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 …

G protein-coupled receptors: structure-and function-based drug discovery

D Yang, Q Zhou, V Labroska, S Qin… - Signal transduction and …, 2021 - nature.com
As one of the most successful therapeutic target families, G protein-coupled receptors
(GPCRs) have experienced a transformation from random ligand screening to knowledge …

The G-protein coupled receptor family: actors with many faces

L George, C Arnau, P Leonardo - Current pharmaceutical …, 2012 - ingentaconnect.com
G-protein coupled receptors (GPCRs) comprise the largest family of proteins in our body,
which have many important physiological functions and are implicated in the …

Emerging opportunities for allosteric modulation of G-protein coupled receptors

CIA Wang, RJ Lewis - Biochemical pharmacology, 2013 - Elsevier
Their ubiquitous nature, wide cellular distribution and versatile molecular recognition and
signalling help make G-protein binding receptors (GPCRs) the most important class of …

G-protein-coupled receptors: from classical modes of modulation to allosteric mechanisms

TM Bridges, CW Lindsley - ACS chemical biology, 2008 - ACS Publications
Heterotrimeric G-protein-coupled receptors (GPCRs) represent a large protein family
responsible for mediating extracellular to intracellular signaling within a broad range of …

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 …

Chemical diversity in the G protein-coupled receptor superfamily

M Vass, AJ Kooistra, D Yang, RC Stevens… - Trends in …, 2018 - cell.com
G protein-coupled receptors (GPCRs) are the largest family of cell signaling transmembrane
proteins that can be modulated by a plethora of chemical compounds. Systematic …

Functional selectivity in GPCR signaling: understanding the full spectrum of receptor conformations

E Goupil, SA Laporte, TE Hebert - Mini reviews in medicinal …, 2012 - ingentaconnect.com
The great versatility of G protein-coupled receptors (GPCRs), in terms of both their ability to
bind different types of ligands and initiate a large number of distinct cellular signaling events …

Elucidating the interactome of G protein-coupled receptors and receptor activity-modifying proteins

IB Kotliar, E Lorenzen, JM Schwenk, DL Hay… - Pharmacological …, 2023 - ASPET
G protein-coupled receptors (GPCRs) are known to interact with several other classes of
integral membrane proteins that modulate their biology and pharmacology. However, the …

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 …