Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Thomas Coudrat"'
Autor:
Kaleeckal G. Harikumar, Thomas Coudrat, Aditya J. Desai, Maoqing Dong, Daniela G. Dengler, Sebastian G. B. Furness, Arthur Christopoulos, Denise Wootten, Eduard A. Sergienko, Patrick M. Sexton, Laurence J. Miller
Publikováno v:
Frontiers in Endocrinology, Vol 12 (2021)
Drugs useful in prevention/treatment of obesity could improve health. Cholecystokinin (CCK) is a key regulator of appetite, working through the type 1 CCK receptor (CCK1R); however, full agonists have not stimulated more weight loss than dieting. We
Externí odkaz:
https://doaj.org/article/895703c860ab400c964a97eea810e55b
Autor:
Carmen Klein Herenbrink, David A. Sykes, Prashant Donthamsetti, Meritxell Canals, Thomas Coudrat, Jeremy Shonberg, Peter J. Scammells, Ben Capuano, Patrick M. Sexton, Steven J. Charlton, Jonathan A. Javitch, Arthur Christopoulos, J. Robert Lane
Publikováno v:
Nature Communications, Vol 7, Iss 1, Pp 1-14 (2016)
Biased agonists act at a receptor to preferentially induce distinct intracellular signalling responses over others. Here the authors show how kinetics of ligand binding and signaling responses greatly influence observed bias profiles, and hence must
Externí odkaz:
https://doaj.org/article/0783ff6940594b04b8cd38d7c0762fb1
Publikováno v:
PLoS Computational Biology, Vol 13, Iss 11, p e1005819 (2017)
G protein-coupled receptors (GPCRs) play crucial roles in cell physiology and pathophysiology. There is increasing interest in using structural information for virtual screening (VS) of libraries and for structure-based drug design to identify novel
Externí odkaz:
https://doaj.org/article/4e7ed5d171f84e11b0c5527b7366249d
Publikováno v:
PLoS ONE, Vol 12, Iss 4, p e0174719 (2017)
Structure based drug discovery on GPCRs harness atomic detail X-ray binding pockets and large libraries of potential drug lead candidates in virtual screening (VS) to identify novel lead candidates. Relatively small conformational differences between
Externí odkaz:
https://doaj.org/article/368748b6e73040d4ad0de31eafdf4017
Two distinct domains of the glucagon-like peptide-1 receptor control peptide-mediated biased agonism
Autor:
Patrick M. Sexton, Antao Dai, Thomas Coudrat, Arthur Christopoulos, Lachlan Clydesdale, Yi Lynn Liang, Dehua Yang, Peishen Zhao, Denise Wootten, Saifei Lei, Cassandra Koole, Xiaoqing Cai, Yang Feng, Ming-Wei Wang
Publikováno v:
Journal of Biological Chemistry. 293:9370-9387
G protein–coupled receptors (GPCRs) can be differentially activated by ligands to generate multiple and distinct downstream signaling profiles, a phenomenon termed biased agonism. The glucagon-like peptide-1 receptor (GLP-1R) is a class B GPCR and
Autor:
Brian K. Kobilka, Georgios Skiniotis, Maryam Khoshouei, Laurence J. Miller, Jeffrey T. Tarrasch, Patrick M. Sexton, Yan Zhang, Thomas Coudrat, Mazdak Radjainia, George Christopoulos, Wolfgang Baumeister, Radostin Danev, Alisa Glukhova, Sebastian G.B. Furness, Arthur Christopoulos, Yi Lynn Liang, David M. Thal, Denise Wootten
Publikováno v:
Nature
SUMMARY Class B G protein-coupled receptors are major targets for treatment of chronic diseases, including osteoporosis, diabetes and obesity. Here we report the structure of a full-length class B receptor, the calcitonin receptor, in complex with pe
Publikováno v:
PLoS Computational Biology
PLoS Computational Biology, Vol 13, Iss 11, p e1005819 (2017)
PLoS Computational Biology, Vol 13, Iss 11, p e1005819 (2017)
G protein-coupled receptors (GPCRs) play crucial roles in cell physiology and pathophysiology. There is increasing interest in using structural information for virtual screening (VS) of libraries and for structure-based drug design to identify novel
Publikováno v:
PLoS ONE
PLoS ONE, Vol 12, Iss 4, p e0174719 (2017)
PLoS ONE, Vol 12, Iss 4, p e0174719 (2017)
Structure based drug discovery on GPCRs harness atomic detail X-ray binding pockets and large libraries of potential drug lead candidates in virtual screening (VS) to identify novel lead candidates. Relatively small conformational differences between
Autor:
THOMAS COUDRAT
G protein-coupled receptors (GPCRs) are a superfamily of transmembrane proteins that play crucial roles in cell physiology. Being key drug targets in many diseases, drug discovery efforts harness structural information about these receptors to ration
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::4360d6b33d8199bb5b6b80fca865ce57
Autor:
Arthur Christopoulos, J. Robert Lane, Meritxell Canals, Georgina L. Thompson, Patrick M. Sexton, Thomas Coudrat
Publikováno v:
Biochemical pharmacology. 113
Biased agonism describes the ability of distinct G protein-coupled receptor (GPCR) ligands to stabilise distinct receptor conformations leading to the activation of different cell signalling pathways that can deliver different physiologic outcomes. T