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.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Androstenedione / biosynthesis
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Androstenes
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Androstenols / chemical synthesis
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Androstenols / chemistry
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Androstenols / pharmacology
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Animals
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology
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Dehydroepiandrosterone / biosynthesis
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Dihydrotestosterone / metabolism
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology
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Humans
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Male
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Molecular Structure
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Pregnenolone / metabolism
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Progesterone / metabolism
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Prostatic Neoplasms / pathology
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Steroid 17-alpha-Hydroxylase / antagonists & inhibitors*
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Testosterone / biosynthesis
Substances
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Androstenes
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Androstenols
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Antineoplastic Agents
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Enzyme Inhibitors
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Dihydrotestosterone
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Testosterone
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Androstenedione
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Dehydroepiandrosterone
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Progesterone
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Pregnenolone
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Steroid 17-alpha-Hydroxylase
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abiraterone