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 …

Allosteric modulation of G protein-coupled receptor signaling

S Shen, C Zhao, C Wu, S Sun, Z Li, W Yan… - Frontiers in …, 2023 - frontiersin.org
G protein-coupled receptors (GPCRs), the largest family of transmembrane proteins,
regulate a wide array of physiological processes in response to extracellular signals …

A µ-opioid receptor modulator that works cooperatively with naloxone

ES O'Brien, VA Rangari, A El Daibani, SO Eans… - Nature, 2024 - nature.com
The µ-opioid receptor (µOR) is a well-established target for analgesia, yet conventional
opioid receptor agonists cause serious adverse effects, notably addiction and respiratory …

Positive allosteric modulation of a GPCR ternary complex

WAC Burger, CJ Draper-Joyce, C Valant… - Science …, 2024 - science.org
The activation of a G protein–coupled receptor (GPCR) leads to the formation of a ternary
complex between agonist, receptor, and G protein that is characterized by high-affinity …

Stabilization of pre-existing neurotensin receptor conformational states by β-arrestin-1 and the biased allosteric modulator ML314

F Bumbak, JB Bower, SC Zemmer, A Inoue… - Nature …, 2023 - nature.com
Abstract The neurotensin receptor 1 (NTS1) is a G protein-coupled receptor (GPCR) with
promise as a drug target for the treatment of pain, schizophrenia, obesity, addiction, and …

Unraveling allostery within the angiotensin II type 1 receptor for Gαq and β-arrestin coupling

Y Cao, WJC van der Velden, Y Namkung… - Science …, 2023 - science.org
G protein–coupled receptors engage both G proteins and β-arrestins, and their coupling can
be biased by ligands and mutations. Here, to resolve structural elements and mechanisms …

Multiple recent HCAR2 structures demonstrate a highly dynamic ligand binding and G protein activation mode

A Shenol, R Tenente, M Lückmann, TM Frimurer… - Nature …, 2024 - nature.com
A surprisingly clear picture of the allosteric mechanism connecting G protein-coupled
receptor agonists with G protein binding—and back–is revealed by a puzzle of thirty novel …

The M3 muscarinic acetylcholine receptor can signal through multiple G protein families

JS Smith, AS Hilibrand, MA Skiba… - Molecular …, 2024 - Elsevier
The M3 muscarinic acetylcholine receptor (M 3 R) is a G protein–coupled receptor (GPCR)
that regulates important physiologic processes, including vascular tone, bronchoconstriction …

Functional dynamics of G protein-coupled receptors reveal new routes for drug discovery

P Conflitti, E Lyman, MSP Sansom… - Nature Reviews Drug …, 2025 - nature.com
G protein-coupled receptors (GPCRs) are the largest human membrane protein family that
transduce extracellular signals into cellular responses. They are major pharmacological …

Progress on the development of Class A GPCR‐biased ligands

P Morales, MM Scharf, M Bermudez… - British Journal of …, 2024 - Wiley Online Library
Class AG 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 …