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Structural insights into G protein-coupled receptor signaling [PDF]
Structural DynamicsG 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
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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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The Open Question of How GPCRs Interact with GPCR Kinases (GRKs)
Biomolecules, 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
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DEER Analysis of GPCR Conformational Heterogeneity
Biomolecules, 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
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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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Quantitative approaches for studying G protein-coupled receptor signalling and pharmacology.
J Cell SciPearce A +9 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 Kinases Take Central Stage
Cells, 2022 The relevance of the family of G protein-coupled receptor kinases (GRKs) is based on its key participation in the regulation and intracellular dynamics of the largest family of membrane receptors, namely G protein-coupled receptors (GPCRs) [...]
Federico Mayor, Cristina Murga
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