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 …

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 …

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 …

The molecular basis of G protein–coupled receptor activation

WI Weis, BK Kobilka - Annual review of biochemistry, 2018 - annualreviews.org
G protein–coupled receptors (GPCRs) mediate the majority of cellular responses to external
stimuli. Upon activation by a ligand, the receptor binds to a partner heterotrimeric G protein …

[HTML][HTML] Structural studies of G protein-coupled receptors

D Zhang, Q Zhao, B Wu - Molecules and cells, 2015 - Elsevier
G protein-coupled receptors (GPCRs) constitute the largest and the most physiologically
important membrane protein family that recognizes a variety of environmental stimuli, and …

[HTML][HTML] G protein-coupled receptors: the evolution of structural insight

SB Gacasan, DL Baker, AL Parrill - AIMS biophysics, 2017 - ncbi.nlm.nih.gov
G protein-coupled receptors (GPCR) comprise a diverse superfamily of over 800 proteins
that have gained relevance as biological targets for pharmaceutical drug design. Although …

A new era of GPCR structural and chemical biology

S Granier, B Kobilka - Nature chemical biology, 2012 - nature.com
G protein–coupled receptors (GPCRs) are versatile molecular machines that regulate the
majority of physiological responses to chemically diverse hormones and neurotransmitters …

Conformational basis of G protein-coupled receptor signaling versatility

LM Wingler, RJ Lefkowitz - Trends in cell biology, 2020 - cell.com
G protein-coupled receptors (GPCRs) are privileged structural scaffolds in biology that have
the versatility to regulate diverse physiological processes. Interestingly, many GPCR ligands …

Allostery at G protein-coupled receptor homo-and heteromers: uncharted pharmacological landscapes

NJ Smith, G Milligan - Pharmacological reviews, 2010 - ASPET
For many years seven transmembrane domain G protein-coupled receptors (GPCRs) were
thought to exist and function exclusively as monomeric units. However, evidence both from …

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 …