5-alpha-reductase type 2 (SRD5A2)
5-alpha-reductase turns testosterone into the more potent dihydrotestosterone inside the prostate; finasteride and dutasteride block it, and two large trials showed they cut prostate cancer diagnoses by about a quarter while raising concern about high-grade tumours.
Overview
Steroid 5-alpha-reductase type 2 converts testosterone to dihydrotestosterone, the androgen that drives prostate growth. Finasteride (type 2 selective) and dutasteride (types 1 and 2) are approved for benign prostatic enlargement and were tested for prevention in the Prostate Cancer Prevention Trial and the REDUCE trial, where they reduced the overall incidence of prostate cancer but were associated with a small excess of high-grade cancers, so neither is approved for prevention. In castration-resistant prostate cancer, tumour cells raise their own 5-alpha-reductase and other steroidogenic enzymes to make androgens, part of the rationale for abiraterone and the newer androgen receptor blockers.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · 5-alpha-reductase turns testosterone into the more potent dihydrotestosterone inside the prostate; finasteride and dutasteride block it, and two large trials showed they cut prostate cancer diagnoses by about a quarter while raising concern about high-grade tumours.
- 1 · What it is
5-alpha-reductase turns testosterone into the more potent dihydrotestosterone inside the prostate; finasteride and dutasteride block it, and two large trials showed they cut prostate cancer diagnoses by about a quarter while raising concern about high-grade tumours.
- 2 · What goes wrong in cancer
A membrane enzyme of the endoplasmic reticulum in prostate, genital skin and hair follicles; it is NADPH-dependent and genetic loss causes a disorder of sex development.
- 3 · How drugs use it
No product in this corpus aims at 5-alpha-reductase type 2 (SRD5A2) yet. Inhibitors are shaped to fit the enzyme's active site so the reaction the cancer relies on stops.
External identifiers
Biology
A membrane enzyme of the endoplasmic reticulum in prostate, genital skin and hair follicles; it is NADPH-dependent and genetic loss causes a disorder of sex development.
- Prostate epithelium and stroma
- Castration-resistant prostate cancer cells making their own androgens
Latest papers
topQuery for this target: (TITLE:"5-alpha-reductase type 2" OR ABSTRACT:"5-alpha-reductase type 2" OR TITLE:"SRD5A2" OR ABSTRACT:"SRD5A2") 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 5-alpha-reductase type 2 (SRD5A2), not a curated reading list.
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