CYP11A1 (cholesterol side-chain cleavage enzyme)
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.
Overview
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.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
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.
- 1 · What it is
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.
- 2 · What goes wrong in cancer
A mitochondrial cytochrome P450 of adrenal cortex, gonads and placenta; it requires adrenodoxin and adrenodoxin reductase to receive electrons from NADPH.
- 3 · How drugs use it
No product in this corpus aims at CYP11A1 (cholesterol side-chain cleavage enzyme) yet. Inhibitors are shaped to fit the enzyme's active site so the reaction the cancer relies on stops.
External identifiers
Biology
A mitochondrial cytochrome P450 of adrenal cortex, gonads and placenta; it requires adrenodoxin and adrenodoxin reductase to receive electrons from NADPH.
- Adrenal cortex, ovary, testis and placenta
- Adrenocortical carcinoma and steroid-producing tumours
Latest papers
topQuery 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.
Similar pages
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Shares CYP17A1 (17-alpha-hydroxylase/17,20-lyase), Prostate cancer.
- TreatmentExemestane
Shares Aromatase (CYP19A1), HR-positive / HER2-negative breast cancer.
- TermCastration-resistant prostate cancer (CRPC)
Shares CYP17A1 (17-alpha-hydroxylase/17,20-lyase), Prostate cancer.
- TermmCRPC and mHSPC (castration-resistant vs hormone-sensitive prostate cancer)
Shares CYP17A1 (17-alpha-hydroxylase/17,20-lyase), Prostate cancer.
- TreatmentLetrozole (and other aromatase inhibitors)
Shares Aromatase (CYP19A1), HR-positive / HER2-negative breast cancer.
- TreatmentAbiraterone acetate
Shares CYP17A1 (17-alpha-hydroxylase/17,20-lyase), Prostate cancer.