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- W2153523207 abstract "A ligand containing an SNpys group, Le. 3-nitro-2-pyridinesulfenyl linked to a mercapto (or thiol) group, can bind covalently to a free mercapto group to form a disulfide bond via the thiol-disulfide exchange reaction. This SNpys chemistry has been successfully applied to the discriminative aflfinity labeling of ft and 8 opioid receptors with SNpys-contain ing enkephalins [Yasunaga, T. et aL (1996) J. Biochem. 120, 459–465]. In order to explore the mercapto groups conserved at or near the ligand binding sites of three opioid receptor subtypes, we synthesized two Cys(Npys)-containing analogs of dynorphin A, namely, [D-Ala3, Cys(Npys)8]dynorphin A-(l-9) amide (1) and [D-Ala2, Cys(Npys)12]dynorphin A-(l-13) amide (2). When rat (/i and 8) or guinea pig (x) brain membranes were incubated with these Cys(Npys)-containing dynorphin A analogs and then assayed for inhibition of the binding of DAGO (/i), deltorphin II (8), and U-69593 (x), the number of receptors decreased sharply, depending upon the concentrations of these Cys(Npys)-containing dynorphin A analogs. It was found that dynorphin A analogs 1 and 2 effectively label μ receptors (EC50=27-33 nM), but also label 8 receptors fairly well (160–180 nM). However, for x receptors they showed drastically different potencies as to affinity labeling; Le., EC50=210 nM for analog 1, but 10, 000 nM for analog 2. Analog 2 labeled x receptors about 50 times more weakly than analog 1. These results suggested that dynorphin A analog 1 labels the Cys residues conserved in μ, 8, and x receptors, whereas analog 2 only labels the Cys residues conserved in μ and 8 receptors." @default.
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- W2153523207 date "1999-07-01" @default.
- W2153523207 modified "2023-10-16" @default.
- W2153523207 title "Exploration of Universal Cysteines in the Binding Sites of Three Opioid Receptor Subtypes by Disulfide-Bonding Affinity Labeling with Chemically Activated Thiol-Containing Dynorphin A Analogs" @default.
- W2153523207 doi "https://doi.org/10.1093/oxfordjournals.jbchem.a022430" @default.
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