title: [Advances in the study of steroidal inhibitors of cytochrome P45017alpha].
abstract: 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.
authors.affiliation: State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
authors.forename: Juan-Juan
authors.initials: JJ
authors.lastname: Du
authors.forename: Hong-Li
authors.initials: HL
authors.lastname: Chen
authors.forename: Yuan-Chao
authors.initials: YC
authors.lastname: Li
mesh_terms: D000735:Androstenedione / Q000096:biosynthesis; D000736:Androstenes; D000737:Androstenols / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D003687:Dehydroepiandrosterone / Q000096:biosynthesis; D013196:Dihydrotestosterone / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D008297:Male; D015394:Molecular Structure; D011284:Pregnenolone / Q000378:metabolism; D011374:Progesterone / Q000378:metabolism; D011471:Prostatic Neoplasms / Q000473:pathology; D013254:Steroid 17-alpha-Hydroxylase / Q000037:antagonists & inhibitors*; D013739:Testosterone / Q000096:biosynthesis
chemical_list: D000736:Androstenes; D000737:Androstenols; D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D013196:Dihydrotestosterone; D013739:Testosterone; D000735:Androstenedione; D003687:Dehydroepiandrosterone; D011374:Progesterone; D011284:Pregnenolone; D013254:Steroid 17-alpha-Hydroxylase; C089740:abiraterone