Results 21 to 30 of about 92,178 (306)

GPCR photopharmacology

open access: yesMolecular and Cellular Endocrinology, 2019
New technologies for spatial and temporal remote control of G protein-coupled receptors (GPCRs) are necessary to unravel the complexity of GPCR signalling in cells, tissues and living organisms. An effective approach, recently developed, consists on the design of light-operated ligands whereby light-dependent GPCR activity regulation can be achieved ...
Maria Ricart-Ortega   +2 more
openaire   +3 more sources

Specific and behaviorally consequential astrocyte Gq GPCR signaling attenuation in vivo with iβARK.

open access: yesNeuron, 2021
Astrocytes respond to neurotransmitters and neuromodulators using G-protein-coupled receptors (GPCRs) to mediate physiological responses. Despite their importance, there has been no method to genetically, specifically, and effectively attenuate astrocyte
J. Nagai   +11 more
semanticscholar   +1 more source

Impact of GPCR Structures on Drug Discovery.

open access: yesCell, 2020
Structures of 70 unique G protein-coupled receptors (GPCRs) have been determined, with over 370 structures in total bound to different ligands and the receptors in various conformational states.
M. Congreve   +3 more
semanticscholar   +1 more source

Platelet calcium signaling by G-protein coupled and ITAM-linked receptors regulating anoctamin-6 and procoagulant activity

open access: yesPlatelets, 2021
Most agonists stimulate platelet Ca2+ rises via G-protein coupled receptors (GPCRs) or ITAM-linked receptors (ILRs). Well studied are the GPCRs stimulated by the soluble agonists thrombin (PAR1, PAR4), ADP (P2Y1, P2Y12), and thromboxane A2 (TP ...
Delia I. Fernández   +2 more
doaj   +1 more source

An Insight into GPCR and G-Proteins as Cancer Drivers

open access: yesCells, 2021
G-protein-coupled receptors (GPCRs) are the largest family of cell surface signaling receptors known to play a crucial role in various physiological functions, including tumor growth and metastasis.
P. Chaudhary, Soochong Kim
semanticscholar   +1 more source

GPCR Signaling Regulation: The Role of GRKs and Arrestins

open access: yesFrontiers in Pharmacology, 2019
Every animal species expresses hundreds of different G protein-coupled receptors (GPCRs) that respond to a wide variety of external stimuli. GPCRs-driven signaling pathways are involved in pretty much every physiological function and in many pathologies.
V. Gurevich, E. Gurevich
semanticscholar   +1 more source

Angiotensin and biased analogs induce structurally distinct active conformations within a GPCR

open access: yesScience, 2020
Choosing the drug to fit the protein Many approved drugs bind to G protein–coupled receptors (GPCRs). A challenge in targeting GPCRs is that different ligands preferentially activate different signaling pathways.
L. Wingler   +9 more
semanticscholar   +1 more source

A computational model for GPCR-ligand interaction prediction

open access: yesJournal of Integrative Bioinformatics, 2020
G protein-coupled receptors (GPCRs) play an essential role in critical human activities, and they are considered targets for a wide range of drugs. Accordingly, based on these crucial roles, GPCRs are mainly considered and focused on pharmaceutical ...
Karimi Shiva   +3 more
doaj   +1 more source

GPCR homo-oligomerization [PDF]

open access: yesCurrent Opinion in Cell Biology, 2019
G protein-coupled receptors (GPCRs) are an extensive class of trans-plasma membrane proteins that function to regulate a wide range of physiological functions. Despite a general perception that GPCRs exist as monomers an extensive literature has examined whether GPCRs can also form dimers and even higher-order oligomers, and if such organization ...
Milligan, Graeme   +2 more
openaire   +2 more sources

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