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The enzyme that makes androgens in the testes, the adrenal glands and prostate tumours themselves. Abiraterone blocks it, cutting androgen production below what castration alone achieves.
CYP17A1 catalyses two steps, 17-alpha-hydroxylation and 17,20-lyase cleavage, that convert pregnenolone and progesterone into DHEA and androstenedione, the precursors of testosterone and dihydrotestosterone. Because castration-resistant prostate cancer keeps making androgens from adrenal precursors and inside the tumour, blocking CYP17A1 with abiraterone lowers androgens further than castration and restores control in many patients. Blocking the enzyme also diverts steroid synthesis towards mineralocorticoids, which is why abiraterone is given with prednisone or prednisolone.
In plain words · The enzyme that makes androgens in the testes, the adrenal glands and prostate tumours themselves. Abiraterone blocks it, cutting androgen production below what castration alone achieves.
The enzyme that makes androgens in the testes, the adrenal glands and prostate tumours themselves. Abiraterone blocks it, cutting androgen production below what castration alone achieves.
Cytochrome P450 enzyme of the adrenal cortex, testis and prostate cancer cells; the rate-limiting step of androgen synthesis from pregnenolone.
2 products aim at CYP17A1 (17-alpha-hydroxylase/17,20-lyase): small molecules. Inhibitors are shaped to fit the enzyme's active site so the reaction the cancer relies on stops.
Tumour-associated overexpression: HPA finds the RNA cancer enhanced in cancer (Liver Hepatocellular Carcinoma (TCGA)) and tissue enriched in normal adrenal gland, so the tumour and the normal tissue it comes from share the target and the medicine relies on the difference in level. HPA CYP17A1: RNA tissue enriched (adrenal gland 8,353 nTPM); high antibody staining in 2 normal tissues. Distribution: 1 cancer family in the corpus carries a prevalence row, label threshold or catalogue link for it (Prostate cancer); Open Targets associates it with 2 specific cancer types at or above 0.5 (17,20-lyase deficiency, isolated, prostate cancer); the corpus evidence decides and the Open Targets list is quoted for comparison. (Rule 7 of scripts/fetch-target-specificity.ts.)
Sources: Human Protein Atlas CYP17A1 tissue; Human Protein Atlas CYP17A1 pathology; Open Targets ENSG00000148795 associations
First described 1987. Earliest sequence paper UniProt cites for the protein: Chung B.-C. et al, Proc. Natl. Acad. Sci. U.S.A, 1987, "Cytochrome P450c17 (steroid 17 alpha-hydroxylase/17,20 lyase): cloning of human adrenal and testis cDNAs indicates the same gene is expressed in both tissues". Source.
Cytochrome P450 enzyme of the adrenal cortex, testis and prostate cancer cells; the rate-limiting step of androgen synthesis from pregnenolone.
RNA: tissue enriched (adrenal gland 8,353 nTPM), detected in many normal tissues.
RNA cancer enhanced: Liver Hepatocellular Carcinoma 50 pTPM.
No cancer stained high; medium in colorectal cancer.
HPA CYP17A1 tissue · HPA CYP17A1 pathology · HPA protein class: FDA approved drug targets
Human Protein Atlas version 25.1, antibody staining at reliability approved, enhanced or supported; used under CC BY-SA 3.0. Staining counts are patients per level in the atlas cohort, not population prevalence.
| Cancer | Prevalence | Measure | Note | Source |
|---|---|---|---|---|
| Prostate cancer | nearly all% | Androgen-driven at diagnosis; abiraterone acts on androgen synthesis in almost every prostate cancer, resistance develops later | cancer.gov |
Approximate, population-level figures; the measure column says what was counted. Ranges show the midpoint as a bar.
An experimental prostate cancer tablet meant to work in men whose cancer makes a broken form of the androgen receptor. The trial designed to prove it collapsed.
A more selective version of abiraterone that was meant to avoid the need for steroids. It delayed the cancer on scans but did not help men live longer, and was abandoned.
Query for this target: (TITLE:"CYP17A1" OR ABSTRACT:"CYP17A1" OR TITLE:"17-alpha-hydroxylase/17,20-lyase" OR ABSTRACT:"17-alpha-hydroxylase/17,20-lyase") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about CYP17A1 (17-alpha-hydroxylase/17,20-lyase), not a curated reading list.
Shares Orteronel, Galeterone, ELM-PC 4, ARMOR3-SV.
Shares ELM-PC 4, Abiraterone acetate, Castration-resistant prostate cancer (CRPC), Androgen receptor.
Shares ARMOR3-SV, Castration-resistant prostate cancer (CRPC), Androgen receptor, Metastatic castration-resistant prostate cancer.
Shares Galeterone, ARMOR3-SV, Castration-resistant prostate cancer (CRPC), Androgen receptor.
Shares AR ligand-binding-domain mutation (L702H, W742C, H875Y, T878A, F877L), Abiraterone acetate, Androgen receptor, Metastatic castration-resistant prostate cancer.
Shares ARMOR3-SV, Castration-resistant prostate cancer (CRPC), Androgen receptor, Metastatic castration-resistant prostate cancer.
Shares Abiraterone acetate, Castration-resistant prostate cancer (CRPC), Androgen receptor, Metastatic castration-resistant prostate cancer.
Shares Abiraterone acetate, Castration-resistant prostate cancer (CRPC), Androgen receptor, Metastatic castration-resistant prostate cancer.