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

被引:26
|
作者
Frick, W [1 ]
Bauer-Schäfer, A [1 ]
Bauer, J [1 ]
Girbig, F [1 ]
Corsiero, D [1 ]
Heuer, H [1 ]
Kramer, W [1 ]
机构
[1] Aventis Pharma Deutschland GmbH, Dis Grp Metab Dis Ind Pk Hochst, D-65926 Frankfurt, Germany
关键词
D O I
10.1016/S0968-0896(03)00047-6
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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. (C) 2003 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1639 / 1642
页数:4
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