Results 31 to 40 of about 1,156,973 (433)

G protein-coupled receptors not currently in the spotlight: free fatty acid receptor 2 and GPR35 [PDF]

, 2017
It is widely appreciated that G protein-coupled receptors have been the most successfully exploited class of targets for the development of small molecule medicines. Despite this, to date, less than 15% of the non-olfactory G protein-coupled receptors in
Milligan, Graeme
core   +1 more source

A G Protein-coupled Receptor Responsive to Bile Acids*

Journal of Biological Chemistry, 2003
So far some nuclear receptors for bile acids have been identified. However, no cell surface receptor for bile acids has yet been reported. We found that a novel G protein-coupled receptor, TGR5, is responsive to bile acids as a cell-surface receptor ...
Y. Kawamata, Ryo Fujii, M. Hosoya, M. Harada, Hiromi Yoshida, M. Miwa, S. Fukusumi, Y. Habata, T. Itoh, Y. Shintani, S. Hinuma, Y. Fujisawa, M. Fujino   +12 more
semanticscholar   +1 more source

Increased accuracy of ligand sensing by receptor diffusion on cell surface [PDF]

Physical Review E 82, 041902 (2010), 2010
The physical limit with which a cell senses external ligand concentration corresponds to the perfect absorber, where all ligand particles are absorbed and overcounting of same ligand particles does not occur. Here we analyze how the lateral diffusion of receptors on the cell membrane affects the accuracy of sensing ligand concentration.
arxiv   +1 more source

An allosteric role for receptor activity-modifying proteins in defining GPCR pharmacology [PDF]

, 2016
G protein-coupled receptors are allosteric proteins that control transmission of external signals to regulate cellular response. Although agonist binding promotes canonical G protein signalling transmitted through conformational changes, G protein ...
A Christopoulos, A Manglik, A Sali, AA Pioszak, AA Pioszak, C Parthier, C Weston, CJ Tsai, CR Underwood, CS Walker, D Wootten, DL Hay, DL Hay, DL Hay, DL Hay, DR Poyner, G Christopoulos, H Li, HN Motlagh, IM Dickerson, J Simms, JJ Gingell, JK Archbold, JM Booe, K Hollenstein, KG Harikumar, LM McLatchie, M Morfis, M Udawela, M Udawela, MC Lagerstrom, N Tilakaratne, O Poirot, PM Lenhart, PM Sexton, R Sounier, RA Laskowski, RJ Bailey, RO Dror, S Runge, SG Rasmussen, T Bouschet, T Haliloglu, T Kenakin, T Qi, TJ Dolinsky, V Pham, W Huang   +47 more
core   +1 more source

Competing G protein‐coupled receptor kinases balance G protein and β‐arrestin signaling

Molecular Systems Biology, 2012
Seven‐transmembrane receptors (7TMRs) are involved in nearly all aspects of chemical communications and represent major drug targets. 7TMRs transmit their signals not only via heterotrimeric G proteins but also through β‐arrestins, whose recruitment to ...
Domitille Heitzler, Guillaume Durand, Nathalie Gallay, Aurélien Rizk, Seungkirl Ahn, Jihee Kim, Jonathan D Violin, Laurence Dupuy, Christophe Gauthier, Vincent Piketty, Pascale Crépieux, Anne Poupon, Frédérique Clément, François Fages, Robert J Lefkowitz, Eric Reiter   +15 more
doaj   +1 more source

Receptor Quaternary Organization Explains G Protein-Coupled Receptor Family Structure

Cell Reports, 2017
The organization of Rhodopsin-family G protein-coupled receptors (GPCRs) at the cell surface is controversial. Support both for and against the existence of dimers has been obtained in studies of mostly individual receptors.
James H. Felce, Sarah L. Latty, Rachel G. Knox, Susan R. Mattick, Yuan Lui, Steven F. Lee, David Klenerman, Simon J. Davis   +7 more
doaj   +1 more source

The Expression Pattern of Adhesion G Protein-Coupled Receptor F5 Is Related to Cell Adhesion and Metastatic Pathways in Colorectal Cancer—Comprehensive Study Based on In Silico Analysis

Cells, 2022
Adhesion G protein-coupled receptor F5 (ADGRF5) is involved inthe neoplastic transformation of some cancer types. However, the significance of ADGRF5 expression signature and the impact of signaling pathways mediated by ADGRF5 during neoplastic ...
Huining Kang, Jakub Fichna, Ksenia Matlawska-Wasowska, Damian Jacenik   +3 more
doaj   +1 more source

G-protein coupled receptor structure

Biochimica et Biophysica Acta (BBA) - Biomembranes, 2007
Because of their central role in regulation of cellular function, structure/function relationships for G-protein coupled receptors (GPCR) are of vital importance, yet only recently have sufficient data been obtained to begin mapping those relationships. GPCRs regulate a wide range of cellular processes, including the senses of taste, smell, and vision,
Philip L. Yeagle, Arlene D. Albert
openaire   +3 more sources

Estrogen-induced activation of Erk-1 and Erk-2 requires the G protein-coupled receptor homolog, GPR30, and occurs via trans-activation of the epidermal growth factor receptor through release of HB-EGF.

Molecular Endocrinology, 2000
Estrogen rapidly activates the mitogen-activated protein kinases, Erk-1 and Erk-2, via an as yet unknown mechanism. Here, evidence is provided that estrogen-induced Erk-1/-2 activation occurs independently of known estrogen receptors, but requires the ...
E. Filardo, Jeffrey A. Quinn, K. Bland, A. Frackelton, Roger Williams   +4 more
semanticscholar   +1 more source

G protein-coupled receptor dimerisation: molecular basis and relevance to function [PDF]

, 2007
The belief that G protein-coupled receptors exist and function as monomeric, non-interacting species has been largely supplanted in recent years by evidence, derived from a range of approaches, that indicate they can form dimers and/or higher-order ...
Milligan, Graeme
core   +1 more source