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


  • This research was supported by a CTI grant (6813.2 BTS-LS) and Lipideon AG. L.K. was supported by a fellowship from The Technical University of Denmark. T.R. thanks the Fonds der Chemischen Industrie for a Kekulé Fellowship.


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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).

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