CYP17A1
CYP17A1 is a cytochrome P450 enzyme that drives steroidogenesis by catalyzing 17α-hydroxylation and 17,20-lyase reactions required for androgen precursor formation[1]. Mechanistically, this dual activity connects pregnenolone and progesterone metabolism with androgen biosynthesis, making CYP17A1 central to steroid hormone research[1][2]. In disease models, CYP17A1 supports androgen production relevant to castration-resistant prostate cancer, where abiraterone suppresses tumor growth by inhibiting this steroidogenic enzyme[3]. Compared with teleost Cyp17a2, which shows only 17α-hydroxylase activity, Cyp17a1 retains both 17α-hydroxylase and 17,20-lyase activities, supporting isoform-specific experimental design[4]. For inhibitor research, abiraterone and TOK-001 structures reveal active-site binding features useful for CYP17A1 drug-design studies, while non-steroidal CYP17A1 inhibitors support selectivity-focused medicinal chemistry[5][6].
References:
- [1]. Guengerich FP, et al. Steroid 17α-hydroxylase/17, 20-lyase (cytochrome P450 17A1). Methods Enzymol. 2023;689:39-63. [Content Brief]
- [2]. Petrunak EM, et al. Human cytochrome P450 17A1 structures with metabolites of prostate cancer drug abiraterone reveal substrate-binding plasticity and a second binding site. J Biol Chem. 2023 Mar;299(3):102999. [Content Brief]
- [3]. Mostaghel EA, et al. Resistance to CYP17A1 inhibition with abiraterone in castration-resistant prostate cancer: induction of steroidogenesis and androgen receptor splice variants. Clin Cancer Res. 2011 Sep 15;17(18):5913-25. [Content Brief]
- [4]. Shi S, et al. Characterization of the Interrenal Gland and Sexual Traits Development in cyp17a2-Deficient Zebrafish. Front Endocrinol (Lausanne). 2022 Jun 6;13:910639. [Content Brief]
- [5]. DeVore NM, et al. Structures of cytochrome P450 17A1 with prostate cancer drugs abiraterone and TOK-001. Nature. 2012 Jan 22;482(7383):116-9. [Content Brief]
- [6]. Bonomo S, et al. Promising Tools in Prostate Cancer Research: Selective Non-Steroidal Cytochrome P450 17A1 Inhibitors. Sci Rep. 2016 Jul 12;6:29468. [Content Brief]
All Product Categories
-
CYP17A1 Related Products (5)
Related Products (5)
-
4-Pyridylmethyl adamantanecarboxamide
0 Images4-Pyridylmethyl adamantanecarboxamide (Compound 11) is an Aromatase inhibitor with an IC50 of 1.5 μM against hAromatase. 4-Pyridylmethyl adamantanecarboxamide inhibits the C17,20-lyase activity of testicular cytochrome P45017α with an IC50 of 1600 nM, and also inhibits the 17α-hydroxylase activity of this enzyme with an IC50 of 7700 nM. 4-Pyridylmethyl adamantanecarboxamide can be used in the research of prostate cancer.
-
CYP17A1/HDAC6-IN-1
0 ImagesCat. No.: HY-163359CAS No.: 3047489-22-2CYP17A1/HDAC6-IN-1 (compound 12) is a potent inhibitor of CYP17A1/HDAC6, with IC50 of 0.284μM and 0.6015 μM,respectively. CYP17A1/HDAC6-IN-1 has anti-tumor activity.
-
YXG-158
0 ImagesCat. No.: HY-155666CAS No.: 2952994-34-0YXG‑158 is an orally active, anticancer bifunctional steroid analog with both androgen receptor (AR) degradation activity (DC50 = 1.28 μM) and CYP17A1 inhibitory activity (IC50 = 100 nM). YXG-158 reduces AR protein and mRNA expression via proteasome-dependent degradation, degrades AR-V7, and inhibits CYP17A1 enzymatic activity to block androgen biosynthesis. YXG-158 inhibits the activities of ERα and ERβ, as well as cancer cell proliferation. YXG-158 decreases the weight of androgen-sensitive organs in castrated rats treated with testosterone propionate, downregulates AR protein, reduces PSA levels, and suppresses tumor growth in Enzalutamide (HY-70002)-sensitive and -resistant xenograft models. YXG-158 can be used in prostate cancer-related research.
-
ASN-001
0 ImagesCat. No.: HY-164457CAS No.: 1429329-63-4ASN-001 is an orally active CYP-17A1 lyase inhibitor that selectively inhibits testosterone synthesis. ASN-001 has anticancer activity and can be used for research in the field of prostate cancer.
-
CYP17A1-IN-2
0 ImagesCat. No.: HY-181045CYP17A1-IN-2 is a potent inhibitor of CYP17A1. CYP17A1-IN-2 exhibits anti-proliferative activity against prostate cancer cells. CYP17A1-IN-2 can be used in research related to castration-resistant prostate cancer.
