Functional selectivity of GPCR-directed drug action through location bias. [PDF]
, 2017 G-protein-coupled receptors (GPCRs) are increasingly recognized to operate from intracellular membranes as well as the plasma membrane. The β 2 -adrenergic GPCR can activate G s -linked cyclic AMP (G s -cAMP) signaling from endosomes.
Conti, Marco +6 more
core +3 more sources
Dynamic regulation of quaternary organization of the M1 muscarinic receptor by subtype-selective antagonist drugs [PDF]
, 2016 Although rhodopsin-like G protein-coupled receptors can exist as both monomers and non-covalently associated dimers/oligomers, the steady-state proportion of each form and whether this is regulated by receptor ligands is unknown.
Godin, Antoine G. +4 more
core +1 more source
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
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 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
G-protein-coupled receptor kinases
Trends in Biochemical Sciences, 1991 Rhodopsin kinase and the beta-adrenergic receptor kinase (beta ARK) catalyse the phosphorylation of the activated forms of the G-protein-coupled receptors, rhodopsin and the beta 2-adrenergic receptor (beta 2AR), respectively. The interaction between receptor and kinase is independent of second messengers and appears to involve a multipoint attachment ...
Palczewskl, Krzvsztof +1 more
openaire +4 more sources
Structural and Functional Analysis of a β2-Adrenergic Receptor Complex with GRK5. [PDF]
, 2017 The phosphorylation of agonist-occupied G-protein-coupled receptors (GPCRs) by GPCR kinases (GRKs) functions to turn off G-protein signaling and turn on arrestin-mediated signaling.
Adams, Christopher M. +12 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
A G protein-gated K channel is activated via beta 2-adrenergic receptors and G beta gamma subunits in Xenopus oocytes [PDF]
, 1995 In many tissues, inwardly rectifying K channels are coupled to seven- helix receptors via the Gi/Go family of heterotrimeric G proteins. This activation proceeds at least partially via G beta gamma subunits.
Dascal, Nathan +4 more
core +2 more sources
G-protein-coupled receptor kinases
Kidney International, 1996 beta-Adrenergic receptors are prototypes of the many G-protein-coupled receptors. Activation and inactivation of these receptors are regulated by multiple mechanisms which can affect either their function or their expression. The most obvious changes of such receptor systems are induced by activation of the receptors themselves by their respective ...
Lohse, Martin J. +3 more
openaire +2 more sources