– volume: 293
  start-page: 12535
  year: 2018
  end-page: 12541
  ident: b0170
  article-title: Structural insights into the heterodimeric complex of the nuclear receptors FXR and RXR
  publication-title: J Biol Chem
– reference: Künnemann K, The Liver Meeting 2016 - American Association for the Study of Liver Diseases, 67th Annual Meeting (November 11-15, 2016 - Boston, Massachusetts, USA): Drugs Today (Barc). 2016 Dec;52(12):673-680. DOI:10.1358/dot.2016.52.12.2571703.
– volume: 26
  start-page: 4240
  year: 2018
  end-page: 4253
  ident: b0480
  article-title: Structural optimization and in vitro profiling of N-phenylbenzamide-based farnesoid X receptor antagonists
  publication-title: Bioorg Med Chem
– volume: 145
  start-page: 574
  year: 2013
  end-page: 582
  ident: b0250
  article-title: Efficacy and safety of the farnesoid X receptor agonist obeticholic acid in patients with type 2 diabetes and nonalcoholic fatty liver disease
  publication-title: Gastroenterology
– volume: 148
  start-page: 751
  year: 2015
  end-page: 761
  ident: b0525
  article-title: Efficacy of obeticholic acid in patients with primary biliary cirrhosis and inadequate response to ursodeoxycholic acid
  publication-title: Gastroenterology
– volume: 276
  start-page: 28857
  year: 2001
  end-page: 28865
  ident: b0070
  article-title: Human bile salt export pump promoter is transactivated by the farnesoid X receptor/bile acid receptor
  publication-title: J Biol Chem
– volume: 7
  start-page: 12502
  year: 2017
  ident: b0110
  article-title: The FXR agonist, obeticholic acid, suppresses HCC proliferation & metastasis: role of IL-6/STAT3 signalling pathway
  publication-title: Sci Rep
– volume: 10
  start-page: 2915
  year: 2019
  ident: b0190
  article-title: Molecular tuning of farnesoid X receptor partial agonism
  publication-title: Nat Commun
– volume: 52
  start-page: 904
  year: 2009
  end-page: 907
  ident: b0280
  article-title: Discovery of XL335 (WAY-362450), a highly potent, selective, and orally active agonist of the farnesoid X receptor (FXR)
  publication-title: J Med Chem
– volume: 723
  start-page: 108
  year: 2014
  end-page: 115
  ident: b0475
  article-title: Effects of a farnesoid X receptor antagonist on hepatic lipid metabolism in primates
  publication-title: Eur J Pharmacol
– volume: 1864
  start-page: 1335
  year: 2018
  end-page: 1344
  ident: b0115
  article-title: Differential effects of FXR or TGR5 activation in cholangiocarcinoma progression
  publication-title: Biochim Biophys Acta Mol Basis Dis
– volume: 17
  start-page: 536
  year: 2016
  ident: b0390
  article-title: Structural investigation for optimization of anthranilic acid derivatives as partial FXR agonists by in silico approaches
  publication-title: Int J Mol Sci
– volume: 29
  start-page: 623
  year: 2020
  end-page: 632
  ident: b0230
  article-title: Bile acid modulators for the treatment of nonalcoholic steatohepatitis (NASH)
  publication-title: Expert Opin Investig Drugs
– volume: 587
  start-page: 499
  year: 2020
  end-page: 504
  ident: b0555
  article-title: Structural basis of GPBAR activation and bile acid recognition
  publication-title: Nature
– volume: 102
  start-page: 731
  year: 2000
  end-page: 744
  ident: b0350
  article-title: Targeted disruption of the nuclear receptor FXR/BAR impairs bile acid and lipid homeostasis
  publication-title: Cell
– volume: 55
  start-page: 7037
  year: 2012
  end-page: 7053
  ident: b0470
  article-title: Discovery and optimization of 1,3,4-trisubstituted-pyrazolone derivatives as novel, potent, and nonsteroidal farnesoid X receptor (FXR) selective antagonists
  publication-title: J Med Chem
– volume: 60
  start-page: 9960
  year: 2017
  end-page: 9973
  ident: b0295
  article-title: Discovery of tropifexor (LJN452), a highly potent non-bile acid FXR agonist for the treatment of cholestatic liver diseases and nonalcoholic steatohepatitis (NASH)
  publication-title: J Med Chem
– volume: 275
  start-page: 10638
  year: 2000
  end-page: 10647
  ident: b0145
  article-title: Identification of the DNA binding specificity and potential target genes for the farnesoid X-activated receptor
  publication-title: J Biol Chem
– volume: 176
  start-page: 1098
  year: 2019
  end-page: 1112
  ident: b0030
  article-title: FXR regulates intestinal cancer stem cell proliferation
  publication-title: Cell
– volume: 51
  start-page: 1410
  year: 2010
  end-page: 1419
  ident: b0160
  article-title: Genome-wide tissue-specific farnesoid X receptor binding in mouse liver and intestine
  publication-title: Hepatology
– volume: 2
  start-page: 821
  year: 2018
  end-page: 835
  ident: b0265
  article-title: Molecular magnetic resonance imaging accurately measures the antifibrotic effect of EDP-305, a novel farnesoid X receptor agonist
  publication-title: Hepatol Commun
– volume: 58
  start-page: 9768
  year: 2015
  end-page: 9772
  ident: b0275
  article-title: Discovery of 6-(4-{[5-Cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl]methoxy}piperidin-1-yl)-1-methyl-1H-indole-3-carboxylic Acid: a novel FXR agonist for the treatment of dyslipidemia
  publication-title: J Med Chem
– volume: 3
  start-page: 1191
  year: 2013
  end-page: 1212
  ident: b0245
  article-title: Bile acid metabolism and signaling
  publication-title: Compr Physiol
– volume: 378
  start-page: 681
  year: 1995
  end-page: 689
  ident: b0195
  article-title: Crystal structure of the RAR-gamma ligand-binding domain bound to all-trans retinoic acid
  publication-title: Nature
– volume: 70
  start-page: 276
  year: 2019
  end-page: 293
  ident: b0080
  article-title: Enhanced microbial bile acid deconjugation and impaired ileal uptake in pregnancy repress intestinal regulation of bile acid synthesis
  publication-title: Hepatology
– volume: 256
  start-page: 283
  year: 2019
  end-page: 295
  ident: b0345
  article-title: Obeticholic acid: an update of its pharmacological activities in liver disorders
  publication-title: Handb Exp Pharmacol
– volume: 9
  start-page: 6
  year: 2018
  ident: b0045
  article-title: Interaction of glucocorticoids with FXR/FGF19/FGF21-mediated ileum-liver crosstalk
  publication-title: Biochim Biophys Acta Mol Basis Dis
