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Structural insights into G protein-coupled receptor signaling [PDF]

open access: yesStructural Dynamics
G protein-coupled receptors (GPCRs) are the largest single family of transmembrane proteins encoded in the human genome, and they are among the most successful classes of therapeutic drug targets of all time.
Andrew Kruse
doaj   +2 more sources

G protein-coupled receptor kinases. [PDF]

open access: yesAnnual Review of Biochemistry, 1998
G protein–coupled receptor kinases (GRKs) constitute a family of six mammalian serine/threonine protein kinases that phosphorylate agonist-bound, or activated, G protein–coupled receptors (GPCRs) as their primary substrates. GRK-mediated receptor phosphorylation rapidly initiates profound impairment of receptor signaling, or desensitization.
J. Pitcher, N. Freedman, R. Lefkowitz
semanticscholar   +3 more sources

AXOR12, a Novel Human G Protein-coupled Receptor, Activated by the Peptide KiSS-1*

open access: hybridJournal of Biological Chemistry, 2001
A novel human G protein-coupled receptor named AXOR12, exhibiting 81% homology to the rat orphan receptor GPR54, was cloned from a human brain cDNA library.
A. Muir   +21 more
semanticscholar   +2 more sources

G-Protein-Coupled Receptors [PDF]

open access: yesJournal of Biological Chemistry, 1998
G-protein-coupled receptors (GPCRs) constitute a huge family of membrane receptors to numerous hormones, neurotransmitters and diverse compounds. A large part of cardiovascular and neurological pharmacology is based upon the knowledge of these receptors and on the identification of molecules able to interfere with them, in an agonistic or antagonistic ...
Tae H. Ji, Mathis Grossmann, Inhae Ji
  +6 more sources

The Open Question of How GPCRs Interact with GPCR Kinases (GRKs)

open access: yesBiomolecules, 2021
G protein-coupled receptors (GPCRs), which regulate a vast number of eukaryotic processes, are desensitized by various mechanisms but, most importantly, by the GPCR kinases (GRKs).
M. Claire Cato   +6 more
doaj   +1 more source

DEER Analysis of GPCR Conformational Heterogeneity

open access: yesBiomolecules, 2021
G protein-coupled receptors (GPCRs) represent a large class of transmembrane helical proteins which are involved in numerous physiological signaling pathways and therefore represent crucial pharmacological targets.
Matthias Elgeti, Wayne L. Hubbell
doaj   +1 more source

G Protein-Coupled Receptors in Osteoarthritis [PDF]

open access: yesFrontiers in Endocrinology, 2022
Osteoarthritis (OA) is the most common chronic joint disease characterized, for which there are no available therapies being able to modify the progression of OA and prevent long-term disability. Critical roles of G-protein coupled receptors (GPCRs) have been established in OA cartilage degeneration, subchondral bone sclerosis and chronic pain. In this
Fanhua Wang   +4 more
openaire   +5 more sources

Lysophospholipid G Protein-coupled Receptors [PDF]

open access: yesJournal of Biological Chemistry, 2004
The many biological responses documented for lysophospholipids that include lysophosphatidic acid and sphingosine 1-phosphate can be mechanistically attributed to signaling through specific G protein-coupled receptors. At least nine receptors have now been identified, and the total number is likely to be larger.
Brigitte, Anliker, Jerold, Chun
openaire   +2 more sources

G Protein–Coupled Receptor Deorphanizations [PDF]

open access: yesAnnual Review of Pharmacology and Toxicology, 2013
G protein–coupled receptors (GPCRs) are major regulators of intercellular interactions. They initiate these actions by being activated by a wide variety of natural ligands. Historically, ligands were discovered first, but the advent of molecular biology reversed this trend.
Olivier, Civelli   +5 more
openaire   +2 more sources

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