SELECTIVE INHIBITORS OF PLACENTAL STEROID AROMATASE

本提案的目标包括设计、综合和 人胎盘芳香化酶（雌激素）特异性抑制剂的评价 合成酶）。 这些抑制剂包括酶产生的不可逆的 抑制剂以及竞争性可逆抑制剂。 特异性抑制剂 胎盘组织和其他组织中的人类生物合成。 他们可能 在雌激素依赖性肿瘤的研究和治疗中也有价值， 以及研究雄激素外周芳构化在 男性内分泌学 这些抑制剂的机制研究应该是进一步研究的兴趣。 检查芳香化酶的作用机制。 共价标记 通过放射性标记的抑制剂纯化的酶可以提供有价值的信息 酶的活性位点 芳香化酶的化学模型已经被 开发，这个模型将在酶方面进行评估， 过程的立体化学和动力学行为。

The objectives of this proposal include the design, synthesis an devaluation 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 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 be of interest in further examination of the mechanism of action of aromatase. Covalent labeling of purified enzyme by radiolabeled inhibitors may provide valuable information about the enzyme's active site. A chemical model for aromatase has been developed, and this model will be evaluated in terms of the enzymatic process's stereochemical and kinetic behavior.