– volume: 109
  start-page: 961
  year: 2002
  end-page: 971
  ident: b0150
  article-title: Bile acid-activated nuclear receptor FXR suppresses apolipoprotein A-I transcription via a negative FXR response element
  publication-title: J Clin Invest
– volume: 534
  start-page: 1047
  year: 2021
  end-page: 1052
  ident: b0185
  article-title: Structural basis of tropifexor as a potent and selective agonist of farnesoid X receptor
  publication-title: Biochem Biophys Res Commun
– volume: 48
  start-page: 192
  year: 2008
  end-page: 199
  ident: b0320
  article-title: Enhancement of genotype 1 hepatitis C virus replication by bile acids through FXR
  publication-title: J Hepatol
– volume: 10
  start-page: 504
  year: 2019
  end-page: 510
  ident: b0490
  article-title: Investigation around the oxadiazole core in the discovery of a new chemotype of potent and selective FXR antagonists
  publication-title: ACS Med Chem Lett
– volume: 6
  start-page: 517
  year: 2000
  end-page: 526
  ident: b0040
  article-title: A regulatory cascade of the nuclear receptors FXR, SHP-1, and LRH-1 represses bile acid biosynthesis
  publication-title: Mol Cell
– volume: 10
  year: 2015
  ident: b0415
  article-title: Impaired itching perception in murine models of cholestasis is supported by dysregulation of GPBAR1 signaling
  publication-title: PLoS One
– volume: 22
  start-page: 2919
  year: 2014
  end-page: 2938
  ident: b0485
  article-title: Identification of trisubstituted-pyrazol carboxamide analogs as novel and potent antagonists of farnesoid X receptor
  publication-title: Bioorg Med Chem
– volume: 40
  start-page: 16
  year: 2015
  end-page: 24
  ident: b0200
  article-title: Nuclear receptor full-length architectures: confronting myth and illusion with high resolution
  publication-title: Trends Biochem Sci
– volume: 34
  start-page: 99
  year: 2018
  end-page: 119
  ident: b0210
  article-title: D3R Grand Challenge 2: blind prediction of protein-ligand poses, affinity rankings, and relative binding free energies
  publication-title: J Comput Aided Mol Des
– volume: 11
  start-page: 1093
  year: 2003
  end-page: 1100
  ident: b0175
  article-title: Structural basis for bile acid binding and activation of the nuclear receptor FXR
  publication-title: Mol Cell
– volume: 63
  start-page: 3868
  year: 2020
  end-page: 3880
  ident: b0305
  article-title: Nidufexor (LMB763), a novel FXR modulator for the treatment of nonalcoholic steatohepatitis
  publication-title: J Med Chem
– volume: 7
  start-page: 42801
  year: 2017
  ident: b0400
  article-title: BAR502, a dual FXR and GPBAR1 agonist, promotes browning of white adipose tissue and reverses liver steatosis and fibrosis
  publication-title: Sci Rep
– volume: 275
  start-page: 27
  year: 2014
  end-page: 38
  ident: b0495
  article-title: Muricholic bile acids are potent regulators of bile acid synthesis via a positive feedback mechanism
  publication-title: J Intern Med
– volume: 76
  start-page: 1221
  year: 2016
  end-page: 1226
  ident: b0120
  article-title: Obeticholic acid: first global approval
  publication-title: Drugs
– volume: 64
  start-page: 1158
  year: 2016
  end-page: 1166
  ident: b0065
  article-title: Gene expression profiling in human precision cut liver slices in response to the FXR agonist obeticholic acid
  publication-title: J Hepatol
– volume: 278
  start-page: 10214
  year: 2003
  end-page: 10220
  ident: b0505
  article-title: Guggulsterone is a farnesoid X receptor antagonist in coactivator association assays but acts to enhance transcription of bile salt export pump
  publication-title: J Biol Chem
– volume: 9
  year: 2014
  ident: b0155
  article-title: Genome-wide binding and transcriptome analysis of human farnesoid X receptor in primary human hepatocytes
  publication-title: PLoS One
– volume: 74
  start-page: 90
  year: 2011
  end-page: 94
  ident: b0520
  article-title: Tuberatolides, potent FXR antagonists from the Korean marine tunicate Botryllus tuberatus
  publication-title: J Nat Prod
– volume: 51
  start-page: 1831
  year: 2008
  end-page: 1841
  ident: b0540
  article-title: Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies
  publication-title: J Med Chem
– volume: 256
  start-page: 207
  year: 2019
  end-page: 234
  ident: b0240
  article-title: Potential of intestine-selective FXR modulation for treatment of metabolic disease
  publication-title: Handb Exp Pharmacol
– volume: 37
  start-page: 1628
  year: 2019
  end-page: 1640
  ident: b0425
  article-title: Computational study of the binding mechanism between farnesoid X receptor α and antagonist N-benzyl-N-(3-(tertbutyl)-4-hydroxyphenyl)-2,6-dichloro-4-(dimethylamino) benzamide
  publication-title: J Biomol Struct Dyn
– volume: 17
  start-page: 225
  year: 2013
  end-page: 235
  ident: b0310
  article-title: Gut microbiota regulates bile acid metabolism by reducing the levels of tauro-beta-muricholic acid, a naturally occurring FXR antagonist
  publication-title: Cell Metab
– volume: 67
  start-page: 1890
  year: 2018
  end-page: 1902
  ident: b0530
  article-title: A randomized trial of obeticholic acid monotherapy in patients with primary biliary cholangitis
  publication-title: Hepatology
– volume: 25
  start-page: 131
  year: 2008
  end-page: 143
  ident: b0010
  article-title: Analysis of nuclear receptor pseudogenes in vertebrates: how the silent tell their stories
  publication-title: Mol Biol Evol
– volume: 29
  start-page: 118
  year: 2018
  end-page: 137
  ident: b0395
  article-title: FXR/TGR5 dual agonist prevents progression of nephropathy in diabetes and obesity
  publication-title: J Am Soc Nephrol
– volume: 78
  start-page: 617
  year: 2010
  end-page: 630
  ident: b0405
  article-title: Functional characterization of the semisynthetic bile acid derivative INT-767, a dual farnesoid X receptor and TGR5 agonist
  publication-title: Mol Pharmacol
– volume: 4
  year: 2013
  ident: b0220
  article-title: The antiparasitic drug ivermectin is a novel FXR ligand that regulates metabolism
  publication-title: Nat Commun
– reference: Verbeke L, Nevens F and Laleman W, Steroidal or non-steroidal FXR agonists - Is that the question? Vol. 66(4). 2017: J Hepatol. 680-681.
