Synthesis of a biotin-tagged photoaffinity probe of 2-azetidinone cholesterol absorption inhibitors.

Bioorg Med Chem

Aventis Pharma Deutschland GmbH, Disease Group Metabolic Diseases Industriepark Höchst, Building G 879 D-65926, Frankfurt am Main, Germany.

Published: April 2003

The design and synthesis of a biotin-tagged photoreactive analogue C-4 of the cholesterol absorption inhibitor Ezetimibe is described. Photoaffinity labeling of intestinal brush border membrane vesicles with C-4 and subsequent streptavidin-biotin chromatography leads to selective extraction of a 145 kDa integral membrane protein as the molecular target for cholesterol absorption inhibitors.

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http://dx.doi.org/10.1016/s0968-0896(03)00047-6DOI Listing

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