Key result
A novel intestinal brush border membrane vesicle assay successfully identified new nonhydrolyzable glycosides and an oxazolidinone as potent in vitro inhibitors of cholesterol absorption.
A novel in vitro intestinal brush border membrane vesicle assay can effectively screen and identify small-molecule inhibitors of cholesterol absorption.
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May aid in vitro screening for cholesterol absorption inhibitors; leaves open in vivo efficacy and clinical translation.
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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Kværnø et al. (2004) studied this question. A novel intestinal brush border membrane vesicle assay successfully identified new nonhydrolyzable glycosides and an oxazolidinone as potent in vitro inhibitors of cholesterol absorption.
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