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G-Protein-Coupled Receptors [PDF]
Journal 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
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G Protein-Coupled Receptors in Osteoarthritis [PDF]
Frontiers 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
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Lysophospholipid G Protein-coupled Receptors [PDF]
Journal 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
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G Protein–Coupled Receptor Deorphanizations [PDF]
Annual 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
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Powdered G-Protein-Coupled Receptors [PDF]
The Journal of Physical Chemistry Letters, 2016 Preparation and storage of functional membrane proteins such as G-protein-coupled receptors (GPCRs) are crucial to the processes of drug delivery and discovery. Here, we describe a method of preparing powdered GPCRs using rhodopsin as the prototype. We purified rhodopsin in CHAPS detergent with low detergent to protein ratio so the bulk of the sample ...
Suchithranga M D C, Perera +2 more
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G Protein–Coupled Receptor Heteromers [PDF]
Annual Review of Pharmacology and Toxicology, 2016 G protein–coupled receptors (GPCRs) compose one of the largest families of membrane proteins involved in intracellular signaling. They are involved in numerous physiological and pathological processes and are prime candidates for drug development. Over the past decade, an increasing number of studies have reported heteromerization between GPCRs.
Gomes, Ivone +5 more
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G PROTEIN–COUPLED RECEPTOR KINASES [PDF]
Annual 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 A, Pitcher +2 more
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G-protein coupled receptor structure
Biochimica et Biophysica Acta (BBA) - Biomembranes, 2007 Because of their central role in regulation of cellular function, structure/function relationships for G-protein coupled receptors (GPCR) are of vital importance, yet only recently have sufficient data been obtained to begin mapping those relationships. GPCRs regulate a wide range of cellular processes, including the senses of taste, smell, and vision,
Yeagle, Philip L., Albert, Arlene D.
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G Protein–Coupled Receptor Rhodopsin [PDF]
Annual Review of Biochemistry, 2006 The rhodopsin crystal structure provides a structural basis for understanding the function of this and other G protein–coupled receptors (GPCRs). The major structural motifs observed for rhodopsin are expected to carry over to other GPCRs, and the mechanism of transformation of the receptor from inactive to active forms is thus likely conserved ...
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G-protein-coupled receptor kinases
Trends in Biochemical Sciences, 1991 Rhodopsin kinase and the beta-adrenergic receptor kinase (beta ARK) catalyse the phosphorylation of the activated forms of the G-protein-coupled receptors, rhodopsin and the beta 2-adrenergic receptor (beta 2AR), respectively. The interaction between receptor and kinase is independent of second messengers and appears to involve a multipoint attachment ...
Palczewskl, Krzvsztof +1 more
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