Frick Wendelin, Bauer-Schäfer Andrea, Bauer Jochen, Girbig Frank, Corsiero Daniel, Heuer Hubert, Kramer Werner
Aventis Pharma Deutschland GmbH, Disease Group Metabolic Diseases Industriepark Höchst, Building G 879 D-65926, Frankfurt am Main, Germany.
Bioorg Med Chem. 2003 Apr 17;11(8):1639-42. doi: 10.1016/s0968-0896(03)00047-6.
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.
描述了胆固醇吸收抑制剂依泽替米贝的生物素标记光反应类似物C-4的设计与合成。用C-4对肠刷状缘膜囊泡进行光亲和标记,随后通过链霉亲和素-生物素色谱法可选择性提取一种145 kDa的整合膜蛋白,作为胆固醇吸收抑制剂的分子靶点。