Du Juan-Juan, Chen Hong-Li, Li Yuan-Chao
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Yao Xue Xue Bao. 2013 Jan;48(1):25-31.
The steroidal enzyme cytochrome P45017alpha catalyzes the conversion of progesterone and pregnenolone into androgens, androstenedione and dehydroepiandrosterone, respectively, the direct precursors of estrogens and testosterone. Dihydrotestosterone is the principal active androgen in the prostate, testosterone is also an active stimulant of the growth of prostatic cancer tissue. Inhibition of this enzyme as a mechanism for inhibiting androgen biosynthesis could be a worthwhile therapeutic strategy for the treatment of PCA. In this paper, four categories of steroidal inhibitors of cytochrome P45017alpha will be reviewed, a diverse range of steroidal inhibitors had been synthesized and shown to be potent inhibitors of P45017alpha.
甾体酶细胞色素P45017α分别催化孕酮和孕烯醇酮转化为雄激素雄烯二酮和脱氢表雄酮，它们分别是雌激素和睾酮的直接前体。双氢睾酮是前列腺中的主要活性雄激素，睾酮也是前列腺癌组织生长的活性刺激物。抑制这种酶作为抑制雄激素生物合成的一种机制，可能是治疗前列腺癌的一种有价值的治疗策略。本文将综述细胞色素P45017α的四类甾体抑制剂，已经合成了多种甾体抑制剂，并证明它们是P45017α的有效抑制剂。
