Results 241 to 250 of about 1,102,643 (357)

Arrestin‐centred interactions at the membrane and their conformational determinants

open access: yesBritish Journal of Pharmacology, Volume 182, Issue 14, Page 3135-3150, July 2025.
Abstract More than 30 years after their discovery, arrestins are recognised multiprotein scaffolds that play essential roles in G protein‐coupled receptor (GPCR) regulation and signalling. Originally named for their capacity to hinder GPCR coupling to G proteins and facilitate receptor desensitisation, arrestins have emerged as key hubs for a myriad of
Owen Underwood   +3 more
wiley   +1 more source

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

open access: yesBritish Journal of Pharmacology, Volume 182, Issue 14, Page 3178-3210, July 2025.
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

Allosterism in the adenosine A2A and cannabinoid CB2 heteromer

open access: yesBritish Journal of Pharmacology, Volume 182, Issue 14, Page 3371-3384, July 2025.
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

Progress on the development of Class A GPCR‐biased ligands

open access: yesBritish Journal of Pharmacology, Volume 182, Issue 14, Page 3249-3300, July 2025.
Class A G protein‐coupled receptors (GPCRs) continue to garner interest for their essential roles in cell signalling and their importance as drug targets. Although numerous drugs in the clinic target these receptors, over 60% GPCRs remain unexploited. Moreover, the adverse effects triggered by the available unbiased GPCR modulators, limit their use and
Paula Morales   +20 more
wiley   +1 more source

The path to the G protein‐coupled receptor structural landscape: Major milestones and future directions

open access: yesBritish Journal of Pharmacology, Volume 182, Issue 14, Page 3225-3248, July 2025.
G protein‐coupled receptors (GPCRs) play a crucial role in cell function by transducing signals from the extracellular environment to the inside of the cell. They mediate the effects of various stimuli, including hormones, neurotransmitters, ions, photons, food tastants and odorants, and are renowned drug targets.
Małgorzata M. Kogut‐Günthel   +11 more
wiley   +1 more source

Home - About - Disclaimer - Privacy