An In Vitro Assay for Evaluation of Small-Molecule Inhibitors of Cholesterol Absorption

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 inhibit...

Full description

Saved in:
Bibliographic Details
Published in:Angewandte Chemie (International ed.) 2004-09, Vol.43 (35), p.4653-4656
Main Authors: Kværnø, Lisbet, Ritter, Tobias, Werder, Moritz, Hauser, Helmut, Carreira, Erick M.
Format: Article
Language:English
Subjects:
Absorption - drug effects
Animals
cholesterol
Cholesterol - chemistry
Cholesterol - metabolism
Cricetinae
Glycosides - chemistry
Hydrolysis
inhibitors
medicinal chemistry
membranes
Molecular Structure
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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).
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.200460348