– volume: 27
  start-page: 1876
  year: 2018
  end-page: 1892
  ident: b0125
  article-title: The nuclear receptor superfamily: a structural perspective
  publication-title: Protein Sci
– volume: 24
  start-page: 14549
  year: 2020
  end-page: 14560
  ident: b0105
  article-title: Farnesoid X receptor activation induces antitumour activity in colorectal cancer by suppressing JAK2/STAT3 signalling via transactivation of SOCS3 gene
  publication-title: J Cell Mol Med
– volume: 12
  start-page: 420
  year: 2021
  end-page: 425
  ident: b0510
  article-title: Discovery of orally active and nonsteroidal farnesoid X Receptor (FXR) antagonist with propensity for accumulation and responsiveness in ileum
  publication-title: ACS Med Chem Lett
– volume: 52
  start-page: 3043
  year: 2012
  end-page: 3052
  ident: b0355
  article-title: Unbinding pathways of GW4064 from human farnesoid X receptor as revealed by molecular dynamics simulations
  publication-title: J Chem Inf Model
– volume: 39
  start-page: 93
  year: 2017
  end-page: 103
  ident: b0075
  article-title: Pharmacotoxicology of clinically-relevant concentrations of obeticholic acid in an organotypic human hepatocyte system
  publication-title: Toxicol In Vitro
– volume: 8
  start-page: 842
  year: 2011
  end-page: 850
  ident: b0025
  article-title: Regulation of FXR transcriptional activity in health and disease: Emerging roles of FXR cofactors and post-translational modifications
  publication-title: Biochim Biophys Acta
– volume: 9
  start-page: 395
  year: 2020
  end-page: 410
  ident: b0370
  article-title: Safety, tolerability, pharmacokinetics, and pharmacodynamics of the novel non-bile acid FXR agonist tropifexor (LJN452) in healthy volunteers
  publication-title: Clin Pharmacol Drug Dev
– volume: 38
  start-page: 356
  year: 2019
  end-page: 370
  ident: b0440
  article-title: Guggulsterone, a farnesoid X receptor antagonist lowers plasma trimethylamine-N-oxide levels: an evidence from in vitro and in vivo studies
  publication-title: Hum Exp Toxicol
– volume: 10
  start-page: 1412
  year: 2019
  end-page: 1419
  ident: b0315
  article-title: Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool
  publication-title: Medchemcomm
– volume: 11
  start-page: 1132
  year: 2019
  ident: b0410
  article-title: Transcriptome analysis of dual FXR and GPBAR1 agonism in rodent model of NASH reveals modulation of lipid droplets formation
  publication-title: Nutrients
– volume: 296
  start-page: 1703
  year: 2002
  end-page: 1706
  ident: b0465
  article-title: A natural product that lowers cholesterol as an antagonist ligand for FXR
  publication-title: Science
– volume: 317
  start-page: G108
  year: 2019
  end-page: G115
  ident: b0085
  article-title: FXR agonist GW4064 improves liver and intestinal pathology and alters bile acid metabolism in rats undergoing small intestinal resection
  publication-title: Am J Physiol Gastrointest Liver Physiol
– volume: 59
  start-page: 6553
  year: 2016
  end-page: 6579
  ident: b0460
  article-title: Recent progress on bile acid receptor modulators for treatment of metabolic diseases
  publication-title: J Med Chem
– volume: 11
  start-page: 1478
  year: 2019
  ident: b0435
  article-title: Protein expression profiling identifies key proteins and pathways involved in growth inhibitory effects exerted by guggulsterone in human colorectal cancer cells
  publication-title: Cancers
– volume: 12
  start-page: 267
  year: 2021
  end-page: 274
  ident: b0375
  article-title: A new FXR ligand chemotype with agonist/antagonist switch
  publication-title: ACS Med Chem Lett
– volume: 7
  year: 2012
  ident: b0445
  article-title: Discovery that theonellasterol a marine sponge sterol is a highly selective FXR antagonist that protects against liver injury in cholestasis
  publication-title: PLoS One
– volume: 293
  start-page: 18180
  issue: 47
  year: 2018
  ident: 10.1016/j.csbj.2021.04.029_b0140
  article-title: Ligand binding and heterodimerization with retinoid X receptor α (RXRα) induce farnesoid X receptor (FXR) conformational changes affecting coactivator binding
  publication-title: J Biol Chem
  doi: 10.1074/jbc.RA118.004652
– volume: 68
  start-page: S584
  issue: S1
  year: 2018
  ident: 10.1016/j.csbj.2021.04.029_b0330
  article-title: Pharmacokinetics, pharmacodynamics, and safety of EDP-305, in healthy and presumptive NAFLD subjects
  publication-title: J Hepatol
  doi: 10.1016/S0168-8278(18)31427-2
– volume: 48
  start-page: 192
  issue: 2
  year: 2008
  ident: 10.1016/j.csbj.2021.04.029_b0320
  article-title: Enhancement of genotype 1 hepatitis C virus replication by bile acids through FXR
  publication-title: J Hepatol
  doi: 10.1016/j.jhep.2007.09.015
– volume: 26
  start-page: 4240
  issue: 14
  year: 2018
  ident: 10.1016/j.csbj.2021.04.029_b0480
  article-title: Structural optimization and in vitro profiling of N-phenylbenzamide-based farnesoid X receptor antagonists
  publication-title: Bioorg Med Chem
  doi: 10.1016/j.bmc.2018.07.017
– volume: 31
  start-page: 572
  issue: 10
  year: 2006
  ident: 10.1016/j.csbj.2021.04.029_b0005
  article-title: FXR, a multipurpose nuclear receptor
  publication-title: Trends Biochem Sci
  doi: 10.1016/j.tibs.2006.08.002
– volume: 70
  start-page: 788
  issue: 3
  year: 2019
  ident: 10.1016/j.csbj.2021.04.029_b0365
  article-title: The nonsteroidal farnesoid X receptor agonist cilofexor (GS-9674) improves markers of cholestasis and liver injury in patients with primary sclerosing cholangitis
  publication-title: Hepatology
  doi: 10.1002/hep.30509
– volume: 1864
  start-page: 1335
  issue: 4 Pt B
  year: 2018
  ident: 10.1016/j.csbj.2021.04.029_b0115
  article-title: Differential effects of FXR or TGR5 activation in cholangiocarcinoma progression
  publication-title: Biochim Biophys Acta Mol Basis Dis
  doi: 10.1016/j.bbadis.2017.08.016
– volume: 278
  start-page: 10214
  issue: 12
  year: 2003
  ident: 10.1016/j.csbj.2021.04.029_b0505
