Results 31 to 40 of about 47,712 (207)

Molecular Characterisation of Small Molecule Agonists Effect on the Human Glucagon Like Peptide-1 Receptor Internalisation [PDF]

, 2016
The glucagon-like peptide receptor (GLP-1R), which is a G-protein coupled receptor (GPCR), signals through both Gαs and Gαq coupled pathways and ERK phosphorylation to stimulate insulin secretion.
A Bond, A Thompson, A Thompson, A Thompson, A Thompson, AC Hanyaloglu, Aiysha Thompson, B Thorens, BD Green, C Koole, C Montrose-Rafizadeh, C Orskov, CE Groer, CR Underwood, D Wootten, D Wootten, DJ Drucker, FS Willard, FS Willard, GG Holz, JC Davies, JC Davies, Jeffrey W. Stephens, JT Patterson, K Coopman, K Venkateswarlu, K Zahn, KW Sloop, L Ma, LB Knudsen, M Edavalath, ME Doyle, MR Price, N Irwin, N Li, P Vazquez, R Goke, R López de Maturana, Rasheed Ahmad, RL Thomas, RS Kuna, S Takhar, SK Mathi, SN Roed, Stephen C. Bain, T Kim Chung le, TM Bridges, TP Vahl, V Kanamarlapudi, V Serre, Venkateswarlu Kanamarlapudi, WM Nolte, YH Cheong   +52 more
core   +2 more sources

Extracellular loops 2 and 3 of the calcitonin receptor selectively modify agonist binding and efficacy. [PDF]

, 2018
Class B peptide hormone GPCRs are targets for the treatment of major chronic disease. Peptide ligands of these receptors display biased agonism and this may provide future therapeutic advantage.
Andreassen, Arthur Christopoulos, Baldwin, Barwell, Belcheva, Berendsen, Black, Booe, Caroline A. Hick, Christopher A. Reynolds, Christopoulos, Christopoulos, Cosman, Dal Maso, de Graaf, Debbie L. Hay, Dehua Yang, Denise Wootten, Doerr, Dolinsky, Dong, Dong, Emma Dal Maso, Epand, Essmann, Eswar, Feyen, Furness, Gingell, Giuseppe Deganutti, Hamelryck, Harikumar, Harvey, Hay, Hilton, Huang, Humphrey, Johansson, Jorgensen, Koole, Koole, Krautler, Kuestner, Kuwasako, Kuwasako, Langston, Li, Liang, Lomize, Loncharich, Ming-Wei Wang, Minhas, Morfis, Orlowski, Patrick M. Sexton, Poyner, Sebastian G.B. Furness, Sommer, Udawela, Udawela, Vi Pham, Watkins, Weaver, Weston, Weston, Woolley, Woolley, Wootten, Wootten, Yue Zhu, Zhang   +70 more
core   +1 more source

Future Perspectives on GLP-1 Receptor Agonists and GLP-1/glucagon Receptor Co-agonists in the Treatment of NAFLD [PDF]

Frontiers in Endocrinology, 2018
Along the obesity pandemic, the prevalence of non-alcoholic fatty liver disease (NAFLD), often regarded as the hepatic manifestation of the metabolic syndrome, increases worldwide representing now the prevalent liver disease in western countries. No pharmacotherapy is approved for the treatment of NAFLD and, currently, the cornerstone treatment is ...
Marta Seghieri, Marta Seghieri, Alexander S. Christensen, Andreas Andersen, Anna Solini, Filip K. Knop, Filip K. Knop, Filip K. Knop, Tina Vilsbøll, Tina Vilsbøll   +9 more
openaire   +6 more sources

The therapeutic potential of allosteric ligands for free fatty acid sensitive GPCRs [PDF]

, 2013
G protein coupled receptors (GPCRs) are the most historically successful therapeutic targets. Despite this success there are many important aspects of GPCR pharmacology and function that have yet to be exploited to their full therapeutic potential.
Hudson, Brian D., Milligan, Graeme, Ulven, Trond   +2 more
core   +1 more source

Adverse effects of GLP – 1 Receptor Agonists

Journal of Education, Health and Sport
Introduction and purpose Glucagon-like peptide-1 receptor agonists (GLP – 1 RAs) are indicated in type 2 diabetes (T2D) and obesity because of their high efficacy in controlling blood glucose levels and inducing weight loss.
Anna Kasprzak, Monika Kułaga, Monika Grzybek, Diana Mazur-Lesińska, Barbara Szostak, Sylwia Wielgosz-Biała, Krzysztof Tyszkiewicz, Borys Łozowski, Małgorzata Kasprzak, Barbara Wilczyńska   +9 more
doaj   +1 more source

Activation of the GLP-1 receptor by a non-peptidic agonist [PDF]

Nature, 2020
Class B G-protein-coupled receptors are major targets for the treatment of chronic diseases, including diabetes and obesity1. Structures of active receptors reveal peptide agonists engage deep within the receptor core, leading to an outward movement of extracellular loop 3 and the tops of transmembrane helices 6 and 7, an inward movement of ...
Zhao, Peishen, Liang, Yi-Lynn, Belousoff, Matthew J, Deganutti, Giuseppe, Fletcher, Madeleine M, Willard, Francis S, Bell, Michael G, Christe, Michael E, Sloop, Kyle W, Inoue, Asuka, Truong, Tin T, Clydesdale, Lachlan, Furness, Sebastian GB, Christopoulos, Arthur, Wang, Ming-Wei, Miller, Laurence J, Reynolds, Christopher A, Danev, Radostin, Sexton, Patrick M, Wootten, Denise   +19 more
openaire   +4 more sources

Structure and dynamics of semaglutide- and taspoglutide-bound GLP-1R-Gs complexes

Cell Reports, 2021
Summary: The glucagon-like peptide-1 receptor (GLP-1R) regulates insulin secretion, carbohydrate metabolism, and appetite and is an important target for treatment of type 2 diabetes and obesity. Multiple GLP-1R agonists have entered into clinical trials,
Xin Zhang, Matthew J. Belousoff, Yi-Lynn Liang, Radostin Danev, Patrick M. Sexton, Denise Wootten   +5 more
doaj   +1 more source

The role of ECL2 in CGRP receptor activation: a combined modelling and experimental approach [PDF]

, 2013
The calcitonin gene-related peptide (CGRP) receptor is a complex of a calcitonin receptor-like receptor (CLR), which is a family B G-protein-coupled receptor (GPCR) and receptor activity modifying protein 1.
Alex C. Conner, Barwell J, Bruck Taddese, Christopher A. Reynolds, Conner AC, David R. Poyner, Debbie L. Hay, Harriet A. Watkins, James Barwell, Kevin J. Smith, Michael. J. Woolley, Urano D, Watkins HA, Z. Gamze Karakullukcu   +13 more
core   +2 more sources

Pharmacogenetics of type 2 diabetes mellitus, the route toward tailored medicine [PDF]

, 2019
Type 2 diabetes mellitus (T2DM) is a chronic disease that has reached the levels of a global epidemic. In order to achieve optimal glucose control, it is often necessary to rely on combination therapy of multiple drugs or insulin because uncontrolled ...
Andreozzi, F, Mannino, Gc, Sesti, G
core   +1 more source

GLP-1 receptor agonists or DPP-4 inhibitors: How to guide the clinician? [PDF]

, 2013
Pharmacological treatment of type 2 diabetes has been enriched during recent years, with the launch of incretin therapies targeting glucagon-like peptide-1 (GLP-1).
SCHEEN, André
core   +1 more source