[HTML][HTML] Activation pathway of a G protein-coupled receptor uncovers conformational intermediates as targets for allosteric drug design
S Lu, X He, Z Yang, Z Chai, S Zhou, J Wang… - Nature …, 2021 - nature.com
G protein-coupled receptors (GPCRs) are the most common proteins targeted by approved
drugs. A complete mechanistic elucidation of large-scale conformational transitions …
drugs. A complete mechanistic elucidation of large-scale conformational transitions …
Molecular mechanism of biased signaling in a prototypical G-protein-coupled receptor
Over one-third of current drugs target G-protein-coupled receptors (GPCRs). Leveraging the
phenomenon of biased signaling, where different ligands that bind to the same GPCR …
phenomenon of biased signaling, where different ligands that bind to the same GPCR …
Deciphering biased-agonism complexity reveals a new active AT1 receptor entity
A Saulière, M Bellot, H Paris, C Denis, F Finana… - Nature chemical …, 2012 - nature.com
Functional selectivity of G protein–coupled receptor (GPCR) ligands toward different
downstream signals has recently emerged as a general hallmark of this receptor class …
downstream signals has recently emerged as a general hallmark of this receptor class …
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 …
[HTML][HTML] Distinctive activation mechanism for angiotensin receptor revealed by a synthetic nanobody
The angiotensin II (AngII) type 1 receptor (AT1R) is a critical regulator of cardiovascular and
renal function and is an important model for studies of G-protein-coupled receptor (GPCR) …
renal function and is an important model for studies of G-protein-coupled receptor (GPCR) …
Identification of ligand-specific G-protein coupled receptor states and prediction of downstream efficacy via data-driven modeling
O Fleetwood, L Delemotte - Biophysical Journal, 2021 - cell.com
G protein-coupled receptors (GPCRs) shift between inactive non-signalling states and active
signalling states, to which intracellular binding partners can bind. Extracellular binding of …
signalling states, to which intracellular binding partners can bind. Extracellular binding of …
Ligand-Dependent Activation and Deactivation of the Human Adenosine A2A Receptor
G-protein-coupled receptors (GPCRs) are membrane proteins with critical functions in
cellular signal transduction, representing a primary class of drug targets. Acting by direct …
cellular signal transduction, representing a primary class of drug targets. Acting by direct …
[HTML][HTML] Differences in allosteric communication pipelines in the inactive and active states of a GPCR
S Bhattacharya, N Vaidehi - Biophysical journal, 2014 - cell.com
G-protein-coupled receptors (GPCRs) are membrane proteins that allosterically transduce
the signal of ligand binding in the extracellular (EC) domain to couple to proteins in the …
the signal of ligand binding in the extracellular (EC) domain to couple to proteins in the …
Differential β-arrestin–dependent conformational signaling and cellular responses revealed by angiotensin analogs
B Zimmerman, A Beautrait, B Aguila, R Charles… - Science …, 2012 - science.org
The angiotensin type 1 receptor (AT1R) and its octapeptide ligand, angiotensin II (AngII),
engage multiple downstream signaling pathways, including those mediated by …
engage multiple downstream signaling pathways, including those mediated by …
[HTML][HTML] Structural determinants for binding, activation, and functional selectivity of the angiotensin AT1 receptor
P Balakumar, G Jagadeesh - Journal of molecular …, 2014 - jme.bioscientifica.com
The renin–angiotensin system (RAS) plays an important role in the pathophysiology of
cardiovascular disorders. Pharmacologic interventions targeting the RAS cascade have led …
cardiovascular disorders. Pharmacologic interventions targeting the RAS cascade have led …