Sigma Receptor Binding Assays
نویسندگان
چکیده
منابع مشابه
Label-Free Receptor Assays.
Label-free biosensors offer integrated, kinetic and multi-parametric measures of receptor biology and ligand pharmacology in whole cells. Being highly sensitive and pathway-unbiased, label-free receptor assays can be used to probe the systems cell biology including pleiotropic signaling of receptors, and to characterize the functional selectivity and phenotypic pharmacology of ligand molecules....
متن کاملSigma 1 receptor modulation of G-protein-coupled receptor signaling: potentiation of opioid transduction independent from receptor binding.
sigma Ligands modulate opioid actions in vivo, with agonists diminishing morphine analgesia and antagonists enhancing the response. Using human BE(2)-C neuroblastoma cells that natively express opioid receptors and human embryonic kidney (HEK) cells transfected with a cloned mu opioid receptor, we now demonstrate a similar modulation of opioid function, as assessed by guanosine 5'-O-(3-[(35)S]t...
متن کاملIdentification of the PGRMC1 protein complex as the putative sigma-2 receptor binding site
The sigma-2 receptor, whose gene remains to be cloned, has been validated as a biomarker for tumour cell proliferation. Here we report the use of a novel photoaffinity probe, WC-21, to identify the sigma-2 receptor-binding site. WC-21, a sigma-2 ligand containing both a photoactive azide moiety and a fluorescein isothiocyanate group, irreversibly labels sigma-2 receptors in rat liver; the membr...
متن کاملSequence analysis, structure and binding site prediction of Sigma 1 receptor protein by in silico method
Sigma 1 Receptor is a subtype of opioid receptor that participates in membrane remodeling and cellular differentiation in the nervous system. Sigma1 Receptor protein with amino acid length ranging from 229 is widely distributed in the liver and moderately in the intestine, kidney, white pulp of the spleen, adrenal gland, brain, placenta and the lung. In this study, the three dimensional structu...
متن کاملAntagonists show GTP-sensitive high-affinity binding to the sigma-1 receptor.
BACKGROUND AND PURPOSE Sigma-1 receptors are atypical receptors with potentially two transmembrane domains. Antagonists require doses significantly higher than their published affinities to have biological effects. We have reassessed the binding characteristics of these ligands and found antagonists bind to high- and low-affinity states not distinguished by agonists. EXPERIMENTAL APPROACH The...
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ژورنال
عنوان ژورنال: Current Protocols in Pharmacology
سال: 2015
ISSN: 1934-8282,1934-8290
DOI: 10.1002/0471141755.ph0134s71