title: The selectivity of beauveriolide derivatives in inhibition toward the two isozymes of acyl-CoA: cholesterol acyltransferase.
abstract: 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.
authors.affiliation: Graduate School of Pharmaceutical Sciences, Kitasato University, Tokyo, Japan.
authors.forename: Taichi
authors.initials: T
authors.lastname: Ohshiro
authors.forename: Daisuke
authors.initials: D
authors.lastname: Matsuda
authors.forename: Kenichiro
authors.initials: K
authors.lastname: Nagai
authors.forename: Takayuki
authors.initials: T
authors.lastname: Doi
authors.forename: Toshiaki
authors.initials: T
authors.lastname: Sunazuka
authors.forename: Takashi
authors.initials: T
authors.lastname: Takahashi
authors.forename: Lawrence Lee
authors.initials: LL
authors.lastname: Rudel
authors.forename: Satoshi
authors.initials: S
authors.lastname: Omura
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Tomoda