Mutations in G protein–coupled receptors: mechanisms, pathophysiology and potential therapeutic approaches

T Schöneberg, I Liebscher, P Insel - Pharmacological reviews, 2021 - Elsevier
There are approximately 800 annotated G protein–coupled receptor (GPCR) genes, making
these membrane receptors members of the most abundant gene family in the human …

Opportunities for therapeutic antibodies directed at G-protein-coupled receptors

CJ Hutchings, M Koglin, WC Olson… - Nature reviews Drug …, 2017 - nature.com
G-protein-coupled receptors (GPCRs) are activated by a diverse range of ligands, from large
proteins and proteases to small peptides, metabolites, neurotransmitters and ions. They are …

Translating the force—mechano-sensing GPCRs

C Wilde, J Mitgau, T Suchý… - American Journal of …, 2022 - journals.physiology.org
Incorporating mechanical cues into cellular responses allows us to experience our direct
environment. Specialized cells can perceive and discriminate between different physical …

Mechano-dependent signaling by Latrophilin/CIRL quenches cAMP in proprioceptive neurons

N Scholz, C Guan, M Nieberler, A Grotemeyer… - Elife, 2017 - elifesciences.org
Adhesion-type G protein-coupled receptors (aGPCRs), a large molecule family with over 30
members in humans, operate in organ development, brain function and govern …

New paradigms in GPCR drug discovery

KA Jacobson - Biochemical pharmacology, 2015 - Elsevier
G protein-coupled receptors (GPCRs) remain a major domain of pharmaceutical discovery.
The identification of GPCR lead compounds and their optimization are now structure-based …

Truncating mutations in the adhesion G protein-coupled receptor G2 gene ADGRG2 cause an X-linked congenital bilateral absence of vas deferens

O Patat, A Pagin, A Siegfried, V Mitchell… - The American Journal of …, 2016 - cell.com
In 80% of infertile men with obstructive azoospermia caused by a congenital bilateral
absence of the vas deferens (CBAVD), mutations are identified in the cystic fibrosis …

Conformational coupling between extracellular and transmembrane domains modulates holo-adhesion GPCR function

SP Kordon, K Cechova, SJ Bandekar, K Leon… - Nature …, 2024 - nature.com
Abstract Adhesion G Protein-Coupled Receptors (aGPCRs) are key cell-adhesion
molecules involved in numerous physiological functions. aGPCRs have large multi-domain …

Gq activity-and β-arrestin-1 scaffolding-mediated ADGRG2/CFTR coupling are required for male fertility

DL Zhang, YJ Sun, ML Ma, Y Wang, H Lin, RR Li… - Elife, 2018 - elifesciences.org
Luminal fluid reabsorption plays a fundamental role in male fertility. We demonstrated that
the ubiquitous GPCR signaling proteins Gq and β-arrestin-1 are essential for fluid …

[HTML][HTML] The adhesion G protein-coupled receptor GPR56/ADGRG1 is an inhibitory receptor on human NK cells

GW Chang, CC Hsiao, YM Peng, FAV Braga… - Cell reports, 2016 - cell.com
Natural killer (NK) cells possess potent cytotoxic mechanisms that need to be tightly
controlled. Here, we explored the regulation and function of GPR56/ADGRG1, an adhesion …

Adhesion G protein–coupled receptor Gpr126/Adgrg6 is essential for placental development

R Torregrosa-Carrión, R Piñeiro-Sabarís… - Science …, 2021 - science.org
Mutations in the G protein–coupled receptor GPR126/ADGRG6 cause human diseases,
including defective peripheral nervous system (PNS) myelination. To study GPR126 …