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CYP11A1 is the first enzyme in making every steroid hormone from cholesterol; the historic breast cancer drug aminoglutethimide blocked it, cutting oestrogen and adrenal steroids, before aromatase inhibitors made that approach precise.
CYP11A1 converts cholesterol to pregnenolone inside mitochondria, the rate-limiting first step for cortisol, aldosterone, androgens and oestrogens. Aminoglutethimide, introduced for advanced breast cancer and Cushing's syndrome in the 1960s and 1970s, inhibited CYP11A1 and aromatase, producing a medical adrenalectomy that required cortisol replacement; it was displaced by the selective aromatase inhibitors anastrozole, letrozole and exemestane. Blocking steroid synthesis further downstream at CYP17A1 with abiraterone is the modern equivalent in prostate cancer. The enzyme is also a marker of adrenocortical carcinoma.
In plain words · CYP11A1 is the first enzyme in making every steroid hormone from cholesterol; the historic breast cancer drug aminoglutethimide blocked it, cutting oestrogen and adrenal steroids, before aromatase inhibitors made that approach precise.
CYP11A1 is the first enzyme in making every steroid hormone from cholesterol; the historic breast cancer drug aminoglutethimide blocked it, cutting oestrogen and adrenal steroids, before aromatase inhibitors made that approach precise.
A mitochondrial cytochrome P450 of adrenal cortex, gonads and placenta; it requires adrenodoxin and adrenodoxin reductase to receive electrons from NADPH.
1 product aims at CYP11A1 (cholesterol side-chain cleavage enzyme): 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 (Kidney Chromophobe (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 CYP11A1: RNA tissue enriched (adrenal gland 991 nTPM); blood lineage lineage enriched (granulocytes 10 nTPM); high antibody staining in 3 normal tissues. Distribution: 2 cancer families in the corpus carry a prevalence row, label threshold or catalogue link for it (Breast cancer (all types), Prostate cancer); Open Targets associates it with 2 specific cancer types at or above 0.5 (Congenital adrenal insufficiency with 46, XY sex reversal OR 46,XY disorder of sex development-adrenal insufficiency due to CYP11A1 deficiency, adrenal cortex carcinoma). (Rule 7 of scripts/fetch-target-specificity.ts.)
Sources: Human Protein Atlas CYP11A1 tissue; Human Protein Atlas CYP11A1 pathology; Open Targets ENSG00000140459 associations
First described 1986. Earliest sequence paper UniProt cites for the protein: Chung B.-C. et al, Proc. Natl. Acad. Sci. U.S.A, 1986, "Human cholesterol side-chain cleavage enzyme, P450scc: cDNA cloning, assignment of the gene to chromosome 15, and expression in the placenta". Source.
A mitochondrial cytochrome P450 of adrenal cortex, gonads and placenta; it requires adrenodoxin and adrenodoxin reductase to receive electrons from NADPH.
RNA: tissue enriched (adrenal gland 991 nTPM), detected in many normal tissues. Blood: lineage enriched (granulocytes 10 nTPM).
RNA cancer enhanced: Kidney Chromophobe 11 pTPM.
No cancer sample stained medium or high.
HPA CYP11A1 tissue · HPA CYP11A1 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 |
|---|---|---|---|---|
| HR-positive / HER2-negative breast cancer | host% | Host target: first enzyme of steroid synthesis. Not a tumour alteration, so no prevalence applies; the drug acts on normal tissue or on symptoms. |
Approximate, population-level figures; the measure column says what was counted. Ranges show the midpoint as a bar.
Aminoglutethimide produced a medical adrenalectomy for advanced breast and prostate cancer in the 1970s and 1980s, the ancestor of today's aromatase inhibitors, and was withdrawn once selective drugs arrived.
Query for this target: (TITLE:"CYP11A1" OR ABSTRACT:"CYP11A1" OR TITLE:"cholesterol side-chain cleavage enzyme" OR ABSTRACT:"cholesterol side-chain cleavage enzyme") 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 CYP11A1 (cholesterol side-chain cleavage enzyme), not a curated reading list.
Shares Aminoglutethimide, Prostate cancer.
Shares Aromatase (CYP19A1), HR-positive / HER2-negative breast cancer.
Shares CYP17A1 (17-alpha-hydroxylase/17,20-lyase), Prostate cancer.
Shares CYP17A1 (17-alpha-hydroxylase/17,20-lyase), Prostate cancer.
Shares CYP17A1 (17-alpha-hydroxylase/17,20-lyase), Prostate cancer.
Shares CYP17A1 (17-alpha-hydroxylase/17,20-lyase), Prostate cancer.
Shares CYP17A1 (17-alpha-hydroxylase/17,20-lyase), Prostate cancer.
Shares CYP17A1 (17-alpha-hydroxylase/17,20-lyase), Prostate cancer.