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.
Zhiwei Wang +5 more
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Positive allosteric modulators of the a-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor [PDF]
, 2010 L-glutamate is the major excitatory neurotransmitter in the mammalian central nervous system (CNS) and plays a fundamental role in the control of motor function, cognition and mood.
Grove, Simon J .A. +4 more
core +1 more source
M3 muscarinic acetylcholine receptor facilitates the endocytosis of mu opioid receptor mediated by morphine independently of the formation of heteromeric complexes [PDF]
, 2017 Morphine inefficiency to induce the internalization of mu opioid (MOP) receptors observed in numerous experimental models constitutes a paradigm of G-protein coupled receptor (GPCR) functional selectivity.
Alvarez-Curto, Elisa +2 more
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G3: Genes, Genomes, Genetics, 2018 G protein-coupled receptors are 7-pass transmembrane receptors that couple to heterotrimeric G proteins to mediate cellular responses to a diverse array of stimuli.
Alexander Bowitch +3 more
doaj +1 more source
Modelization of Thermal Fluctuations in G Protein-Coupled Receptors
, 2005 We simulate the electrical properties of a device realized by a G protein coupled receptor (GPCR), embedded in its membrane and in contact with two metallic electrodes through which an external voltage is applied.
Akimov, V. +7 more
core +1 more source
The melanocortin receptors and their accessory proteins. [PDF]
, 2013 The five melanocortin receptors (MCRs) named MC1R-MC5R have diverse physiological roles encompassing pigmentation, steroidogenesis, energy homeostasis and feeding behavior as well as exocrine function.
Chan, LF +3 more
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Effects on Breathing of Agonists to μ-opioid or GABA\u3csub\u3eA\u3c/sub\u3e Receptors Dialyzed into the Ventral Respiratory Column of Awake and Sleeping Goats [PDF]
, 2017 Pulmonary ventilation (V̇I) in awake and sleeping goats does not change when antagonists to several excitatory G protein-coupled receptors are dialyzed unilaterally into the ventral respiratory column (VRC).
Burgraff, Nicholas J. +7 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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Molecular architecture of Gαo and the structural basis for RGS16-mediated deactivation [PDF]
, 2008 Heterotrimeric G proteins relay extracellular cues from heptahelical transmembrane receptors to downstream effector molecules. Composed of an α subunit with intrinsic GTPase activity and a βγ heterodimer, the trimeric complex dissociates upon receptor ...
Berman +34 more
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Multiple endocytic pathways of G protein-coupled receptors delineated by GIT1 sensitivity. [PDF]
, 2000 Recently, we identified a GTPase-activating protein for the ADP ribosylation factor family of small GTP-binding proteins that we call GIT1. This protein initially was identified as an interacting partner for the G protein-coupled receptor kinases, and ...
Achiriloaie, M +6 more
core +1 more source