Acta Pharmaceutica Sinica 2013;48(1):25-31

Advances in the study of steroidal inhibitors of cytochrome P45017alpha.

Juan-Juan DU 1 ; Hong-Li CHEN ; Yuan-Chao LI

Affiliations

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Country

China

Language

Chinese

MeSH

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.