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Non-steroidal CYP17A1 Inhibitors: Discovery and Assessment.

ABSTRACT: CYP17A1 is an enzyme that plays a major role in steroidogenesis and is critically involved in the biosynthesis of steroid hormones. Therefore, it remains an attractive target in several serious hormone-dependent cancer diseases, such as prostate cancer and breast cancer. The medicinal chemistry community has been committed to the discovery and development of CYP17A1 inhibitors for many years, particularly for the treatment of castration-resistant prostate cancer. The current Perspective reflects upon the discovery and evaluation of non-steroidal CYP17A1 inhibitors from a medicinal chemistry angle. Emphasis is placed on the structural aspects of the target, key learnings from the presented chemotypes, and design guidelines for future inhibitors.

SUBMITTER: Wrobel TM

PROVIDER: S-EPMC10226049 | biostudies-literature | 2023 May

REPOSITORIES: biostudies-literature

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Non-steroidal CYP17A1 Inhibitors: Discovery and Assessment.

Wróbel Tomasz M TM Jørgensen Flemming Steen FS Pandey Amit V AV Grudzińska Angelika A Sharma Katyayani K Yakubu Jibira J Björkling Fredrik F

Journal of medicinal chemistry 20230516 10

CYP17A1 is an enzyme that plays a major role in steroidogenesis and is critically involved in the biosynthesis of steroid hormones. Therefore, it remains an attractive target in several serious hormone-dependent cancer diseases, such as prostate cancer and breast cancer. The medicinal chemistry community has been committed to the discovery and development of CYP17A1 inhibitors for many years, particularly for the treatment of castration-resistant prostate cancer. The current Perspective reflects ...[more]

PMID: 37191389

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