Functional diversification of cell signaling by GPCR localization
MJ Klauer, BKA Willette, NG Tsvetanova - Journal of Biological Chemistry, 2024 - jbc.org
G protein-coupled receptors (GPCRs) are the largest family of cell surface receptors and a
critical class of regulators of mammalian physiology. Also known as seven transmembrane …
critical class of regulators of mammalian physiology. Also known as seven transmembrane …
Know your molecule: pharmacological characterization of drug candidates to enhance efficacy and reduce late-stage attrition
T Kenakin - Nature Reviews Drug Discovery, 2024 - nature.com
Despite advances in chemical, computational and biological sciences, the rate of attrition of
drug candidates in clinical development is still high. A key point in the small-molecule …
drug candidates in clinical development is still high. A key point in the small-molecule …
GLP-1R signaling neighborhoods associate with the susceptibility to adverse drug reactions of incretin mimetics
G protein-coupled receptors are important drug targets that engage and activate signaling
transducers in multiple cellular compartments. Delineating therapeutic signaling from …
transducers in multiple cellular compartments. Delineating therapeutic signaling from …
Structural insights into the activation and inhibition of CXC chemokine receptor 3
H Jiao, B Pang, A Liu, Q Chen, Q Pan… - Nature Structural & …, 2024 - nature.com
The chemotaxis of CD4+ type 1 helper cells and CD8+ cytotoxic lymphocytes, guided by
interferon-inducible CXC chemokine 9–11 (CXCL9–11) and CXC chemokine receptor 3 …
interferon-inducible CXC chemokine 9–11 (CXCL9–11) and CXC chemokine receptor 3 …
[HTML][HTML] CXCL9/10-engineered dendritic cells promote T cell activation and enhance immune checkpoint blockade for lung cancer
Immune checkpoint blockade (ICB) with PD-1/PD-L1 inhibition has revolutionized the
treatment of non-small cell lung cancer (NSCLC). Durable responses, however, are …
treatment of non-small cell lung cancer (NSCLC). Durable responses, however, are …
G protein–coupled receptor endocytosis generates spatiotemporal bias in β-arrestin signaling
The stabilization of different active conformations of G protein–coupled receptors is thought
to underlie the varying efficacies of biased and balanced agonists. Here, profiling the …
to underlie the varying efficacies of biased and balanced agonists. Here, profiling the …
Phosphorylation barcodes direct biased chemokine signaling at CXCR3
G protein-coupled receptor (GPCR)-biased agonism, selective activation of certain signaling
pathways relative to others, is thought to be directed by differential GPCR phosphorylation" …
pathways relative to others, is thought to be directed by differential GPCR phosphorylation" …
GPCR kinases differentially modulate biased signaling downstream of CXCR3 depending on their subcellular localization
Some G protein–coupled receptors (GPCRs) demonstrate biased signaling such that
ligands of the same receptor exclusively or preferentially activate certain downstream …
ligands of the same receptor exclusively or preferentially activate certain downstream …
Arrestin‐centred interactions at the membrane and their conformational determinants
More than 30 years after their discovery, arrestins are recognised multiprotein scaffolds that
play essential roles in G protein‐coupled receptor (GPCR) regulation and signalling …
play essential roles in G protein‐coupled receptor (GPCR) regulation and signalling …
Phosphorylation patterns in the AT1R C-terminal tail specify distinct downstream signaling pathways
Different ligands stabilize specific conformations of the angiotensin II type 1 receptor (AT1R)
that direct distinct signaling cascades mediated by heterotrimeric G proteins or β-arrestin …
that direct distinct signaling cascades mediated by heterotrimeric G proteins or β-arrestin …