Výsledky vyhľadávania - "Durant, Stephen T."

The Identification of Potent, Selective, and Orally Available Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase: The Discovery of AZD0156 (8-{6-[3-(Dimethylamino)propoxy]pyridin-3-yl}-3-methyl-1-(tetrahydro-2H-pyran-4-yl)-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one) Autor Pike, Kurt G., Barlaam, Bernard, Cadogan, Elaine, Campbell, Andrew, Chen, Yingxue, Colclough, Nicola, Davies, Nichola L., de-Almeida, Camila, Degorce, Sebastien L., Didelot, Myriam, Dishington, Allan, Ducray, Richard, Durant, Stephen T., Hassall, Lorraine A., Holmes, Jane, Hughes, Gareth D., MacFaul, Philip A., Mulholland, Keith R., McGuire, Thomas M., Ouvry, Gilles, Pass, Martin, Robb, Graeme, Stratton, Natalie, Wang, Zhenhua, Wilson, Joanne, Zhai, Baochang, Zhao, Kang, Al-Huniti, Nidal

“…ATM inhibitors, such as 7, have demonstrated the antitumor potential of ATM inhibition when combined with DNA double-strand break-inducing agents in mouse…”
Zistit podrobnosti o prístupe

Complete loss of ATM function augments replication catastrophe induced by ATR inhibition and gemcitabine in pancreatic cancer models Autor Dunlop, Charles R., Wallez, Yann, Johnson, Timothy Isaac, Bernaldo de Quirós Fernández, Sandra, Durant, Stephen T., Cadogan, Elaine B., Lau, Alan, Richards, Frances M., Jodrell, Duncan I.

“…Background Personalised medicine strategies may improve outcomes in pancreatic ductal adenocarcinoma (PDAC), but validation of predictive biomarkers is…”
Získať plný text

Arginine methylation regulates the p53 response Autor Jansson, Martin, Durant, Stephen T., Cho, Er-Chieh, Sheahan, Sharon, Edelmann, Mariola, Kessler, Benedikt, La Thangue, Nicholas B.

“…The tumour suppressor p53 is subject to complex regulation and arginine methylation is now shown to provide an additional level of control. The protein…”
Získať plný text

H2AX promotes replication fork degradation and chemosensitivity in BRCA-deficient tumours Autor Dibitetto, Diego, Liptay, Martin, Vivalda, Francesca, Dogan, Hülya, Gogola, Ewa, González Fernández, Martín, Duarte, Alexandra, Schmid, Jonas A., Decollogny, Morgane, Francica, Paola, Przetocka, Sara, Durant, Stephen T., Forment, Josep V., Klebic, Ismar, Siffert, Myriam, de Bruijn, Roebi, Kousholt, Arne N., Marti, Nicole A., Dettwiler, Martina, Sørensen, Claus S., Tille, Jean-Christophe, Undurraga, Manuela, Labidi-Galy, Intidhar, Lopes, Massimo, Sartori, Alessandro A., Jonkers, Jos, Rottenberg, Sven

“…Histone H2AX plays a key role in DNA damage signalling in the surrounding regions of DNA double-strand breaks (DSBs). In response to DNA damage, H2AX becomes…”
Získať plný text

Small molecule inhibitors uncover synthetic genetic interactions of human flap endonuclease 1 (FEN1) with DNA damage response genes Autor Ward, Thomas A., McHugh, Peter J., Durant, Stephen T.

“…Flap endonuclease 1 (FEN1) is a structure selective endonuclease required for proficient DNA replication and the repair of DNA damage. Cellularly active…”
Získať plný text

ATM kinase inhibitor AZD0156 in combination with irinotecan and 5-fluorouracil in preclinical models of colorectal cancer Autor Davis, S. Lindsey, Hartman, Sarah J., Bagby, Stacey M., Schlaepfer, Marina, Yacob, Betelehem W., Tse, Tonia, Simmons, Dennis M., Diamond, Jennifer R., Lieu, Christopher H., Leal, Alexis D., Cadogan, Elaine B., Hughes, Gareth D., Durant, Stephen T., Messersmith, Wells A., Pitts, Todd M.

