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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 …
an important class of drug targets, play a role in maintaining numerous physiological …
Allosteric modulation of G protein-coupled receptor signaling
G protein-coupled receptors (GPCRs), the largest family of transmembrane proteins,
regulate a wide array of physiological processes in response to extracellular signals …
regulate a wide array of physiological processes in response to extracellular signals …
A µ-opioid receptor modulator that works cooperatively with naloxone
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 …
opioid receptor agonists cause serious adverse effects, notably addiction and respiratory …
Positive allosteric modulation of a GPCR ternary complex
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 …
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
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 …
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 …
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 …
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 …
that regulates important physiologic processes, including vascular tone, bronchoconstriction …
Functional dynamics of G protein-coupled receptors reveal new routes for drug discovery
G protein-coupled receptors (GPCRs) are the largest human membrane protein family that
transduce extracellular signals into cellular responses. They are major pharmacological …
transduce extracellular signals into cellular responses. They are major pharmacological …
Progress on the development of Class A GPCR‐biased ligands
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 …
roles in cell signalling and their importance as drug targets. Although numerous drugs in the …