The tyrosine phosphatase CD148 is an essential positive regulator of platelet activation and thrombosis [PDF]
, 2009 Platelets play a fundamental role in hemostasis and thrombosis. They are also involved in pathologic conditions resulting from blocked blood vessels, including myocardial infarction and ischemic stroke.
Abtahian +79 more
core +2 more sources
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 +13 more
core +2 more sources
Thrombin Protease-activated Receptor-1 Signals through Gq- and G13-initiated MAPK Cascades Regulating c-Jun Expression to Induce Cell Transformation [PDF]
, 2003 Although the ability of G protein-coupled receptors to stimulate normal and aberrant cell growth has been intensely investigated, the precise nature of the molecular mechanisms underlying their transforming potential are still not fully understood.
Gutkind, J. Silvio +4 more
core +1 more source
Diabetes, 2012 Interest in how the gut microbiome can influence the metabolic state of the host has recently heightened. One postulated link is bacterial fermentation of “indigestible” prebiotics to short-chain fatty acids (SCFAs), which in turn modulate the release of
G. Tolhurst +9 more
semanticscholar +1 more source
G Protein–Coupled Receptor Rhodopsin [PDF]
Annual Review of Biochemistry, 2006 The rhodopsin crystal structure provides a structural basis for understanding the function of this and other G protein–coupled receptors (GPCRs). The major structural motifs observed for rhodopsin are expected to carry over to other GPCRs, and the mechanism of transformation of the receptor from inactive to active forms is thus likely conserved ...
openaire +2 more sources
Ligand-guided homology modeling drives identification of novel histamine H3 receptor ligands [PDF]
, 2019 In this study, we report a ligand-guided homology modeling approach allowing the analysis of relevant binding site residue conformations and the identification of two novel histamine H3 receptor ligands with binding affinity in the nanomolar range.
Hagenow, Stefanie +3 more
core +2 more sources
Molecular mechanism of biased signaling in a prototypical G protein–coupled receptor
Science, 2020 Choosing the drug to fit the protein Many approved drugs bind to G protein–coupled receptors (GPCRs). A challenge in targeting GPCRs is that different ligands preferentially activate different signaling pathways.
Carl-Mikael Suomivuori +10 more
semanticscholar +1 more source
Targeting G protein-coupled receptor for pain management
Brain Circulation, 2017 Pain is an unpleasant sensory and emotional experience associated with actual or potential tissue damage or described in terms of such damage. Great progress has been made in understanding the important roles of various G protein-coupled receptors in the
Hongyan Li +4 more
doaj +1 more source
The Molecular Basis of G Protein-Coupled Receptor Activation.
Annual Review of Biochemistry, 2018 G protein-coupled receptors (GPCRs) mediate the majority of cellular responses to external stimuli. Upon activation by a ligand, the receptor binds to a partner heterotrimeric G protein and promotes exchange of GTP for GDP, leading to dissociation of the
W. Weis, B. Kobilka
semanticscholar +1 more source
Probing the role of the cation–π interaction in the binding sites of GPCRs using unnatural amino acids [PDF]
, 2009 We describe a general application of the nonsense suppression methodology for unnatural amino acid incorporation to probe drug–receptor interactions in functional G protein-coupled receptors (GPCRs), evaluating the binding sites of both the M2 muscarinic
Ballesteros +31 more
core +3 more sources