  article-title: Guggulsterone is a farnesoid X receptor antagonist in coactivator association assays but acts to enhance transcription of bile salt export pump
  publication-title: J Biol Chem
  doi: 10.1074/jbc.M209323200
– volume: 10
  start-page: 504
  issue: 4
  year: 2019
  ident: 10.1016/j.csbj.2021.04.029_b0490
  article-title: Investigation around the oxadiazole core in the discovery of a new chemotype of potent and selective FXR antagonists
  publication-title: ACS Med Chem Lett
  doi: 10.1021/acsmedchemlett.8b00534
– volume: 29
  start-page: 623
  issue: 6
  year: 2020
  ident: 10.1016/j.csbj.2021.04.029_b0230
  article-title: Bile acid modulators for the treatment of nonalcoholic steatohepatitis (NASH)
  publication-title: Expert Opin Investig Drugs
  doi: 10.1080/13543784.2020.1763302
– volume: 49
  start-page: 151
  issue: 1
  year: 2009
  ident: 10.1016/j.csbj.2021.04.029_b0060
  article-title: Low retinol levels differentially modulate bile salt-induced expression of human and mouse hepatic bile salt transporters
  publication-title: Hepatology
  doi: 10.1002/hep.22661
– volume: 11
  start-page: 1247
  year: 2020
  ident: 10.1016/j.csbj.2021.04.029_b0430
  article-title: Farnesoid X receptor agonists as therapeutic target for cardiometabolic diseases
  publication-title: Front Pharmacol
  doi: 10.3389/fphar.2020.01247
– volume: 12
  start-page: 267
  issue: 2
  year: 2021
  ident: 10.1016/j.csbj.2021.04.029_b0375
  article-title: A new FXR ligand chemotype with agonist/antagonist switch
  publication-title: ACS Med Chem Lett
  doi: 10.1021/acsmedchemlett.0c00647
– volume: 275
  start-page: 10918
  issue: 15
  year: 2000
  ident: 10.1016/j.csbj.2021.04.029_b0035
  article-title: Farnesoid X receptor responds to bile acids and represses cholesterol 7alpha-hydroxylase gene (CYP7A1) transcription
  publication-title: J Biol Chem
  doi: 10.1074/jbc.275.15.10918
– volume: 9
  start-page: 6
  issue: 10
  year: 2018
  ident: 10.1016/j.csbj.2021.04.029_b0045
  article-title: Interaction of glucocorticoids with FXR/FGF19/FGF21-mediated ileum-liver crosstalk
  publication-title: Biochim Biophys Acta Mol Basis Dis
– volume: 18
  start-page: 721
  issue: 8
  year: 2017
  ident: 10.1016/j.csbj.2021.04.029_b0215
  article-title: A novel class of natural FXR modulators with a unique mode of selective co-regulator assembly
  publication-title: ChemBioChem
  doi: 10.1002/cbic.201700059
– volume: 147
  start-page: 1417
  issue: 6
  year: 2014
  ident: 10.1016/j.csbj.2021.04.029_b0340
  article-title: The bile acid receptor TGR5 activates the TRPA1 channel to induce itch in mice
  publication-title: Gastroenterology
  doi: 10.1053/j.gastro.2014.08.042
– volume: 59
  start-page: 6553
  issue: 14
  year: 2016
  ident: 10.1016/j.csbj.2021.04.029_b0460
  article-title: Recent progress on bile acid receptor modulators for treatment of metabolic diseases
  publication-title: J Med Chem
  doi: 10.1021/acs.jmedchem.5b00342
– volume: 64
  start-page: 1158
  issue: 5
  year: 2016
  ident: 10.1016/j.csbj.2021.04.029_b0065
  article-title: Gene expression profiling in human precision cut liver slices in response to the FXR agonist obeticholic acid
  publication-title: J Hepatol
  doi: 10.1016/j.jhep.2016.01.016
– volume: 88
  year: 2020
  ident: 10.1016/j.csbj.2021.04.029_b0300
  article-title: A randomized, double-blind, multicenter, phase 2b study to evaluate the safety and efficacy of a combination of tropifexor and cenicriviroc in patients with nonalcoholic steatohepatitis and liver fibrosis: study design of the TANDEM trial
  publication-title: Contemp Clin Trials
  doi: 10.1016/j.cct.2019.105889
– volume: 7
  issue: 10713
  year: 2016
  ident: 10.1016/j.csbj.2021.04.029_b0090
  article-title: Mutations in the nuclear bile acid receptor FXR cause progressive familial intrahepatic cholestasis
  publication-title: Nat Commun
– volume: 39
  start-page: 93
  year: 2017
  ident: 10.1016/j.csbj.2021.04.029_b0075
  article-title: Pharmacotoxicology of clinically-relevant concentrations of obeticholic acid in an organotypic human hepatocyte system
  publication-title: Toxicol In Vitro
  doi: 10.1016/j.tiv.2016.11.014
– volume: 78
  start-page: 617
  issue: 4
  year: 2010
  ident: 10.1016/j.csbj.2021.04.029_b0405
  article-title: Functional characterization of the semisynthetic bile acid derivative INT-767, a dual farnesoid X receptor and TGR5 agonist
  publication-title: Mol Pharmacol
  doi: 10.1124/mol.110.064501
– volume: 51
  start-page: 1410
  issue: 4
  year: 2010
  ident: 10.1016/j.csbj.2021.04.029_b0160
  article-title: Genome-wide tissue-specific farnesoid X receptor binding in mouse liver and intestine
  publication-title: Hepatology
  doi: 10.1002/hep.23450
– volume: 74
  start-page: 90
  issue: 1
  year: 2011
  ident: 10.1016/j.csbj.2021.04.029_b0520
  article-title: Tuberatolides, potent FXR antagonists from the Korean marine tunicate Botryllus tuberatus
  publication-title: J Nat Prod
  doi: 10.1021/np100489u
– volume: 72
  start-page: 58
  issue: 1
  year: 2020
  ident: 10.1016/j.csbj.2021.04.029_b0285
  article-title: Cilofexor, a nonsteroidal FXR agonist, in patients with noncirrhotic NASH: a phase 2 randomized controlled trial
  publication-title: Hepatology
  doi: 10.1002/hep.31205
– volume: 58
  start-page: 9768
  issue: 24
  year: 2015
  ident: 10.1016/j.csbj.2021.04.029_b0275
  article-title: Discovery of 6-(4-{[5-Cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl]methoxy}piperidin-1-yl)-1-methyl-1H-indole-3-carboxylic Acid: a novel FXR agonist for the treatment of dyslipidemia
  publication-title: J Med Chem
  doi: 10.1021/acs.jmedchem.5b01161
– volume: 22
  start-page: 5827
  issue: 21
  year: 2003
  ident: 10.1016/j.csbj.2021.04.029_b0135
  article-title: Structure of the heterodimeric ecdysone receptor DNA-binding complex
  publication-title: Embo J
  doi: 10.1093/emboj/cdg569
– volume: 587
  start-page: 499
  issue: 7834
  year: 2020
  ident: 10.1016/j.csbj.2021.04.029_b0555
  article-title: Structural basis of GPBAR activation and bile acid recognition
  publication-title: Nature
