Threonine 180 Is Required for G-protein-coupled Receptor Kinase 3- and β-Arrestin 2-mediated Desensitization of the µ-Opioid Receptor in Xenopus Oocytes [PDF]
To determine the sites in the µ-opioid receptor (MOR) critical for agonist-dependent desensitization, we constructed and coexpressed MORs lacking potential phosphorylation sites along with G-protein activated inwardly rectifying potassium channels ...
Celvert, Jeremy P. +4 more
core
Regulators of G protein signalling proteins in the human myometrium [PDF]
The contractile state of the human myometrium is controlled by extracellular signals that promote relaxation or contraction. Many of these signals function through G proteincoupled receptors at the cell surface, stimulating heterotrimeric G proteins and ...
Abramow-Newerly +52 more
core +1 more source
Imeglimin attenuates liver fibrosis by inhibiting vesicular ATP release from hepatic stellate cells
Imeglimin, at clinically relevant concentrations, inhibits vesicular ATP accumulation and release from hepatic stellate cells, thereby attenuating purinergic signaling and reducing fibrogenic activation. This mechanism reveals a newly identified antifibrotic action of imeglimin beyond glycemic control.
Seiji Nomura +8 more
wiley +1 more source
The Interaction of Phospholipase C-{beta}3 with Shank2 Regulates mGluR-mediated Calcium Signal [PDF]
Phospholipase C-{beta} isozymes that are activated by G protein-coupled receptors (GPCR) and heterotrimeric G proteins carry a PSD-95/Dlg/ZO-1 (PDZ) domain binding motif at their C terminus. Through interactions with PDZ domains, this motif may endow the
Hwang, Jong-Ik +5 more
core
Functional classification of G-Protein coupled receptors, based on their specific ligand coupling patterns [PDF]
Functional identification of G-Protein Coupled Receptors (GPCRs) is one of the current focus areas of pharmaceutical research. Although thousands of GPCR sequences are known, many of them re- main as orphan sequences (the activating ligand is unknown ...
Bakır, Burcu, Sezerman, Uğur
core +1 more source
Nearly 2000 G protein-coupled receptors (GPCRs) have been reported since bovine opsin was cloned in 1983 (1) and the b-adrenergic receptor in 1986 (2).
T. Ji, M. Grossmann, Inhae Ji
semanticscholar +1 more source
Cancer cell death induced by the NAD antimetabolite Vacor discloses the antitumor potential of SARM1
Vacor, a compound converted into the toxic metabolite Vacor adenine dinucleotide (VAD) by the nicotinamide salvage pathway enzymes NAMPT and NMNAT2, exhibits antitumor activity by inducing rapid and complete NAD depletion. We report that Vacor toxicity is limited to cell lines expressing high levels of SARM1, a NAD glycohydrolase.
Giuseppe Ranieri +5 more
wiley +1 more source
Probing the role of the cation–π interaction in the binding sites of GPCRs using unnatural amino acids [PDF]
We describe a general application of the nonsense suppression methodology for unnatural amino acid incorporation to probe drug–receptor interactions in functional G protein-coupled receptors (GPCRs), evaluating the binding sites of both the M2 muscarinic
Ballesteros +31 more
core +3 more sources
RAD50 missense variants differentially affect the DNA damage response and mitotic progression
RAD50 incorporates into the MRN complex and initiates the DNA damage response. Furthermore, RAD50 promotes mitotic progression. RAD50 missense variants capable of forming an MRN complex supported the DNA damage response and mitotic features to different extents in complementation experiments, indicating these functions are separable and might impact ...
Hanna Redeker +9 more
wiley +1 more source
G protein-coupled receptor (GPCR) activation is followed rapidly by adaptive changes that serve to diminish the responsiveness of a cell to further stimulation.
S.S.G. Ferguson
doaj +1 more source

