Abstract
Prostate cancer is an age-related disease and a major cause of death in Western countries. A large proportion of prostate cancers have been found to be dependent on androgens for growth and various therapeutic approaches have aimed at either decreasing androgen levels or blocking their action. One method of decreasing androgen levels is through inhibition of enzymes involved in the biosynthetic pathway, for example, the P450 enzyme complex 17α-hydroxylase/C17,20-lyase (P450 ), which catalyses the conversion of pregnenolone and progesterone into the androgen precursors dehydroepiandrosterone and androstenedione respectively. A number of researchers have targeted this enzyme and have produced potent steroidal and non-steroidal inhibitors. This review looks at the various inhibitors that have been developed, focussing mainly on more recent inhibitors reported over the last ten years. Some mention is also given to structural requirements suggested to be important for potent activity.
Keywords: Lyase, prostate cancer, enzyme
Anti-Cancer Agents in Medicinal Chemistry
Title: 17α-Hydroxylase/17,20-Lyase (P450 ) Inhibitors in the Treatment of Prostate Cancer: A Review
Volume: 9 Issue: 6
Author(s): Caroline P. Owen
Affiliation:
Keywords: Lyase, prostate cancer, enzyme
Abstract: Prostate cancer is an age-related disease and a major cause of death in Western countries. A large proportion of prostate cancers have been found to be dependent on androgens for growth and various therapeutic approaches have aimed at either decreasing androgen levels or blocking their action. One method of decreasing androgen levels is through inhibition of enzymes involved in the biosynthetic pathway, for example, the P450 enzyme complex 17α-hydroxylase/C17,20-lyase (P450 ), which catalyses the conversion of pregnenolone and progesterone into the androgen precursors dehydroepiandrosterone and androstenedione respectively. A number of researchers have targeted this enzyme and have produced potent steroidal and non-steroidal inhibitors. This review looks at the various inhibitors that have been developed, focussing mainly on more recent inhibitors reported over the last ten years. Some mention is also given to structural requirements suggested to be important for potent activity.
Export Options
About this article
Cite this article as:
Owen P. Caroline, 17α-Hydroxylase/17,20-Lyase (P450 ) Inhibitors in the Treatment of Prostate Cancer: A Review, Anti-Cancer Agents in Medicinal Chemistry 2009; 9 (6) . https://dx.doi.org/10.2174/187152009788680046
DOI https://dx.doi.org/10.2174/187152009788680046 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
A Systematic Review and Meta-Analysis about the Effect of Bisphosphonates on the Risk of Skeletal-Related Event in Men with Prostate Cancer
Anti-Cancer Agents in Medicinal Chemistry Inhibition of Anti-Apoptotic Bcl-2 Family Proteins by Natural Polyphenols New Avenues for Cancer Chemoprevention and Chemotherapy
Current Pharmaceutical Design Mitochondria and Familial Predisposition to Breast Cancer
Current Genomics Protein Kinases and their Modulation in the Central Nervous System
Current Medicinal Chemistry - Central Nervous System Agents Synthetic and Medicinal Prospective of Structurally Modified Curcumins
Current Topics in Medicinal Chemistry Inhibitors of the Ubiquitin-Proteasome System and the Cell Death Machinery: How Many Pathways are Activated?
Current Molecular Pharmacology 7-O-aminoalkyl-2,3-dehydrosilibinins: Synthesis and in vitro Anti-cancer Efficacy
Anti-Cancer Agents in Medicinal Chemistry IGF-I Abuse in Sport
Current Drug Abuse Reviews Gold Nanostructure: Fabrication, Surface Modification, Targeting Imaging, and Enhanced Radiotherapy
Current Nanoscience Resveratrol Promotes HIV-1 Tat Accumulation <i>via</i> AKT/FOXO1 Signaling Axis and Potentiates Vorinostat to Antagonize HIV-1 Latency
Current HIV Research Update on Cancer Related Issues of Mesenchymal Stem Cell-Based Therapies
Current Stem Cell Research & Therapy Antithrombin, an Important Inhibitor in Blood Clots
Current Topics in Medicinal Chemistry Cancer Therapy: Targeting Cell Cycle Regulators
Anti-Cancer Agents in Medicinal Chemistry The Redox Regulation of Thiol Dependent Signaling Pathways in Cancer
Current Pharmaceutical Design Roles of EGFR, PI3K, AKT, and mTOR in Heavy Metal-Induced Cancer
Current Cancer Drug Targets Potassium Channels: Novel Emerging Biomarkers and Targets for Therapy in Cancer
Recent Patents on Anti-Cancer Drug Discovery Immunomodulatory Activities of Glucocorticoids: Insights from Transgenesis and Gene Targeting
Current Pharmaceutical Design Insights in microRNAs Biology
Current Topics in Medicinal Chemistry Cytotoxic Effect of the Red Beetroot (Beta vulgaris L.) Extract Compared to Doxorubicin (Adriamycin) in the Human Prostate (PC-3) and Breast (MCF-7) Cancer Cell Lines
Anti-Cancer Agents in Medicinal Chemistry Targeting RhoA/Rho Kinase and p21-Activated Kinase Signaling to Prevent Cancer Development and Progression
Recent Patents on Anti-Cancer Drug Discovery