  doi: 10.1038/s41586-020-2569-1
– volume: 102
  start-page: 731
  issue: 6
  year: 2000
  ident: 10.1016/j.csbj.2021.04.029_b0350
  article-title: Targeted disruption of the nuclear receptor FXR/BAR impairs bile acid and lipid homeostasis
  publication-title: Cell
  doi: 10.1016/S0092-8674(00)00062-3
– volume: 61
  start-page: 1214
  issue: 5
  year: 2016
  ident: 10.1016/j.csbj.2021.04.029_b0535
  article-title: Global epidemiology of nonalcoholic fatty liver disease and perspectives on US minority populations
  publication-title: Dig Dis Sci
  doi: 10.1007/s10620-016-4143-0
– volume: 2
  start-page: 821
  issue: 7
  year: 2018
  ident: 10.1016/j.csbj.2021.04.029_b0265
  article-title: Molecular magnetic resonance imaging accurately measures the antifibrotic effect of EDP-305, a novel farnesoid X receptor agonist
  publication-title: Hepatol Commun
  doi: 10.1002/hep4.1193
– volume: 52
  start-page: 904
  issue: 4
  year: 2009
  ident: 10.1016/j.csbj.2021.04.029_b0280
  article-title: Discovery of XL335 (WAY-362450), a highly potent, selective, and orally active agonist of the farnesoid X receptor (FXR)
  publication-title: J Med Chem
  doi: 10.1021/jm8014124
– volume: 296
  start-page: 1703
  issue: 5573
  year: 2002
  ident: 10.1016/j.csbj.2021.04.029_b0465
  article-title: A natural product that lowers cholesterol as an antagonist ligand for FXR
  publication-title: Science
  doi: 10.1126/science.1072891
– volume: 215
  start-page: 383
  issue: 2
  year: 2018
  ident: 10.1016/j.csbj.2021.04.029_b0055
  article-title: Bile acids in glucose metabolism in health and disease
  publication-title: J Exp Med
  doi: 10.1084/jem.20171965
– volume: 275
  start-page: 10638
  issue: 14
  year: 2000
  ident: 10.1016/j.csbj.2021.04.029_b0145
  article-title: Identification of the DNA binding specificity and potential target genes for the farnesoid X-activated receptor
  publication-title: J Biol Chem
  doi: 10.1074/jbc.275.14.10638
– volume: 54
  start-page: 1303
  issue: 4
  year: 2011
  ident: 10.1016/j.csbj.2021.04.029_b0550
  article-title: Dual farnesoid X receptor/TGR5 agonist INT-767 reduces liver injury in the Mdr2-/- (Abcb4-/-) mouse cholangiopathy model by promoting biliary HCO−3 output
  publication-title: Hepatology
  doi: 10.1002/hep.24537
– volume: 256
  start-page: 283
  year: 2019
  ident: 10.1016/j.csbj.2021.04.029_b0345
  article-title: Obeticholic acid: an update of its pharmacological activities in liver disorders
  publication-title: Handb Exp Pharmacol
  doi: 10.1007/164_2019_227
– volume: 7
  start-page: 42801
  year: 2017
  ident: 10.1016/j.csbj.2021.04.029_b0400
  article-title: BAR502, a dual FXR and GPBAR1 agonist, promotes browning of white adipose tissue and reverses liver steatosis and fibrosis
  publication-title: Sci Rep
  doi: 10.1038/srep42801
– volume: 723
  start-page: 108
  year: 2014
  ident: 10.1016/j.csbj.2021.04.029_b0475
  article-title: Effects of a farnesoid X receptor antagonist on hepatic lipid metabolism in primates
  publication-title: Eur J Pharmacol
  doi: 10.1016/j.ejphar.2013.10.048
– volume: 145
  start-page: 574
  issue: 3
  year: 2013
  ident: 10.1016/j.csbj.2021.04.029_b0250
  article-title: Efficacy and safety of the farnesoid X receptor agonist obeticholic acid in patients with type 2 diabetes and nonalcoholic fatty liver disease
  publication-title: Gastroenterology
  doi: 10.1053/j.gastro.2013.05.042
– volume: 14
  start-page: 2188
  issue: 19
  year: 2014
  ident: 10.1016/j.csbj.2021.04.029_b0385
  article-title: Medicinal chemistry and pharmacological effects of Farnesoid X Receptor (FXR) antagonists
  publication-title: Curr Top Med Chem
  doi: 10.2174/1568026614666141112103516
– volume: 534
  start-page: 1047
  year: 2021
  ident: 10.1016/j.csbj.2021.04.029_b0185
  article-title: Structural basis of tropifexor as a potent and selective agonist of farnesoid X receptor
  publication-title: Biochem Biophys Res Commun
  doi: 10.1016/j.bbrc.2020.10.039
– volume: 10
  start-page: 1412
  issue: 8
  year: 2019
  ident: 10.1016/j.csbj.2021.04.029_b0315
  article-title: Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool
  publication-title: Medchemcomm
  doi: 10.1039/C9MD00264B
– volume: 55
  start-page: 7037
  issue: 16
  year: 2012
  ident: 10.1016/j.csbj.2021.04.029_b0470
  article-title: Discovery and optimization of 1,3,4-trisubstituted-pyrazolone derivatives as novel, potent, and nonsteroidal farnesoid X receptor (FXR) selective antagonists
  publication-title: J Med Chem
  doi: 10.1021/jm3002718
– volume: 317
  start-page: G108
  issue: 2
  year: 2019
  ident: 10.1016/j.csbj.2021.04.029_b0085
  article-title: FXR agonist GW4064 improves liver and intestinal pathology and alters bile acid metabolism in rats undergoing small intestinal resection
  publication-title: Am J Physiol Gastrointest Liver Physiol
  doi: 10.1152/ajpgi.00356.2017
– volume: 60
  start-page: 9960
  issue: 24
  year: 2017
  ident: 10.1016/j.csbj.2021.04.029_b0295
  article-title: Discovery of tropifexor (LJN452), a highly potent non-bile acid FXR agonist for the treatment of cholestatic liver diseases and nonalcoholic steatohepatitis (NASH)
  publication-title: J Med Chem
  doi: 10.1021/acs.jmedchem.7b00907
– volume: 109
  start-page: 961
  issue: 7
  year: 2002
  ident: 10.1016/j.csbj.2021.04.029_b0150
  article-title: Bile acid-activated nuclear receptor FXR suppresses apolipoprotein A-I transcription via a negative FXR response element
  publication-title: J Clin Invest
  doi: 10.1172/JCI0214505
– volume: 9
  issue: 9
  year: 2014
  ident: 10.1016/j.csbj.2021.04.029_b0155
  article-title: Genome-wide binding and transcriptome analysis of human farnesoid X receptor in primary human hepatocytes
  publication-title: PLoS One
  doi: 10.1371/journal.pone.0105930
– volume: 11
  start-page: 1132
  issue: 5
  year: 2019
  ident: 10.1016/j.csbj.2021.04.029_b0410
  article-title: Transcriptome analysis of dual FXR and GPBAR1 agonism in rodent model of NASH reveals modulation of lipid droplets formation
