The selectivity of beauveriolide derivatives in inhibition toward the two isozymes of acyl-CoA: Cholesterol acyltransferase

Taichi Ohshiro, Daisuke Matsuda, Kenichiro Nagai, Takayuki Doi, Toshiaki Sunazuka, Takashi Takahashi, Lawrence Lee Rudel, Satoshi Omura, Hiroshi Tomoda

研究成果: Article査読

16 被引用数 (Scopus)

抄録

The selectivity of synthetic beauveriolide derivatives in inhibition toward the two isozymes of acyl-CoA : cholesterol acyltrasferase (ACAT), ACAT1 and ACAT2, was studied in cell-based assays using ACAT1- or ACAT2-expressing Chinese hamster ovary (CHO) cells. NBV274, 285 and 300 showed ACAT1 selective inhibition similar to that of natural beauveriolides I and III, NBV345 inhibited both isozymes with similar potency, but NBV281, 331 and 249 were found to selectively inhibit the ACAT2 isozyme. The structure-activity relationships indicated that a subtle structural difference in beauveriolide derivatives can affect the selectivity of inhibition of the ACAT isozymes.

本文言語English
ページ(範囲)377-381
ページ数5
ジャーナルChemical and Pharmaceutical Bulletin
57
4
DOI
出版ステータスPublished - 2009
外部発表はい

ASJC Scopus subject areas

  • 化学 (全般)
  • 創薬

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