Abstract
Prostate cancer is the most common carcinoma among aged males in western countries and more aggressive and lethal castration resistant prostate cancer often occurs after androgen deprivation therapy. The high expression of androgens and androgen receptor is closely related to prostate cancer. Efficient androgen receptor antagonists, such as enzalutamide and ARN-509, could be employed as potent anti-prostate cancer agents. Nevertheless, recent studies have revealed that F876L mutation in androgen receptor converts the action of enzalutamide and ARN-509 from an antagonist to agonist, so that novel strategies are urgent to address this resistance mechanism. In this review, we focus on the discussion about some novel strategies, which targets androgen receptor mainly through the degrading pathway as potential treatments for prostate cancer.
Keywords: Resistance mechanism, androgen receptor, degradation, prostate cancer, small molecules, new strategies.
Current Cancer Drug Targets
Title:Degradation of Androgen Receptor through Small Molecules for Prostate Cancer
Volume: 18 Issue: 7
Author(s): Raoling Ge, Xi Xu, Pengfei Xu, Lei Li, Zhiyu Li*Jinlei Bian*
Affiliation:
- Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009,China
- Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009,China
Keywords: Resistance mechanism, androgen receptor, degradation, prostate cancer, small molecules, new strategies.
Abstract: Prostate cancer is the most common carcinoma among aged males in western countries and more aggressive and lethal castration resistant prostate cancer often occurs after androgen deprivation therapy. The high expression of androgens and androgen receptor is closely related to prostate cancer. Efficient androgen receptor antagonists, such as enzalutamide and ARN-509, could be employed as potent anti-prostate cancer agents. Nevertheless, recent studies have revealed that F876L mutation in androgen receptor converts the action of enzalutamide and ARN-509 from an antagonist to agonist, so that novel strategies are urgent to address this resistance mechanism. In this review, we focus on the discussion about some novel strategies, which targets androgen receptor mainly through the degrading pathway as potential treatments for prostate cancer.
Export Options
About this article
Cite this article as:
Ge Raoling , Xu Xi , Xu Pengfei , Li Lei , Li Zhiyu *, Bian Jinlei *, Degradation of Androgen Receptor through Small Molecules for Prostate Cancer, Current Cancer Drug Targets 2018; 18 (7) . https://dx.doi.org/10.2174/1568009617666171107103936
DOI https://dx.doi.org/10.2174/1568009617666171107103936 |
Print ISSN 1568-0096 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5576 |
Call for Papers in Thematic Issues
Advances in Cancer Biomarkers and Potential Drug Targets: From Diagnosis to Therapy
Cancer biomarkers play a crucial role in the diagnosis, prognosis, and treatment of cancer. They provide valuable information for cancer detection, risk assessment, treatment selection, and monitoring response to therapy. With advancements in molecular biology and high-throughput technologies, there has been an increasing interest in identifying and characterizing cancer biomarkers ...read more
Novel Therapeutic Approaches to Target Drug Resistant Tumors
With the development of disciplines such as chemical biology and molecular biology, the genes or proteins closely related to tumor occurrence and development have gradually become clear. Targeted therapies targeting these genes or proteins provide more effective methods for tumor treatment. Tumor targeted drugs generally only act on specific targets ...read more
ROLE OF IMMUNE AND GENOTOXIC RESPONSE BIOMARKERS IN TUMOR MICROENVIRONMENT IN CANCER DIAGNOSIS AND TREATMENT
Biological biomarkers have been used in medical research as an indicator of a normal or abnormal process inside the body, or of a disease. Nowadays, various researchers are in process to explore and investigate the biological markers for the early assessment of cancer. DNA Damage response (DDR) pathways and immune ...read more
Targeting the battlefield between host and tumor: basic research and clinical practice on reshaping tumor immune microenvironment
Immune system protects host against malignant tumors through effector cells and molecules. Cancer development and its response to therapy are regulated by inflammation, which either promotes or suppresses cancer progression. Chronic inflammation facilitates cancer progression and treatment resistance, whereas induction of acute inflammatory reactions often lead to anti-cancer immune responses. ...read more
- 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 Timely Review of State-of-the-Art Chronopharmaceuticals Synchronized with Biological Rhythms
Current Drug Delivery Regulation of EMT by KLF4 in Gastrointestinal Cancer
Current Cancer Drug Targets MicroRNAs in Cancer Stem Cells: New Regulators of Stemness
Current Pharmaceutical Design Relations between GPR4 Expression, Microvascular Density (MVD) and Clinical Pathological Characteristics of Patients with Epithelial Ovarian Carcinoma (EOC)
Current Pharmaceutical Design Essential Oils as Active Ingredients of Lipid Nanocarriers for Chemotherapeutic Use
Current Pharmaceutical Biotechnology Mechanisms of Activation and Key Roles of SGK3 Under Physiological Conditions and in Prostate and Breast Cancer
Current Signal Transduction Therapy MRP1-dependent Collateral Sensitivity of Multidrug-resistant Cancer Cells: Identifying Selective Modulators Inducing Cellular Glutathione Depletion
Current Medicinal Chemistry Advances of AKT Pathway in Human Oncogenesis and as a Target for Anti-Cancer Drug Discovery
Current Cancer Drug Targets Oncolytic Viruses Driven by Tumor-Specific Promoters
Current Cancer Drug Targets Nitric Oxide and Cancer Therapy: The Emperor has NO Clothes
Current Pharmaceutical Design Unlocking the Molecular Mechanisms of DNA Repair and Platinum Drug Resistance in Cancer Chemotherapy
Current Drug Therapy The Long and Winding Road to Cancer Treatment: The Trail System
Current Pharmaceutical Design Tankyrases: Structure, Function and Therapeutic Implications in Cancer
Current Pharmaceutical Design A Survey of Prostate Segmentation Techniques in Different Imaging Modalities
Current Medical Imaging Receptor Tyrosine Kinases as Target for Anti-Cancer Therapy
Current Pharmaceutical Design Neuropilin-1 (NRP-1) and Magnetic Nanoparticles, a Potential Combination for Diagnosis and Therapy of Gliomas
Current Pharmaceutical Design Oncolytic Viruses for Induction of Anti-Tumor Immunity
Current Pharmaceutical Biotechnology Nanotechnology and Antioxidant Therapy: An Emerging Approach for Neurodegenerative Diseases
Current Medicinal Chemistry Do we Need a New Procedure for the Assessment of Adverse Events in Anti-migraine Clinical Trials?
Recent Patents on CNS Drug Discovery (Discontinued) Cancer and Treatment Modalities
Current Cancer Therapy Reviews