Conformational Analysis of Tetragastrin in Comparison with Antigastric 5,1-Benzothiazocines

概要

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Conformational analysis of the minimum active unit of gastrin, tetragastrin (Trp-Met-Asp-Phe-NH_2), led to the formulation of common hypothetical receptor binding moieties with 5,1-benzothiazocines, these moieties being a benzene ring, a nonbasic nitrogen and a hydrophobic group. A molecular mechanics calculation study of tetragastrin was carried out in an attempt to find a stereochemical correlation with a representative 5,1-benzothiazocine, RS-2039,which had been structurally elucidated by X-ray crystallographic analysis. Several stable conformers of tetragastrin were discovered to have a close approximation of the 3-dimensional array of receptor binding moieties to that of RS-2039. It has thus been theoretically demonstrated that gastrins and 5,1-benzothiazocines could bind with an identical receptor.
社団法人日本薬学会の論文
1986-02-25