  publication-title: Nutrients
  doi: 10.3390/nu11051132
– volume: 11
  start-page: 1079
  issue: 4
  year: 2003
  ident: 10.1016/j.csbj.2021.04.029_b0165
  article-title: A chemical, genetic, and structural analysis of the nuclear bile acid receptor FXR
  publication-title: Mol Cell
  doi: 10.1016/S1097-2765(03)00104-7
– volume: 6
  issue: 10166
  year: 2015
  ident: 10.1016/j.csbj.2021.04.029_b0500
  article-title: Intestine-selective farnesoid X receptor inhibition improves obesity-related metabolic dysfunction
  publication-title: Nat Commun
– volume: 34
  start-page: 99
  issue: 2
  year: 2018
  ident: 10.1016/j.csbj.2021.04.029_b0210
  article-title: D3R Grand Challenge 2: blind prediction of protein-ligand poses, affinity rankings, and relative binding free energies
  publication-title: J Comput Aided Mol Des
– volume: 17
  start-page: 536
  issue: 4
  year: 2016
  ident: 10.1016/j.csbj.2021.04.029_b0390
  article-title: Structural investigation for optimization of anthranilic acid derivatives as partial FXR agonists by in silico approaches
  publication-title: Int J Mol Sci
  doi: 10.3390/ijms17040536
– volume: 27
  start-page: 1876
  issue: 11
  year: 2018
  ident: 10.1016/j.csbj.2021.04.029_b0125
  article-title: The nuclear receptor superfamily: a structural perspective
  publication-title: Protein Sci
  doi: 10.1002/pro.3496
– volume: 25
  start-page: 131
  issue: 1
  year: 2008
  ident: 10.1016/j.csbj.2021.04.029_b0010
  article-title: Analysis of nuclear receptor pseudogenes in vertebrates: how the silent tell their stories
  publication-title: Mol Biol Evol
  doi: 10.1093/molbev/msm251
– volume: 11
  start-page: 1478
  issue: 10
  year: 2019
  ident: 10.1016/j.csbj.2021.04.029_b0435
  article-title: Protein expression profiling identifies key proteins and pathways involved in growth inhibitory effects exerted by guggulsterone in human colorectal cancer cells
  publication-title: Cancers
  doi: 10.3390/cancers11101478
– volume: 24
  start-page: 14549
  issue: 24
  year: 2020
  ident: 10.1016/j.csbj.2021.04.029_b0105
  article-title: Farnesoid X receptor activation induces antitumour activity in colorectal cancer by suppressing JAK2/STAT3 signalling via transactivation of SOCS3 gene
  publication-title: J Cell Mol Med
  doi: 10.1111/jcmm.16083
– volume: 10
  start-page: 31622
  issue: 10
  year: 2020
  ident: 10.1016/j.csbj.2021.04.029_b0290
  article-title: Combination therapies including cilofexor and firsocostat for bridging fibrosis and cirrhosis due to NASH
  publication-title: Hepatology
– volume: 12
  start-page: 420
  issue: 3
  year: 2021
  ident: 10.1016/j.csbj.2021.04.029_b0510
  article-title: Discovery of orally active and nonsteroidal farnesoid X Receptor (FXR) antagonist with propensity for accumulation and responsiveness in ileum
  publication-title: ACS Med Chem Lett
  doi: 10.1021/acsmedchemlett.0c00640
– volume: 6
  start-page: 140
  year: 2018
  ident: 10.1016/j.csbj.2021.04.029_b0180
  article-title: Discovery of natural products as novel and potent FXR antagonists by virtual screening
  publication-title: Front Chem
  doi: 10.3389/fchem.2018.00140
– volume: 52
  start-page: 3043
  issue: 11
  year: 2012
  ident: 10.1016/j.csbj.2021.04.029_b0355
  article-title: Unbinding pathways of GW4064 from human farnesoid X receptor as revealed by molecular dynamics simulations
  publication-title: J Chem Inf Model
  doi: 10.1021/ci300459k
– volume: 63
  start-page: 3868
  issue: 8
  year: 2020
  ident: 10.1016/j.csbj.2021.04.029_b0305
  article-title: Nidufexor (LMB763), a novel FXR modulator for the treatment of nonalcoholic steatohepatitis
  publication-title: J Med Chem
  doi: 10.1021/acs.jmedchem.9b01621
– volume: 37
  start-page: 136
  issue: 1
  year: 2018
  ident: 10.1016/j.csbj.2021.04.029_b0100
  article-title: Up-regulation of FGF15/19 signaling promotes hepatocellular carcinoma in the background of fatty liver
  publication-title: J Exp Clin Cancer Res
  doi: 10.1186/s13046-018-0781-8
– volume: 290
  start-page: 19888
  issue: 32
  year: 2015
  ident: 10.1016/j.csbj.2021.04.029_b0225
  article-title: Structural basis for small molecule NDB (N-Benzyl-N-(3-(tert-butyl)-4-hydroxyphenyl)-2,6-dichloro-4-(dimethylamino) Benzamide) as a selective antagonist of farnesoid X receptor α (FXRα) in stabilizing the homodimerization of the receptor
  publication-title: J Biol Chem
  doi: 10.1074/jbc.M114.630475
– volume: 394
  start-page: 2184
  issue: 10215
  year: 2019
  ident: 10.1016/j.csbj.2021.04.029_b0255
  article-title: Obeticholic acid for the treatment of non-alcoholic steatohepatitis: interim analysis from a multicentre, randomised, placebo-controlled phase 3 trial
  publication-title: Lancet
  doi: 10.1016/S0140-6736(19)33041-7
– volume: 98
  start-page: 245
  issue: 3
  year: 2010
  ident: 10.1016/j.csbj.2021.04.029_b0130
  article-title: Two farnesoid X receptor alpha isoforms in Japanese medaka (Oryzias latipes) are differentially activated in vitro
  publication-title: Aquat Toxicol
  doi: 10.1016/j.aquatox.2010.02.020
– volume: 9
  issue: 12
  year: 2014
  ident: 10.1016/j.csbj.2021.04.029_b0015
  article-title: Hepatic farnesoid X-receptor isoforms α2 and α4 differentially modulate bile salt and lipoprotein metabolism in mice
  publication-title: PLoS One
  doi: 10.1371/journal.pone.0115028
– volume: 256
  start-page: 167
  year: 2019
  ident: 10.1016/j.csbj.2021.04.029_b0360
  article-title: Nonsteroidal FXR ligands: current status and clinical applications
  publication-title: Handb Exp Pharmacol
  doi: 10.1007/164_2019_232
– volume: 22
  start-page: 2919
  issue: 11
  year: 2014
  ident: 10.1016/j.csbj.2021.04.029_b0485
  article-title: Identification of trisubstituted-pyrazol carboxamide analogs as novel and potent antagonists of farnesoid X receptor
  publication-title: Bioorg Med Chem
  doi: 10.1016/j.bmc.2014.04.014
– volume: 2
  start-page: 217
  issue: 4
  year: 2005
  ident: 10.1016/j.csbj.2021.04.029_b0050
  article-title: Fibroblast growth factor 15 functions as an enterohepatic signal to regulate bile acid homeostasis
