Results 11 to 20 of about 92,178 (306)
Nature Communications, 2022 GPCR kinases (GRKs) regulate GPCR interactions and thus functions. Here, the authors report a comprehensive panel of GRK knockout cells, used to assess the GRK-specific β-arrestin recruitment. Selective engagement of GRKs induces distinct GPCR–β-arrestin
J. Drube +15 more
doaj +2 more sources
GPCR activation and GRK2 assembly by a biased intracellular agonist
Nature, 2023 Structural studies on the complex containing G-protein-coupled receptor kinase 2 (GRK2), neurotensin receptor 1 (NTSR1), Gα_q and the arrestin-biased ligand SBI-553 provide insights into these interactions and a foundation for the design of arrestin ...
J. Duan +18 more
semanticscholar +1 more source
Structure, function and drug discovery of GPCR signaling
Molecular Biomedicine, 2023 G protein-coupled receptors (GPCRs) are versatile and vital proteins involved in a wide array of physiological processes and responses, such as sensory perception (e.g., vision, taste, and smell), immune response, hormone regulation, and ...
Lin Cheng +12 more
semanticscholar +1 more source
GPCR activation mechanisms across classes and macro/microscales
Nature Structural & Molecular Biology, 2021 Two-thirds of human hormones and one-third of clinical drugs activate ~350 G-protein-coupled receptors (GPCR) belonging to four classes: A, B1, C and F.
A. Hauser +7 more
semanticscholar +1 more source
Common coupling map advances GPCR-G protein selectivity
bioRxiv, 2022 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 transducers from literature are annotated in the Guide to Pharmacology database,
A. Hauser +6 more
semanticscholar +1 more source
“TRUPATH, an Open-Source Biosensor Platform for Interrogating the GPCR Transducerome”
Nature Chemical Biology, 2020 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 (collectively named the transducerome) to exert their actions.
Reid H. J. Olsen +10 more
semanticscholar +1 more source
Biased Allosteric Modulators: New Frontiers in GPCR Drug Discovery.
TIPS - Trends in Pharmacological Sciences, 2021 G protein-coupled receptors (GPCRs) are the largest class of cell surface receptors in the genome and the most successful family of targets of FDA-approved drugs.
L. Slosky, M. Caron, L. Barak
semanticscholar +1 more source
GPCRdb in 2021: integrating GPCR sequence, structure and function
Nucleic Acids Res., 2020 G protein-coupled receptors (GPCRs) form both the largest family of membrane proteins and drug targets, mediating the action of one-third of medicines. The GPCR database, GPCRdb serves >4 000 researchers every month and offers reference data, analysis of
A. Kooistra +7 more
semanticscholar +1 more source
The mechanism for ligand activation of the GPCR–G protein complex
Proceedings of the National Academy of Sciences of the United States of America, 2022 Significance We report the detailed atomistic mechanism for how molecules such as morphine, dopamine, or epinephrine binding outside of a cell to a G protein–coupled receptor (GPCR) in the cell membrane cause a G protein (GP) bound at the inside of the ...
Amirhossein Mafi +2 more
semanticscholar +1 more source
Cell, 2022 G protein-coupled receptors (GPCRs) relay extracellular stimuli into specific cellular functions. Cells express many different GPCRs, but all these GPCRs signal to only a few second messengers such as cAMP.
Selma E. Anton +10 more
semanticscholar +1 more source