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 …
the versatility to regulate diverse physiological processes. Interestingly, many GPCR ligands …
New insights into modes of GPCR activation
W Wang, Y Qiao, Z Li - Trends in pharmacological sciences, 2018 - cell.com
In classical G-protein-coupled receptor (GPCR) activation, GPCRs couple to a variety of
heterotrimeric G proteins on the membrane and then activate downstream signaling …
heterotrimeric G proteins on the membrane and then activate downstream signaling …
Angiotensin analogs with divergent bias stabilize distinct receptor conformations
Summary" Biased" G protein-coupled receptor (GPCR) agonists preferentially activate
pathways mediated by G proteins or β-arrestins. Here, we use double electron-electron …
pathways mediated by G proteins or β-arrestins. Here, we use double electron-electron …
Biased ligands at G-protein-coupled receptors: promise and progress
JD Violin, AL Crombie, DG Soergel, MW Lark - Trends in pharmacological …, 2014 - cell.com
Drug discovery targeting G protein-coupled receptors (GPCRs) is no longer limited to
seeking agonists or antagonists to stimulate or block cellular responses associated with a …
seeking agonists or antagonists to stimulate or block cellular responses associated with a …
Angiotensin and biased analogs induce structurally distinct active conformations within a GPCR
Biased agonists of G protein–coupled receptors (GPCRs) preferentially activate a subset of
downstream signaling pathways. In this work, we present crystal structures of angiotensin II …
downstream signaling pathways. In this work, we present crystal structures of angiotensin II …
Teaching old receptors new tricks: biasing seven-transmembrane receptors
Abstract Seven-transmembrane receptors (7TMRs; also known as G protein-coupled
receptors) are the largest class of receptors in the human genome and are common targets …
receptors) are the largest class of receptors in the human genome and are common targets …
Biased agonism: An emerging paradigm in GPCR drug discovery
G protein coupled receptors have historically been one of the most druggable classes of
cellular proteins. The members of this large receptor gene family couple to primary effectors …
cellular proteins. The members of this large receptor gene family couple to primary effectors …
β-arrestins and cell signaling
SM DeWire, S Ahn, RJ Lefkowitz… - Annu. Rev. Physiol …, 2007 - annualreviews.org
Upon their discovery, β-arrestins 1 and 2 were named for their capacity to sterically hinder
the G protein coupling of agonist-activated seven-transmembrane receptors, ultimately …
the G protein coupling of agonist-activated seven-transmembrane receptors, ultimately …
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) …
Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery
T Kenakin, LJ Miller - Pharmacological reviews, 2010 - ASPET
It is useful to consider seven transmembrane receptors (7TMRs) as disordered proteins able
to allosterically respond to a number of binding partners. Considering 7TMRs as allosteric …
to allosterically respond to a number of binding partners. Considering 7TMRs as allosteric …