  publication-title: Cell Metab
  doi: 10.1016/j.cmet.2005.09.001
– volume: 6
  start-page: 517
  issue: 3
  year: 2000
  ident: 10.1016/j.csbj.2021.04.029_b0040
  article-title: A regulatory cascade of the nuclear receptors FXR, SHP-1, and LRH-1 represses bile acid biosynthesis
  publication-title: Mol Cell
  doi: 10.1016/S1097-2765(00)00051-4
– volume: 85
  start-page: 126
  year: 2018
  ident: 10.1016/j.csbj.2021.04.029_b0450
  article-title: HS218 as an FXR antagonist suppresses gluconeogenesis by inhibiting FXR binding to PGC-1α promoter
  publication-title: Metabolism
  doi: 10.1016/j.metabol.2018.03.016
– volume: 4
  issue: 1937
  year: 2013
  ident: 10.1016/j.csbj.2021.04.029_b0220
  article-title: The antiparasitic drug ivermectin is a novel FXR ligand that regulates metabolism
  publication-title: Nat Commun
– volume: 385
  start-page: 956
  issue: 9972
  year: 2015
  ident: 10.1016/j.csbj.2021.04.029_b0260
  article-title: Farnesoid X nuclear receptor ligand obeticholic acid for non-cirrhotic, non-alcoholic steatohepatitis (FLINT): a multicentre, randomised, placebo-controlled trial
  publication-title: Lancet
  doi: 10.1016/S0140-6736(14)61933-4
– volume: 29
  start-page: 287
  issue: 4
  year: 2010
  ident: 10.1016/j.csbj.2021.04.029_b0380
  article-title: Target profile prediction: cross-activation of peroxisome proliferator-activated receptor (PPAR) and farnesoid X receptor (FXR)
  publication-title: Mol Inform
  doi: 10.1002/minf.200900009
– volume: 3
  start-page: 543
  issue: 5
  year: 1999
  ident: 10.1016/j.csbj.2021.04.029_b0235
  article-title: Endogenous bile acids are ligands for the nuclear receptor FXR/BAR
  publication-title: Mol Cell
  doi: 10.1016/S1097-2765(00)80348-2
– volume: 276
  start-page: 28857
  issue: 31
  year: 2001
  ident: 10.1016/j.csbj.2021.04.029_b0070
  article-title: Human bile salt export pump promoter is transactivated by the farnesoid X receptor/bile acid receptor
  publication-title: J Biol Chem
  doi: 10.1074/jbc.M011610200
– ident: 10.1016/j.csbj.2021.04.029_b0325
  doi: 10.1358/dot.2016.52.12.2571703
– volume: 1844
  start-page: 1684
  issue: 9
  year: 2014
  ident: 10.1016/j.csbj.2021.04.029_b0205
  article-title: Conformational dynamics of human FXR-LBD ligand interactions studied by hydrogen/deuterium exchange mass spectrometry: insights into the antagonism of the hypolipidemic agent Z-guggulsterone
  publication-title: Biochim Biophys Acta
  doi: 10.1016/j.bbapap.2014.06.007
– volume: 105
  start-page: 5337
  issue: 14
  year: 2008
  ident: 10.1016/j.csbj.2021.04.029_b0545
  article-title: Identification of a potent synthetic FXR agonist with an unexpected mode of binding and activation
  publication-title: Proc Natl Acad Sci U S A
  doi: 10.1073/pnas.0710981105
– volume: 176
  start-page: 1098
  issue: 5
  year: 2019
  ident: 10.1016/j.csbj.2021.04.029_b0030
  article-title: FXR regulates intestinal cancer stem cell proliferation
  publication-title: Cell
  doi: 10.1016/j.cell.2019.01.036
– volume: 76
  start-page: 1221
  issue: 12
  year: 2016
  ident: 10.1016/j.csbj.2021.04.029_b0120
  article-title: Obeticholic acid: first global approval
  publication-title: Drugs
  doi: 10.1007/s40265-016-0616-x
– volume: 275
  start-page: 27
  issue: 1
  year: 2014
  ident: 10.1016/j.csbj.2021.04.029_b0495
  article-title: Muricholic bile acids are potent regulators of bile acid synthesis via a positive feedback mechanism
  publication-title: J Intern Med
  doi: 10.1111/joim.12140
– volume: 293
  start-page: 12535
  issue: 32
  year: 2018
  ident: 10.1016/j.csbj.2021.04.029_b0170
  article-title: Structural insights into the heterodimeric complex of the nuclear receptors FXR and RXR
  publication-title: J Biol Chem
  doi: 10.1074/jbc.RA118.004188
– volume: 148
  start-page: 751
  issue: 4
  year: 2015
  ident: 10.1016/j.csbj.2021.04.029_b0525
  article-title: Efficacy of obeticholic acid in patients with primary biliary cirrhosis and inadequate response to ursodeoxycholic acid
  publication-title: Gastroenterology
  doi: 10.1053/j.gastro.2014.12.005
– ident: 10.1016/j.csbj.2021.04.029_b0335
  doi: 10.1016/j.jhep.2017.01.013
– volume: 25
  start-page: 75
  issue: 1
  year: 2018
  ident: 10.1016/j.csbj.2021.04.029_b0095
  article-title: Jaundice revisited: recent advances in the diagnosis and treatment of inherited cholestatic liver diseases
  publication-title: J Biomed Sci
  doi: 10.1186/s12929-018-0475-8
– volume: 70
  start-page: 276
  issue: 1
  year: 2019
  ident: 10.1016/j.csbj.2021.04.029_b0080
  article-title: Enhanced microbial bile acid deconjugation and impaired ileal uptake in pregnancy repress intestinal regulation of bile acid synthesis
  publication-title: Hepatology
  doi: 10.1002/hep.30661
– volume: 18
  start-page: 4339
  issue: 15
  year: 2008
  ident: 10.1016/j.csbj.2021.04.029_b0270
  article-title: Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064
  publication-title: Bioorg Med Chem Lett
  doi: 10.1016/j.bmcl.2008.06.073
– volume: 10
  start-page: 2915
  issue: 1
  year: 2019
  ident: 10.1016/j.csbj.2021.04.029_b0190
  article-title: Molecular tuning of farnesoid X receptor partial agonism
  publication-title: Nat Commun
  doi: 10.1038/s41467-019-10853-2
– volume: 11
  start-page: 1093
  issue: 4
  year: 2003
  ident: 10.1016/j.csbj.2021.04.029_b0175
  article-title: Structural basis for bile acid binding and activation of the nuclear receptor FXR
  publication-title: Mol Cell
  doi: 10.1016/S1097-2765(03)00112-6
– volume: 8
  start-page: 842
  year: 2011
  ident: 10.1016/j.csbj.2021.04.029_b0025
  article-title: Regulation of FXR transcriptional activity in health and disease: Emerging roles of FXR cofactors and post-translational modifications
  publication-title: Biochim Biophys Acta
  doi: 10.1016/j.bbadis.2010.11.011
– volume: 378
  start-page: 681
  issue: 6558
  year: 1995
  ident: 10.1016/j.csbj.2021.04.029_b0195
  article-title: Crystal structure of the RAR-gamma ligand-binding domain bound to all-trans retinoic acid
