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Updated: Jul 5, 2026

A Bioluminescent and Fluorescent Orthotopic Syngeneic Murine Model of Androgen-dependent and Castration-resistant Prostate Cancer
Published on: March 6, 2018
CYP17 inhibitors for prostate cancer treatment--an update
V M Moreira1, J A R Salvador, T S Vasaitis
1Laboratório de Química Farmacêutica, Faculdade de Farmácia, Universidade de Coimbra, Rua do Norte, 3000-295 Coimbra, Portugal.
Abstract:
It is almost 70 years since the discovery by Huggins et al. that androgens are essential for prostate cancer (PC) growth and progression, and there has been about 30 years experience using ketoconazole for PC therapy. Since then we have come a long way in learning about the disease and developing new strategies to approach it, among which is cytochrome 17alpha-hydroxylase-C(17,20)-lyase (CYP17) inhibition. This review focuses on the efforts to find prospective CYP17 inhibitors, both steroidal and nonsteroidal, in the absence of a 3D structure of the enzyme. It covers almost 4 decades of literature with highlights on the most significant achievements in this area, providing insight into PC pathophysiology, management and treatment options.
Insights
This review explores cytochrome 17alpha-hydroxylase-C(17,20)-lyase (CYP17) inhibitors for prostate cancer (PC) treatment. It highlights advancements in developing steroidal and nonsteroidal inhibitors to target PC progression.
Area of Science:
- Oncology
- Medicinal Chemistry
- Biochemistry
Background:
- Androgens are crucial for prostate cancer (PC) growth, a fact known for nearly 70 years.
- Ketoconazole has been used for PC therapy for approximately 30 years.
- Cytochrome 17alpha-hydroxylase-C(17,20)-lyase (CYP17) inhibition is a key strategy in PC management.
Purpose of the Study:
- To review the development of CYP17 inhibitors for prostate cancer treatment.
- To explore both steroidal and nonsteroidal inhibitor candidates.
- To provide insight into PC pathophysiology and treatment strategies.
Main Methods:
- Literature review spanning nearly four decades.
- Focus on identifying prospective CYP17 inhibitors.
- Analysis of achievements in the absence of a 3D enzyme structure.
Main Results:
- Significant progress has been made in identifying potential CYP17 inhibitors.
- Development of both steroidal and nonsteroidal compounds targeting CYP17.
- Understanding of PC pathophysiology has advanced.
Conclusions:
- CYP17 inhibition represents a promising therapeutic avenue for prostate cancer.
- Continued research into novel CYP17 inhibitors is essential for improving PC management.
- This review offers insights into PC treatment options and future directions.
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