“…Background AZD0156 is an oral inhibitor of ATM, a serine threonine kinase that plays a key role in DNA damage response (DDR) associated with double-strand…”
Získať plný text

Cellularly active N-hydroxyurea FEN1 inhibitors block substrate entry to the active site Autor Exell, Jack C, Thompson, Mark J, Finger, L David, Shaw, Steven J, Debreczeni, Judit, Ward, Thomas A, McWhirter, Claire, Siöberg, Catrine L B, Molina, Daniel Martinez, Abbott, W Mark, Jones, Clifford D, Nissink, J Willem M, Durant, Stephen T, Grasby, Jane A

“…Structural, enzymatic and cellular target engagement studies reveal the mechanism of action by N -hydroxyurea small molecule inhibitors of the DNA repair…”
Získať plný text

Structures of the Human Poly (ADP-Ribose) Glycohydrolase Catalytic Domain Confirm Catalytic Mechanism and Explain Inhibition by ADP-HPD Derivatives Autor Tucker, Julie A., Bennett, Neil, Brassington, Claire, Durant, Stephen T., Hassall, Giles, Holdgate, Geoff, McAlister, Mark, Nissink, J. Willem M., Truman, Caroline, Watson, Martin

“…Poly(ADP-ribose) glycohydrolase (PARG) is the only enzyme known to catalyse hydrolysis of the O-glycosidic linkages of ADP-ribose polymers, thereby reversing…”
Získať plný text

Telomerase-Independent Paths to Immortality in Predictable Cancer Subtypes Autor Durant, Stephen T

“…The vast majority of cancers commandeer the activity of telomerase - the remarkable enzyme responsible for prolonging cellular lifespan by maintaining the…”
Získať plný text

Mechanisms of activation of the transcription factor Nrf2 by redox stressors, nutrient cues, and energy status and the pathways through which it attenuates degenerative disease Autor Tebay, Lauren E., Robertson, Holly, Durant, Stephen T., Vitale, Steven R., Penning, Trevor M., Dinkova-Kostova, Albena T., Hayes, John D.

“…Nuclear factor-erythroid 2 p45-related factor 2 (Nrf2) regulates the basal and stress-inducible expression of a battery of genes encoding key components of the…”
Získať plný text

The SET domain protein Metnase mediates foreign DNA integration and links integration to nonhomologous end-joining repair Autor Lee, Suk-Hee, Oshige, Masahiko, Durant, Stephen T, Rasila, Kanwaldeep Kaur, Williamson, Elizabeth A, Ramsey, Heather, Kwan, Lori, Nickoloff, Jac A, Hromas, Robert

“…The molecular mechanism by which foreign DNA integrates into the human genome is poorly understood yet critical to many disease processes, including retroviral…”
Zistit podrobnosti o prístupe

Good Timing in the Cell Cycle for Precise DNA Repair by BRCA1 Autor Durant, Stephen T., Nickoloff, Jac A

“…It is now clear that large DNA-binding proteins have evolved in mammals to orchestrate the relatively ancient processes of DNA recombinational repair. These…”
Získať plný text

p53 methylation-the Arg-ument is clear Autor Durant, Stephen T., Cho, Er Chieh, La Thangue, Nicholas B.

“…p53 activity is of critical importance in suppressing human cancer formation, highlighted by the fact that the majority of human tumours have defective or…”
Získať plný text

ATM-Inhibitor AZD1390 Is a Radiosensitizer for Breast Cancer CNS Metastasis Autor Tew, Ben Yi, Kalfa, Alex J, Yang, Zeyi, Hurth, Kyle M, Simon, Thomas, Abnoosian, Eric, Durant, Stephen T, Hamerlik, Petra, Salhia, Bodour

“…Limited effective treatments are currently available for central nervous system (CNS) metastasis (CM). This is largely driven by the inability of current…”
Zistit podrobnosti o prístupe

ATM orchestrates the DNA-damage response to counter toxic non-homologous end-joining at broken replication forks Autor Balmus, Gabriel, Pilger, Domenic, Coates, Julia, Demir, Mukerrem, Sczaniecka-Clift, Matylda, Barros, Ana C., Woods, Michael, Fu, Beiyuan, Yang, Fengtang, Chen, Elisabeth, Ostermaier, Matthias, Stankovic, Tatjana, Ponstingl, Hannes, Herzog, Mareike, Yusa, Kosuke, Martinez, Francisco Munoz, Durant, Stephen T., Galanty, Yaron, Beli, Petra, Adams, David J., Bradley, Allan, Metzakopian, Emmanouil, Forment, Josep V., Jackson, Stephen P.

