SELECTIVE INHIBITORS OF PLACENTAL STEROID AROMATASE

胎盘类固醇芳香酶的选择性抑制剂

• 批准号: 3311688
• 负责人: CECIL H ROBINSON
• 金额: $ 12.8万
• 依托单位: JOHNS HOPKINS UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 1978
• 资助国家: 美国
• 起止时间: 1978-09-01 至 1989-05-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3311688
• 关键词: androgen analog; androgen inhibitor; androstenedione; chemical structure function; drug design /synthesis /production; estrogen analog; estrogen inhibitor; hormone inhibitor; hormone metabolism; hormone regulation /control mechanism; human tissue; ligase; placental hormones; steroid hormone

The objectives of this proposal are the design, synthesis and evaluation of specific inhibitors of human placental aromatase (estrogen synthetase). These inhibitors include enzyme-generated irreversible inhibitors and also competitive reversible inhibitors. Specific inhibitors of human placental aromatase should be valuable tools in studying estrogen biosynthesis in placental tissue and in other tissues. They may also be of value in the study and treatment of estrogen-dependent tumors, and in studying the role played by peripheral aromatization of androgen in male endocrinology. Mechanistic studies with these inhibitors should also be of interest in further examination of the mechanism of action of aromatase.

本提案的目标是设计、综合和评价 人胎盘芳香化酶（雌激素合成酶）的特异性抑制剂。 这些抑制剂包括酶产生的不可逆抑制剂， 竞争性可逆抑制剂。 人胎盘特异性抑制剂 芳香化酶应该是研究雌激素生物合成的有价值的工具， 胎盘组织和其他组织中。 它们也可能是有价值的， 研究和治疗雌激素依赖性肿瘤，并在研究的作用 雄激素外周芳构化在男性内分泌中起重要作用。 这些抑制剂的机制研究也应该是感兴趣的， 进一步研究芳香化酶的作用机制。