An in vitro assay for evaluation of small-molecule inhibitors of cholesterol absorption

被引：36
|
作者：
Kværno, L
Ritter, T
Werder, M
Hauser, H
Carreira, EM
机构：
[1] ETH Honggerberg, Organ Chem Lab, CH-8093 Zurich, Switzerland
[2] ETH Honggerberg, Inst Biochem, CH-8093 Zurich, Switzerland
来源：
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2004年 / 43卷 / 35期
关键词：
cholesterol; inhibitors; medicinal chemistry; membranes;
D O I：
10.1002/anie.200460348
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
Giving cholesterol the brush off: An intestinal brush border membrane vesicle assay has been devised for the convenient in vitro testing of small molecules for inhibition of cholesterol absorption. The assay was used to identify new nonhydrolyzable glycosides as potent cholesterol-absorption inhibitors and an oxazolidinone as an effective replacement of the β-lactam scaffold of ezetimibe (1).
引用
收藏
页码：4653 / 4656
页数：4
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