Výsledky vyhľadávania - "Hurst, Dow"

Molecular Targets of the Phytocannabinoids: A Complex Picture Autor Morales, Paula, Hurst, Dow P, Reggio, Patricia H

“…For centuries, hashish and marihuana, both derived from the Indian hemp Cannabis sativa L., have been used for their medicinal, as well as, their psychotropic…”
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Therapeutic Exploitation of GPR18: Beyond the Cannabinoids? Autor Morales, Paula, Lago-Fernandez, Ana, Hurst, Dow P, Sotudeh, Noori, Brailoiu, Eugen, Reggio, Patricia H, Abood, Mary E, Jagerovic, Nadine

“…GPR18 is a G-protein-coupled receptor that belongs to the orphan class A family. Even though it shares low sequence homology with the cannabinoid receptors CB…”
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The Nucleotide-Free State of the Cannabinoid CB2/Gi Complex Autor Lynch, Diane L, Hurst, Dow P, Reggio, Patricia H

“…In this issue of Cell, two papers report agonist-bound cryo-EM structures of the cannabinoid receptor, CB2, in complex with Gi. Importantly, beyond providing…”
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A lipid pathway for ligand binding is necessary for a cannabinoid G protein-coupled receptor Autor Hurst, Dow P, Grossfield, Alan, Lynch, Diane L, Feller, Scott, Romo, Tod D, Gawrisch, Klaus, Pitman, Michael C, Reggio, Patricia H

“…Recent isothiocyanate covalent labeling studies have suggested that a classical cannabinoid,…”
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TRPV1 Activation by Anandamide via a Unique Lipid Pathway Autor Muller, Chanté, Lynch, Diane L, Hurst, Dow P, Reggio, Patricia H

“…The capsaicin receptor, transient receptor potential vanilloid type 1 (TRPV1), is a polymodal channel that has been implicated in the perception of pain and…”
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Application of Fluorine- and Nitrogen-Walk Approaches: Defining the Structural and Functional Diversity of 2-Phenylindole Class of Cannabinoid 1 Receptor Positive Allosteric Modulators Autor Garai, Sumanta, Kulkarni, Pushkar M., Schaffer, Peter C., Leo, Luciana M., Brandt, Asher L., Zagzoog, Ayat, Black, Tallan, Lin, Xiaoyan, Hurst, Dow P., Janero, David R., Abood, Mary E., Zimmowitch, Anaelle, Straiker, Alex, Pertwee, Roger G., Kelly, Melanie, Szczesniak, Anna-Maria, Denovan-Wright, Eileen M., Mackie, Ken, Hohmann, Andrea G., Reggio, Patricia H., Laprairie, Robert B., Thakur, Ganesh A.

“…Cannabinoid 1 receptor (CB1R) allosteric ligands hold a far-reaching therapeutic promise. We report the application of fluoro- and nitrogen-walk approaches to…”
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A Closer Look at Anandamide Interaction With TRPV1 Autor Muller, Chante, Lynch, Diane L., Hurst, Dow P., Reggio, Patricia H.

“…The transient receptor potential subfamily vanilloid type 1 ion channel (TRPV1), located in the peripheral nervous system has been implicated in the perception…”
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Discovery of a Biased Allosteric Modulator for Cannabinoid 1 Receptor: Preclinical Anti-Glaucoma Efficacy Autor Garai, Sumanta, Leo, Luciana M., Szczesniak, Anna-Maria, Hurst, Dow P., Schaffer, Peter C., Zagzoog, Ayat, Black, Tallan, Deschamps, Jeffrey R., Miess, Elke, Schulz, Stefan, Janero, David R., Straiker, Alex, Pertwee, Roger G., Abood, Mary E., Kelly, Melanie E. M., Reggio, Patricia H., Laprairie, Robert B., Thakur, Ganesh A.

“…We apply the magic methyl effect to improve the potency/efficacy of GAT211, the prototypic 2-phenylindole-based cannabinoid type-1 receptor (CB1R)…”
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Identification of Crucial Amino Acid Residues Involved in Agonist Signaling at the GPR55 Receptor Autor Lingerfelt, Mary A, Zhao, Pingwei, Sharir, Haleli P, Hurst, Dow P, Reggio, Patricia H, Abood, Mary E

“…GPR55 is a newly deorphanized class A G-protein-coupled receptor that has been implicated in inflammatory pain, neuropathic pain, metabolic disorder, bone…”
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GPR6 Structural Insights: Homology Model Construction and Docking Studies Autor Isawi, Israa H., Morales, Paula, Sotudeh, Noori, Hurst, Dow P., Lynch, Diane L., Reggio, Patricia H.

