Common activation mechanism of class A GPCRs

Q Zhou, D Yang, M Wu, Y Guo, W Guo, L Zhong, X Cai… - Elife, 2019 - elifesciences.org
Class A G-protein-coupled receptors (GPCRs) influence virtually every aspect of human
physiology. Understanding receptor activation mechanism is critical for discovering novel …

Structural basis for G protein-coupled receptor activation

A Manglik, AC Kruse - Biochemistry, 2017 - ACS Publications
G protein-coupled receptors (GPCRs) are critical regulators of human physiology and make
up the largest single class of therapeutic drug targets. Although GPCRs regulate highly …

G protein-coupled receptors (GPCRs): advances in structures, mechanisms, and drug discovery

M Zhang, T Chen, X Lu, X Lan, Z Chen… - Signal Transduction and …, 2024 - nature.com
G protein-coupled receptors (GPCRs), the largest family of human membrane proteins and
an important class of drug targets, play a role in maintaining numerous physiological …

Structural insights into ligand recognition and selectivity for classes A, B, and C GPCRs

SM Lee, JM Booe, AA Pioszak - European journal of pharmacology, 2015 - Elsevier
The G protein-coupled receptor (GPCR) superfamily constitutes the largest collection of cell
surface signaling proteins with approximately 800 members in the human genome. GPCRs …

Pharmacogenomic and structural analysis of constitutive G protein–coupled receptor activity

MJ Smit, HF Vischer, RA Bakker… - Annu. Rev …, 2007 - annualreviews.org
G protein–coupled receptors (GPCRs) respond to a chemically diverse plethora of signal
transduction molecules. The notion that GPCRs also signal without an external chemical …

[HTML][HTML] How genetic errors in GPCRs affect their function: possible therapeutic strategies

H Stoy, VV Gurevich - Genes & diseases, 2015 - Elsevier
Activating and inactivating mutations in numerous human G protein-coupled receptors
(GPCRs) are associated with a wide range of disease phenotypes. Here we use several …

Structure-function of the G protein–coupled receptor superfamily

V Katritch, V Cherezov… - Annual review of …, 2013 - annualreviews.org
During the past few years, crystallography of G protein–coupled receptors (GPCRs) has
experienced exponential growth, resulting in the determination of the structures of 16 distinct …

Lifting the lid on GPCRs: the role of extracellular loops

M Wheatley, D Wootten, MT Conner… - British journal of …, 2012 - Wiley Online Library
GPCRs exhibit a common architecture of seven transmembrane helices (TMs) linked by
intracellular loops and extracellular loops (ECLs). Given their peripheral location to the site …

Critical features for biosynthesis, stability, and functionality of a G protein-coupled receptor uncovered by all-versus-all mutations

KM Schlinkmann, A Honegger… - Proceedings of the …, 2012 - National Acad Sciences
The structural features determining efficient biosynthesis, stability in the membrane and,
after solubilization, in detergents are not well understood for integral membrane proteins …

Exploring a role for heteromerization in GPCR signalling specificity

R Rozenfeld, LA Devi - Biochemical Journal, 2011 - portlandpress.com
The critical involvement of GPCRs (G-protein-coupled receptors) in nearly all physiological
processes, and the presence of these receptors at the interface between the extracellular …