“…Mutations in the ATM tumor suppressor gene confer hypersensitivity to DNA-damaging chemotherapeutic agents. To explore genetic resistance mechanisms, we…”
Získať plný text

CRISPR metabolic screen identifies ATM and KEAP1 as targetable genetic vulnerabilities in solid tumors Autor Li, Haojian, Liu, Yue, Xiao, Yunjie, Wilson, Crystal N, Bai, Hui Jen, Jones, Maxwell D, Wang, Shihchun, DeVore, Jennie E, Maier, Esther Y, Durant, Stephen T, Boufraqech, Myriem, Weyemi, Urbain

“…Cancer treatments targeting DNA repair deficiencies often encounter drug resistance, possibly due to alternative metabolic pathways that counteract the most…”
Zistit podrobnosti o prístupe

ALT neuroblastoma chemoresistance due to telomere dysfunction-induced ATM activation is reversible with ATM inhibitor AZD0156 Autor Koneru, Balakrishna, Farooqi, Ahsan, Nguyen, Thinh H, Chen, Wan Hsi, Hindle, Ashly, Eslinger, Cody, Makena, Monish Ram, Burrow, Trevor A, Wilson, Joanne, Smith, Aaron, Pilla Reddy, Venkatesh, Cadogan, Elaine, Durant, Stephen T, Reynolds, C Patrick

“…Cancers overcome replicative immortality by activating either telomerase or an alternative lengthening of telomeres (ALT) mechanism. ALT occurs in ~25% of…”
Zistit podrobnosti o prístupe

Identification of Novel, Selective Ataxia-Telangiectasia Mutated Kinase Inhibitors with the Ability to Penetrate the Blood-Brain Barrier: The Discovery of AZD1390 Autor Pike, Kurt G., Hunt, Thomas A., Barlaam, Bernard, Benstead, David, Cadogan, Elaine, Chen, Kan, Cook, Calum R., Colclough, Nicola, Deng, Chao, Durant, Stephen T., Eatherton, Andrew, Goldberg, Kristin, Johnstro''m, Peter, Liu, Libin, Liu, Zhaoqun, Nissink, J. Willem M., Pang, Chengling, Pass, Martin, Robb, Graeme R., Roberts, Caroline, Schou, Magnus, Steward, Oliver, Sykes, Andy, Yan, Yumei, Zhai, Baochang, Zheng, Li

“…The inhibition of ataxia-telangiectasia mutated (ATM) has been shown to chemo- and radio-sensitize human glioma cells in vitro and therefore might provide an…”
Zistit podrobnosti o prístupe

The brain-penetrant clinical ATM inhibitor AZD1390 radiosensitizes and improves survival of preclinical brain tumor models Autor Durant, Stephen T., Zheng, Li, Wang, Yingchun, Chen, Kan, Zhang, Lingli, Zhang, Tianwei, Yang, Zhenfan, Riches, Lucy, Trinidad, Antonio G., Fok, Jacqueline H. L., Hunt, Tom, Pike, Kurt G., Wilson, Joanne, Smith, Aaron, Colclough, Nicola, Reddy, Venkatesh Pilla, Sykes, Andrew, Janefeldt, Annika, Johnström, Peter, Varnäs, Katarina, Takano, Akihiro, Ling, Stephanie, Orme, Jonathan, Stott, Jonathan, Roberts, Caroline, Barrett, Ian, Jones, Gemma, Roudier, Martine, Pierce, Andrew, Allen, Jasmine, Kahn, Jenna, Sule, Amrita, Karlin, Jeremy, Cronin, Anna, Chapman, Melissa, Valerie, Kristoffer, Illingworth, Ruth, Pass, Martin

“…Preclinical data highlight AZD1390 as a potentially powerful new therapy to enhance brain tumor patient responses to radiotherapy. Poor survival rates of…”
Získať plný text

Orally Bioavailable and Blood-Brain Barrier-Penetrating ATM Inhibitor (AZ32) Radiosensitizes Intracranial Gliomas in Mice Autor Karlin, Jeremy, Allen, Jasmine, Ahmad, Syed F, Hughes, Gareth, Sheridan, Victoria, Odedra, Rajesh, Farrington, Paul, Cadogan, Elaine B, Riches, Lucy C, Garcia-Trinidad, Antonio, Thomason, Andrew G, Patel, Bhavika, Vincent, Jennifer, Lau, Alan, Pike, Kurt G, Hunt, Thomas A, Sule, Amrita, Valerie, Nicholas C K, Biddlestone-Thorpe, Laura, Kahn, Jenna, Beckta, Jason M, Mukhopadhyay, Nitai, Barlaam, Bernard, Degorce, Sebastien L, Kettle, Jason, Colclough, Nicola, Wilson, Joanne, Smith, Aaron, Barrett, Ian P, Zheng, Li, Zhang, Tianwei, Wang, Yingchun, Chen, Kan, Pass, Martin, Durant, Stephen T, Valerie, Kristoffer

“…Inhibition of ataxia-telangiectasia mutated (ATM) during radiotherapy of glioblastoma multiforme (GBM) may improve tumor control by short-circuiting the…”
Zistit podrobnosti o prístupe