  publication-title: Nature
  doi: 10.1038/378681a0
– volume: 95
  year: 2020
  ident: 10.1016/j.csbj.2021.04.029_b0515
  article-title: Andrographolide: chemical modification and its effect on biological activities
  publication-title: Bioorg Chem
  doi: 10.1016/j.bioorg.2019.103511
– volume: 29
  start-page: 118
  issue: 1
  year: 2018
  ident: 10.1016/j.csbj.2021.04.029_b0395
  article-title: FXR/TGR5 dual agonist prevents progression of nephropathy in diabetes and obesity
  publication-title: J Am Soc Nephrol
  doi: 10.1681/ASN.2017020222
– volume: 37
  start-page: 1628
  issue: 6
  year: 2019
  ident: 10.1016/j.csbj.2021.04.029_b0425
  article-title: Computational study of the binding mechanism between farnesoid X receptor α and antagonist N-benzyl-N-(3-(tertbutyl)-4-hydroxyphenyl)-2,6-dichloro-4-(dimethylamino) benzamide
  publication-title: J Biomol Struct Dyn
  doi: 10.1080/07391102.2018.1462735
– volume: 278
  start-page: 104
  issue: 1
  year: 2003
  ident: 10.1016/j.csbj.2021.04.029_b0020
  article-title: Natural structural variants of the nuclear receptor farnesoid X receptor affect transcriptional activation
  publication-title: J Biol Chem
  doi: 10.1074/jbc.M209505200
– volume: 256
  start-page: 207
  year: 2019
  ident: 10.1016/j.csbj.2021.04.029_b0240
  article-title: Potential of intestine-selective FXR modulation for treatment of metabolic disease
  publication-title: Handb Exp Pharmacol
  doi: 10.1007/164_2019_233
– volume: 7
  start-page: 12502
  issue: 1
  year: 2017
  ident: 10.1016/j.csbj.2021.04.029_b0110
  article-title: The FXR agonist, obeticholic acid, suppresses HCC proliferation & metastasis: role of IL-6/STAT3 signalling pathway
  publication-title: Sci Rep
  doi: 10.1038/s41598-017-12629-4
– volume: 51
  start-page: 1831
  issue: 6
  year: 2008
  ident: 10.1016/j.csbj.2021.04.029_b0540
  article-title: Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies
  publication-title: J Med Chem
  doi: 10.1021/jm7015864
– volume: 67
  start-page: 1890
  issue: 5
  year: 2018
  ident: 10.1016/j.csbj.2021.04.029_b0530
  article-title: A randomized trial of obeticholic acid monotherapy in patients with primary biliary cholangitis
  publication-title: Hepatology
  doi: 10.1002/hep.29569
– volume: 17
  start-page: 225
  issue: 2
  year: 2013
  ident: 10.1016/j.csbj.2021.04.029_b0310
  article-title: Gut microbiota regulates bile acid metabolism by reducing the levels of tauro-beta-muricholic acid, a naturally occurring FXR antagonist
  publication-title: Cell Metab
  doi: 10.1016/j.cmet.2013.01.003
– volume: 40
  start-page: 16
  issue: 1
  year: 2015
  ident: 10.1016/j.csbj.2021.04.029_b0200
  article-title: Nuclear receptor full-length architectures: confronting myth and illusion with high resolution
  publication-title: Trends Biochem Sci
  doi: 10.1016/j.tibs.2014.10.011
– volume: 9
  start-page: 395
  issue: 3
  year: 2020
  ident: 10.1016/j.csbj.2021.04.029_b0370
  article-title: Safety, tolerability, pharmacokinetics, and pharmacodynamics of the novel non-bile acid FXR agonist tropifexor (LJN452) in healthy volunteers
  publication-title: Clin Pharmacol Drug Dev
  doi: 10.1002/cpdd.762
– volume: 38
  start-page: 356
  issue: 3
  year: 2019
  ident: 10.1016/j.csbj.2021.04.029_b0440
  article-title: Guggulsterone, a farnesoid X receptor antagonist lowers plasma trimethylamine-N-oxide levels: an evidence from in vitro and in vivo studies
  publication-title: Hum Exp Toxicol
  doi: 10.1177/0960327118817862
– volume: 3
  start-page: 1191
  issue: 3
  year: 2013
  ident: 10.1016/j.csbj.2021.04.029_b0245
  article-title: Bile acid metabolism and signaling
  publication-title: Compr Physiol
  doi: 10.1002/cphy.c120023
– volume: 7
  issue: 1
  year: 2012
  ident: 10.1016/j.csbj.2021.04.029_b0445
  article-title: Discovery that theonellasterol a marine sponge sterol is a highly selective FXR antagonist that protects against liver injury in cholestasis
  publication-title: PLoS One
  doi: 10.1371/journal.pone.0030443
– volume: 63
  start-page: 25
  issue: 23
  year: 2019
  ident: 10.1016/j.csbj.2021.04.029_b0455
  article-title: Capsaicin improves glucose tolerance and insulin sensitivity through modulation of the gut microbiota-bile acid-FXR axis in type 2 diabetic db/db Mice
  publication-title: Mol Nutr Food Res
  doi: 10.1002/mnfr.201900608
– volume: 10
  issue: 7
  year: 2015
  ident: 10.1016/j.csbj.2021.04.029_b0415
  article-title: Impaired itching perception in murine models of cholestasis is supported by dysregulation of GPBAR1 signaling
  publication-title: PLoS One
  doi: 10.1371/journal.pone.0129866
– volume: 57
  start-page: 8477
  issue: 20
  year: 2014
  ident: 10.1016/j.csbj.2021.04.029_b0420
  article-title: Exploitation of cholane scaffold for the discovery of potent and selective farnesoid X receptor (FXR) and G-protein coupled bile acid receptor 1 (GP-BAR1) ligands
  publication-title: J Med Chem
  doi: 10.1021/jm501273r
– reference: 35317235 - Comput Struct Biotechnol J. 2022 Mar 01;20:1227-1228. doi: 10.1016/j.csbj.2022.02.029
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Snippet [Display omitted] Farnesoid X receptor (FXR) is a bile acid activated nuclear receptor (BAR) and is mainly expressed in the liver and intestine. Upon ligand...
Farnesoid X receptor (FXR) is a bile acid activated nuclear receptor (BAR) and is mainly expressed in the liver and intestine. Upon ligand binding, FXR...
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SubjectTerms Agonists
Antagonists
bile
bile acids
biotechnology
domain
drugs
Farnesoid X receptor
intestines
Ligand binding domain
ligands
liver
metabolism
resorption
Review
Structure
therapeutics
Title Farnesoid X receptor (FXR): Structures and ligands
URI https://dx.doi.org/10.1016/j.csbj.2021.04.029
https://www.ncbi.nlm.nih.gov/pubmed/33995909
https://www.proquest.com/docview/2528432525
https://www.proquest.com/docview/2574369312
https://pubmed.ncbi.nlm.nih.gov/PMC8091178
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