CYP17A1

(redirected from CYP17)

CYP17A1

A gene on chromosome 10q24.3 that encodes a member of the cytochrome P450 superfamily of enzymes, which catalyse reactions involved in drug metabolism and synthesis of cholesterol, steroids and other lipids. CYP17A1 localises to the endoplasmic reticulum and has 17 alpha-hydroxylase and 17, 20-lyase activities; it is a key enzyme in the steroidogenic pathway that produces progestins, mineralocorticoids, glucocorticoids, androgens and oestrogens.

Molecular pathology
CYP17A1 mutations are associated with isolated steroid-17 alpha-hydroxylase deficiency, 17-alpha-hydroxylase/17, 20-lyase deficiency, pseudohermaphroditism and adrenal hyperplasia.
References in periodicals archive ?
Although the authors did not examine the mechanism of action of progesterone up-regulation, previous work suggested a direct inhibition of the CYP17 (cytochrome P450 17A1) lyase reaction, independent of ER action (Zhang et al.
may cause hypertension, hypokalemia, and fluid retention as a consequence of increased mineralocorticoid levels resulting from CYP17 inhibition.
39) Looking further at a possible hereditary component to PCOS, women with the disease tend to have a hyperactive production of CYP17 enzyme that is responsible for forming androgens from DHEA-S at those sites.
Abiraterone acetate (abiraterone) is a novel oral agent that specifically inhibits the activity of CYP17 (17-[alpha]-hydroxylase/17, 20-lyase), a key enzyme required for bio-synthesis of androgens in the adrenal glands and in tumour tissues.
Abiraterone acetate is the prodrug of abiraterone that works by inhibiting the CYP17 enzyme complex in the androgen biosynthesis pathway which is important in the production of testosterone and other androgens.
Among specific topics are pharmacogenomics and personalized medicines in cancer treatment, inhibiting DNA repair as a therapeutic target, the renaissance of CYP17 inhibitors for treating prostate cancer, antibody-drug conjugates delivering DNA cytotoxics, and failure modes in anticancer drug discovery and development.
Phase I clinical trial of a selective inhibitor of CYP17, abiraterone acetate, confirms thatcastration-resistant-prostate cancer commonly remains hormone driven.
In preclinical studies, galeterone has demonstrated a novel triple mechanism of action to disrupt the growth and survival of prostate cancer cells by acting as a highly potent and selective CYP17 lyase inhibitor, a potent androgen receptor (AR) antagonist, and by decreasing AR levels in prostate tumors.
This trend continued in 2011 and 2012, when 3 therapies, the CYP17 inhibitor abiraterone acetate (Zytiga; Janssen Biotech) (7), the bone-targeting agent [sup.
2011), like abiraterone acetate, a specific inhibitor of CYP17, a key to androgen and estrogen synthesis, and MDV3100, an AR antagonist, both currently being tested in Phase Ill clinical trials in castration-resistant prostate cancer (Attard et al.
Zytiga works by bringing testosterone production down to a trickle by blocking enzyme CYP17, and so staving the cancer's growth which is fuelled by testosterone production.
It is postulated that these women have a hyperactive production of CYP17 enzyme, which is responsible for forming androgens in the ovaries and adrenals (from dehydroepiandrosterone sulfate, DHEA-S) (Hopkinson 1998).