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- W2082220272 abstract "Neurokinin-2 receptor (NK2R) binding of [3H]-SR48968, a piperidinyl antagonist, is inhibited by methanethiosulfonate ethylammonium (MTSEA) in a time- and concentration-dependent manner. By the systematic alanine replacement of putative loop and transmembrane region cysteine residues (Cys4, Cys81, Cys167, Cys262, Cys281, Cys308, and Cys309), we have determined that MTSEA perturbs [3H]-SR48968 binding by modifying Cys167 in transmembrane helix 4. Data were substantiated using glycine, serine, and threonine substitutions of Cys167. MTSEA preferentially modifies cysteine residues that are in proximity to a negatively charged environment. Hence, aspartate and glutamate residues were systematically substituted with leucine or valine, respectively, and the inhibitory effects of MTSEA on [3H]-SR48968 binding were reevaluated to determine those acidic residues close to the MTSEA binding crevice. Most significantly, substitution of Asp5 in the receptor's extreme N-terminus abolished the effects of MTSEA on [3H]-SR48968 binding. Therefore, our data would suggest close association of the extreme N-terminus with the extracellular surfaces of helices 4 and 3 in the NK2R in forming a binding crevice for MTSEA. The inhibition of SR48968 binding appears to result from loss of the SR48968 binding conformation of Gln166 induced by MTSEA when it is coupled to Cys167. Hence, it is proposed that there is mutually exclusive hydrogen bonding of SR48968 and MTSEA to Gln166." @default.
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- W2082220272 date "2004-02-25" @default.
- W2082220272 modified "2023-10-11" @default.
- W2082220272 title "Evidence for the Proximity of the Extreme N-Terminus of the Neurokinin-2 (NK<sub>2</sub>) Tachykinin Receptor to Cys<sup>167</sup> in the Putative Fourth Transmembrane Helix" @default.
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- W2082220272 doi "https://doi.org/10.1021/bi035475s" @default.
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