Results 11 to 20 of about 92,511 (354)
GPCR kinase knockout cells reveal the impact of individual GRKs on arrestin binding and GPCR regulation [PDF]
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 +3 more sources
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
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
Acta Pharmacologica Sinica, 2012 G-protein-coupled receptors (GPCRs), which represent the largest gene family in the human genome, play a crucial role in multiple physiological functions as well as in tumor growth and metastasis. For instance, various molecules like hormones, lipids, peptides and neurotransmitters exert their biological effects by binding to these seven-transmembrane ...
Lappano R, MAGGIOLINI, Marcello
openaire +3 more sources
GPCR heteromers: An overview of their classification, function and physiological relevance
Frontiers in Endocrinology, 2022 G protein-coupled receptors (GPCRs) are capable of interacting to form higher order structures such as homomers and heteromers. Heteromerisation in particular has implications for receptor function, with research showing receptors can attain unique ...
Natasha C. Dale +2 more
semanticscholar +1 more source
Accelerating GPCR Drug Discovery With Conformation-Stabilizing VHHs
Frontiers in Molecular Biosciences, 2022 The human genome encodes 850 G protein-coupled receptors (GPCRs), half of which are considered potential drug targets. GPCRs transduce extracellular stimuli into a plethora of vital physiological processes.
T. Laeremans +10 more
semanticscholar +1 more source
, 2011 In this chapter, we describe a method for detecting the ubiquitination status of G protein-coupled receptors (GPCRs). This involves co-expression of a GPCR with an epitope-tagged ubiquitin construct in a -heterologous mammalian expression system. Stimulus-dependent modification of the GPCR by -ubiquitin is detected by immunoprecipitation and subsequent
Adriana, Caballero, Adriano, Marchese
openaire +2 more sources
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