STRUCTURE OF HUMAN MEMBRANE CYTOCHROME P450 INVOLVED IN ANDROGEN BIOSYNTHESIS

参与雄激素生物合成的人膜细胞色素P450的结构

• 批准号: 8362388
• 负责人: Emily E Scott
• 金额: $ 0.19万
• 依托单位: STANFORD UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 2011
• 资助国家: 美国
• 起止时间: 2011-03-01 至 2012-02-29
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/8362388
• 关键词: Anabolism; Androgens; Clinical Trials; Complex; Cytochrome P450; Drug Design; Enzymes; Estrogens; Funding; Grant; Human; Malignant neoplasm of prostate; Membrane; National Center for Research Resources; Principal Investigator; Radiation; Research; Research Infrastructure; Resources; Source; Structure; United States National Institutes of Health; base; cancer therapy; cost; design; improved; inhibitor/antagonist; malignant breast neoplasm; structural biology

This subproject is one of many research subprojects utilizing the resources provided by a Center grant funded by NIH/NCRR. Primary support for the subproject and the subproject's principal investigator may have been provided by other sources, including other NIH sources. The Total Cost listed for the subproject likely represents the estimated amount of Center infrastructure utilized by the subproject, not direct funding provided by the NCRR grant to the subproject or subproject staff. There are currently no structures of this important enzyme involved in androgen (and estrogen) synthesis. 80% of prostate cancers are dependent on androgens. Inhibitors of this cytochrome P450 are currently in clinical trials for prostate and breast cancer. We have crystals of the human enzyme in complex with one of the leading clinical trial candidates. This structure will allow us to improve current inhibitors and to use structure-based drug design to improve/design other inhibitors to increase selectivity and improve cancer treatment.

该副本是利用资源的众多研究子项目之一 由NIH/NCRR资助的中心赠款提供。对该子弹的主要支持 而且，副投影的主要研究员可能是其他来源提供的 包括其他NIH来源。 列出的总费用可能 代表subproject使用的中心基础架构的估计量， NCRR赠款不直接向子弹或副本人员提供的直接资金。 目前，这种重要酶在雄激素（和雌激素）合成中尚无结构。 80％的前列腺癌取决于雄激素。 该细胞色素P450的抑制剂目前正在前列腺和乳腺癌的临床试验中。 我们将人类酶的晶体与领先的临床试验候选者之一复合在一起。 这种结构将使我们能够改善当前的抑制剂，并使用基于结构的药物设计来改善/设计其他抑制剂，以提高选择性并改善癌症治疗。