Results 181 to 190 of about 61,419 (246)

ERNEST COST action overview on the (patho)physiology of GPCRs and orphan GPCRs in the nervous system

open access: yesBritish Journal of Pharmacology, EarlyView.
G protein‐coupled receptors (GPCRs) are a large family of cell surface receptors that play a critical role in nervous system function by transmitting signals between cells and their environment. They are involved in many, if not all, nervous system processes, and their dysfunction has been linked to various neurological disorders representing important
Necla Birgül Iyison   +15 more
wiley   +1 more source

Altered desensitization and internalization patterns of rodent versus human glucose‐dependent insulinotropic polypeptide (GIP) receptors. An important drug discovery challenge

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Background and Purpose The gut hormone glucose‐dependent insulinotropic polypeptide (GIP) signals via the GIP receptor (GIPR), resulting in postprandial potentiation of glucose‐stimulated insulin secretion. The translation of results from rodent studies to human studies has been challenged by the unexpected effects of GIPR‐targeting compounds.
Lærke Smidt Gasbjerg   +18 more
wiley   +1 more source

GPCR Engineering Yields High-Resolution Structural Insights into β 2 -Adrenergic Receptor Function

open access: bronze, 2007
Daniel M. Rosenbaum   +10 more
openalex   +1 more source

Relevance of G protein‐coupled receptor (GPCR) dynamics for receptor activation, signalling bias and allosteric modulation

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract G protein‐coupled receptors (GPCRs) are one of the major drug targets. In recent years, computational drug design for GPCRs has mainly focused on static structures obtained through X‐ray crystallography, cryogenic electron microscopy (cryo‐EM) or in silico modelling as a starting point for virtual screening campaigns. However, GPCRs are highly
Marta Lopez‐Balastegui   +6 more
wiley   +1 more source

Evaluation of Cellular Dielectric Spectroscopy, a Whole-Cell, Label-Free Technology for Drug Discovery on Gi-Coupled GPCRs

open access: hybrid, 2007
Matthew F. Peters   +6 more
openalex   +1 more source

Allosterism in the adenosine A2A and cannabinoid CB2 heteromer

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Allosterism is a regulatory mechanism for GPCRs that can be attained by ligand‐binding or protein–protein interactions with another GPCR. We have studied the influence of the dimer interface on the allosteric properties of the A2A receptor and CB2 receptor heteromer.
Claudia Llinas del Torrent   +7 more
wiley   +1 more source

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