Transporters as Drug Targets: Discovery and Development of NPC1L1 Inhibitors

被引：17

作者：

Betters, J. L. ^{[1
]}

Yu, L. ^{[1
]}

机构：

[1] Wake Forest Univ, Bowman Gray Sch Med, Dept Pathol, Winston Salem, NC 27103 USA

来源：

CLINICAL PHARMACOLOGY & THERAPEUTICS | 2010年 / 87卷 / 01期

关键词：

INTESTINAL CHOLESTEROL ABSORPTION; NIEMANN-PICK C1-LIKE-1; EZETIMIBE; MICE; RECEPTOR; BINDING; CELLS; HYPERCHOLESTEROLEMIA; PROTEIN; ACIDS;

D O I：

10.1038/clpt.2009.209

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The potent cholesterol absorption inhibitor ezetimibe was developed as a first-in-class drug for treating hypercholesterolemia even before its molecular target, Niemann-Pick C1-like 1 (NPC1L1), had been identified. The NPC1L1 protein mediates sterol transport across the enterocyte brush border membrane and is essential for intestinal cholesterol absorption, a major pathway controlling whole-body cholesterol homeostasis. An elucidation of the mechanism underlying NPC1L1-dependent cholesterol absorption would greatly facilitate the discovery and development of new cholesterol-lowering agents for treating hypercholesterolemia and other cholesterol-related metabolic disorders.

引用

页码：117 / 121

页数：5

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