Targeting G protein-coupled receptor signalling by blocking G proteins
AP Campbell, AV Smrcka - Nature reviews Drug discovery, 2018 - nature.com
G protein-coupled receptors (GPCRs) are the largest class of drug targets, largely owing to
their druggability, diversity and physiological efficacy. Many drugs selectively target specific …
their druggability, diversity and physiological efficacy. Many drugs selectively target specific …
Complex pharmacology of free fatty acid receptors
G protein-coupled receptors (GPCRs) are historically the most successful family of drug
targets. In recent times it has become clear that the pharmacology of these receptors is far …
targets. In recent times it has become clear that the pharmacology of these receptors is far …
TRUPATH, an open-source biosensor platform for interrogating the GPCR transducerome
G-protein-coupled receptors (GPCRs) remain major drug targets, despite our incomplete
understanding of how they signal through 16 non-visual G-protein signal transducers …
understanding of how they signal through 16 non-visual G-protein signal transducers …
[HTML][HTML] Illuminating G-protein-coupling selectivity of GPCRs
Heterotrimetic G proteins consist of four subfamilies (G s, G i/o, G q/11, and G 12/13) that
mediate signaling via G-protein-coupled receptors (GPCRs), principally by receptors binding …
mediate signaling via G-protein-coupled receptors (GPCRs), principally by receptors binding …
The neuropeptide neuromedin U stimulates innate lymphoid cells and type 2 inflammation
The type 2 cytokines interleukin (IL)-4, IL-5, IL-9 and IL-13 have important roles in
stimulating innate and adaptive immune responses that are required for resistance to …
stimulating innate and adaptive immune responses that are required for resistance to …
[HTML][HTML] Lack of beta-arrestin signaling in the absence of active G proteins
M Grundmann, N Merten, D Malfacini, A Inoue… - Nature …, 2018 - nature.com
G protein-independent, arrestin-dependent signaling is a paradigm that broadens the
signaling scope of G protein-coupled receptors (GPCRs) beyond G proteins for numerous …
signaling scope of G protein-coupled receptors (GPCRs) beyond G proteins for numerous …
[HTML][HTML] A serotonergic axon-cilium synapse drives nuclear signaling to alter chromatin accessibility
Chemical synapses between axons and dendrites mediate neuronal intercellular
communication. Here, we describe a synapse between axons and primary cilia: the axo …
communication. Here, we describe a synapse between axons and primary cilia: the axo …
[HTML][HTML] Structures of the glucocorticoid-bound adhesion receptor GPR97–Go complex
Adhesion G-protein-coupled receptors (GPCRs) are a major family of GPCRs, but limited
knowledge of their ligand regulation or structure is available,–. Here we report that …
knowledge of their ligand regulation or structure is available,–. Here we report that …
Common coupling map advances GPCR-G protein selectivity
Two-thirds of human hormones and one-third of clinical drugs act on membrane receptors
that couple to G proteins to achieve appropriate functional responses. While G protein …
that couple to G proteins to achieve appropriate functional responses. While G protein …
[HTML][HTML] Heterotrimeric Gq proteins act as a switch for GRK5/6 selectivity underlying β-arrestin transducer bias
K Kawakami, M Yanagawa, S Hiratsuka… - Nature …, 2022 - nature.com
Signaling-biased ligands acting on G-protein-coupled receptors (GPCRs) differentially
activate heterotrimeric G proteins and β-arrestins. Although a wealth of structural knowledge …
activate heterotrimeric G proteins and β-arrestins. Although a wealth of structural knowledge …