文章基本信息

标题：Identification and pharmacological characterization of cholesterol-5,6-epoxide hydrolase as a target for tamoxifen and AEBS ligands
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作者：Philippe de Medina ; Michael R. Paillasse ; Gregory Segala 等
期刊名称：Proceedings of the National Academy of Sciences
印刷版ISSN：0027-8424
电子版ISSN：1091-6490
出版年度：2010
卷号：107
期号：30
页码：13520-13525
DOI：10.1073/pnas.1002922107
语种：English
出版社：The National Academy of Sciences of the United States of America
摘要：The microsomal antiestrogen binding site (AEBS) is a high-affinity target for the antitumor drug tamoxifen and its cognate ligands that mediate breast cancer cell differentiation and apoptosis. The AEBS, a hetero-oligomeric complex composed of 3{beta}-hydroxysterol-{Delta}8-{Delta}7-isomerase (D8D7I) and 3{beta}-hydroxysterol-{Delta}7-reductase (DHCR7), binds different structural classes of ligands, including ring B oxysterols. These oxysterols are inhibitors of cholesterol-5,6-epoxide hydrolase (ChEH), a microsomal epoxide hydrolase that has yet to be molecularly identified. We hypothesized that the AEBS and ChEH might be related entities. We show that the substrates of ChEH, cholestan-5{alpha
关键词：breast cancer ; chemoprevention ; cholesterol metabolism ; oxysterol ; docosahexaenoic acid