“…GPR6 is an orphan G protein-coupled receptor that has been associated with the cannabinoid family because of its recognition of a sub-set of cannabinoid…”
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Design, synthesis, and evaluation of substituted alkylindoles that activate G protein-coupled receptors distinct from the cannabinoid CB1 and CB2 receptors Autor Kline, Toni, Xu, Cong, Kreitzer, Faith R., Hurst, Dow P., Eldeeb, Khalil M., Wager-Miller, Jim, Olivas, Kathleen, Hepburn, Seon A., Huffman, John W., Mackie, Ken, Howlett, Allyn C., Reggio, Patricia, Stella, Nephi

“…The alkylindole (AI), WIN55212-2, modulates the activity of several proteins, including cannabinoid receptors 1 and 2 (CB1R, CB2R), and at least additional G…”
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Towards A Molecular Understanding of The Cannabinoid Related Orphan Receptor GPR18: A Focus on Its Constitutive Activity Autor Sotudeh, Noori, Morales, Paula, Hurst, Dow P., Lynch, Diane L., Reggio, Patricia H.

“…The orphan G-protein coupled receptor (GPCR), GPR18, has been recently proposed as a potential member of the cannabinoid family as it recognizes several…”
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Pharmacological evaluation of enantiomerically separated positive allosteric modulators of cannabinoid 1 receptor, GAT591 and GAT593 Autor Brandt, Asher L., Garai, Sumanta, Zagzoog, Ayat, Hurst, Dow P., Stevenson, Lesley A., Pertwee, Roger G., Imler, Gregory H., Reggio, Patricia H., Thakur, Ganesh A., Laprairie, Robert B.

“…Positive allosteric modulation of the type 1 cannabinoid receptor (CB1R) has substantial potential to treat both neurological and immune disorders. To date, a…”
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Identification of CB1 Receptor Allosteric Sites Using Force-Biased MMC Simulated Annealing and Validation by Structure-Activity Relationship Studies Autor Hurst, Dow P, Garai, Sumanta, Kulkarni, Pushkar M, Schaffer, Peter C, Reggio, Patricia H, Thakur, Ganesh A

“…Positive allosteric modulation of the cannabinoid 1 receptor (CB1R) has demonstrated distinct therapeutic advantages that address several limitations…”
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Allosteric modulation of a cannabinoid G protein-coupled receptor: binding site elucidation and relationship to G protein signaling Autor Shore, Derek M, Baillie, Gemma L, Hurst, Dow H, Navas, 3rd, Frank, Seltzman, Herbert H, Marcu, Jahan P, Abood, Mary E, Ross, Ruth A, Reggio, Patricia H

“…The cannabinoid 1 (CB1) allosteric modulator, 5-chloro-3-ethyl-1H-indole-2-carboxylic acid [2-(4-piperidin-1-yl-phenyl)-ethyl]-amide) (ORG27569), has the…”
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Enhanced Functional Activity of the Cannabinoid Type-1 Receptor Mediates Adolescent Behavior Autor Schneider, Miriam, Kasanetz, Fernando, Lynch, Diane L, Friemel, Chris M, Lassalle, Olivier, Hurst, Dow P, Steindel, Frauke, Monory, Krisztina, Schäfer, Carola, Miederer, Isabelle, Leweke, F Markus, Schreckenberger, Mathias, Lutz, Beat, Reggio, Patricia H, Manzoni, Olivier J, Spanagel, Rainer

“…Adolescence is characterized by drastic behavioral adaptations and comprises a particularly vulnerable period for the emergence of various psychiatric…”
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Chromenopyrazole, a Versatile Cannabinoid Scaffold with in Vivo Activity in a Model of Multiple Sclerosis Autor Morales, Paula, Gomez-Canas, Maria, Navarro, Gemma, Hurst, Dow P., Carrillo-Salinas, Francisco J., Lagartera, Laura, Pazos, Ruth, Goya, Pilar, Reggio, Patricia H., Guaza, Carmen, Franco, Rafael, Fernandez-Ruiz, Javier, Jagerovic, Nadine

“…A combination of molecular modeling and structure activity relationship studies has been used to fine-tune CB2 selectivity in the chromenopyrazole ring, a…”
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CB2-Selective Cannabinoid Receptor Ligands: Synthesis, Pharmacological Evaluation, and Molecular Modeling Investigation of 1,8-Naphthyridin-2(1H)‑one-3-carboxamides Autor Lucchesi, Valentina, Hurst, Dow P, Shore, Derek M, Bertini, Simone, Ehrmann, Brandie M, Allarà, Marco, Lawrence, Lyle, Ligresti, Alessia, Minutolo, Filippo, Saccomanni, Giuseppe, Sharir, Haleli, Macchia, Marco, Di Marzo, Vincenzo, Abood, Mary E, Reggio, Patricia H, Manera, Clementina

“…We have recently identified 1,8-naphthyridin-2­(1H)-one-3-carboxamide as a new scaffold very suitable for the development of new CB2 receptor potent and…”
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Endogenous lipid activated G protein-coupled receptors: Emerging structural features from crystallography and molecular dynamics simulations Autor Hurst, Dow P., Schmeisser, Marianne, Reggio, Patricia H.

“…► We compare two Class A GPCR structures, the S1-P1R and rhodopsin, both known to bind lipid-derived endogenous ligands. ► We find that EC loop and N-termini…”
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Methods for the Development of In Silico GPCR Models Autor Morales, Paula, Hurst, Dow P, Reggio, Patricia H

“…The Reggio group has constructed computer models of the inactive and G-protein-activated states of the cannabinoid CB1 and CB2 receptors, as well as, several…”
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