targetsTarget

CYP17A1 (17-alpha-hydroxylase/17,20-lyase)

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.

CYP17A1 (17-alpha-hydroxylase/17,20-lyase): what it is and how drugs act on it · animated generic schematic, not to scale

Target · the protein and the cell it sits on
Drug · antibody, small molecule, cell or radioligand
Effect · signal, damage or kill

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.

1 · What it is
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.
2 · What goes wrong in cancer
Cytochrome P450 enzyme of the adrenal cortex, testis and prostate cancer cells; the rate-limiting step of androgen synthesis from pregnenolone.
3 · How drugs use it
No product in this corpus aims at CYP17A1 (17-alpha-hydroxylase/17,20-lyase) yet. Inhibitors are shaped to fit the enzyme's active site so the reaction the cancer relies on stops.