発癌プロモーターの作用機作解明への有機化学的アプローチ

概要

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Teleocidins are potent tumor promoters produced by actinomycetes. Simpler in structure and of higher stability than other potent tumor promoters, phorbol esters and aplysiatoxins, they are particularly useful for investigating the mechanism of tumor promotion using various synthetic teleocidin analogues. The authors found a teleocidin-producing actinomycete, <I>Streptoverticillium blastmyceticum</I> NA 34-17, which has a characteristic feature of producing (-) -indolactam-Val (ILV) in quantity, the fundamental structure of teleocidins. Using this micro-organism, they have synthesized various ILV derivatives, examined the structure-activity relationships and prepared new fluorescent or photolabile ILV derivatives for the receptor analysis of tumor promoters. They have also investigated the metabolism and biosynthesis of teleocidins. This review mainly deals with the structure-activity relationships of teleocidins, syntheses of fluorescent or photolabile ILV derivatives and their application on the receptor analysis of tumor promoters.
社団法人有機合成化学協会の論文