GPCRs in Intracellular Compartments: New Targets for Drug Discovery
Biomolecules, 2022 The architecture of eukaryotic cells is defined by extensive membrane-delimited compartments, which entails separate metabolic processes that would otherwise interfere with each other, leading to functional differences between cells.
Irene Fasciani +7 more
doaj +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
core +2 more sources
Lysophosphatidic Acid Signaling in Cancer Cells: What Makes LPA So Special?
Cells, 2021 Lysophosphatidic acid (LPA) refers to a family of simple phospholipids that act as ligands for G protein-coupled receptors. While LPA exerts effects throughout the body in normal physiological circumstances, its pathological role in cancer is of great ...
Pravita Balijepalli +2 more
doaj +1 more source
G-protein-coupled receptor kinases
Kidney International, 1996 beta-Adrenergic receptors are prototypes of the many G-protein-coupled receptors. Activation and inactivation of these receptors are regulated by multiple mechanisms which can affect either their function or their expression. The most obvious changes of such receptor systems are induced by activation of the receptors themselves by their respective ...
Lohse, Martin J. +3 more
openaire +2 more sources
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
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
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Mini G protein probes for active G protein–coupled receptors (GPCRs) in live cells
Journal of Biological Chemistry, 2018 G protein–coupled receptors (GPCRs) are key signaling proteins that regulate nearly every aspect of cell function. Studies of GPCRs have benefited greatly from the development of molecular tools to monitor receptor activation and downstream signaling ...
Qingwen Wan +6 more
semanticscholar +1 more source
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
core +4 more sources
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
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
core +1 more source