Abstract
Prostate cancer is the most frequently diagnosed tumor in industrialized countries. Endocrine therapy, which is based on interference with androgen signaling is only palliative. Drugs used in prostate cancer therapy are luteinizing hormone releasing hormone (LHRH) agonists and antiandrogens. Application of LHRH agonists leads to suppression of the levels of circulating androgens, and antiandrogens block the function of the androgen receptor (AR). The steroidal antiandrogen cyproterone acetate and nonsteroidal compounds hydroxyflutamide and bicalutamide are used most frequently. They prevent acquisition of a transcriptionally active conformation of the AR. It became clear that tumors progress to therapy resistance in the presence of the AR which might be structurally altered. These mutations generate receptors that respond to other steroids and antiandrogens by increased activation. In addition, AR expression increases during endocrine treatment. AR is also activated by nonsteroidal compounds such as growth factors, interleukin-6, and neuropeptides. Therefore, new experimental approaches are needed to antagonize AR expression and function more efficiently. The AR associates with a number of proteins, coactivators and corepressors. There are indications that expression of some of these proteins is altered in prostate cancer, a fact which might be important for improvement of endocrine therapy.
Keywords: Antiandrogens, luteinizing hormone releasing hormone (LHRH), nonsteroidal, corepressors, proteins
Current Cancer Drug Targets
Title: Antiandrogens in Prostate Cancer Endocrine Therapy
Volume: 4 Issue: 5
Author(s): Z. Culig, G. Bartsch and A. Bartsch
Affiliation:
Keywords: Antiandrogens, luteinizing hormone releasing hormone (LHRH), nonsteroidal, corepressors, proteins
Abstract: Prostate cancer is the most frequently diagnosed tumor in industrialized countries. Endocrine therapy, which is based on interference with androgen signaling is only palliative. Drugs used in prostate cancer therapy are luteinizing hormone releasing hormone (LHRH) agonists and antiandrogens. Application of LHRH agonists leads to suppression of the levels of circulating androgens, and antiandrogens block the function of the androgen receptor (AR). The steroidal antiandrogen cyproterone acetate and nonsteroidal compounds hydroxyflutamide and bicalutamide are used most frequently. They prevent acquisition of a transcriptionally active conformation of the AR. It became clear that tumors progress to therapy resistance in the presence of the AR which might be structurally altered. These mutations generate receptors that respond to other steroids and antiandrogens by increased activation. In addition, AR expression increases during endocrine treatment. AR is also activated by nonsteroidal compounds such as growth factors, interleukin-6, and neuropeptides. Therefore, new experimental approaches are needed to antagonize AR expression and function more efficiently. The AR associates with a number of proteins, coactivators and corepressors. There are indications that expression of some of these proteins is altered in prostate cancer, a fact which might be important for improvement of endocrine therapy.
Export Options
About this article
Cite this article as:
Culig Z., Bartsch G. and Bartsch A., Antiandrogens in Prostate Cancer Endocrine Therapy, Current Cancer Drug Targets 2004; 4 (5) . https://dx.doi.org/10.2174/1568009043332925
DOI https://dx.doi.org/10.2174/1568009043332925 |
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
-
Microenvironmental Determinants of Adult Neural Stem Cell Proliferation and Lineage Commitment in the Healthy and Injured Central Nervous System
Current Stem Cell Research & Therapy Inhibition of Angiogenesis by Non-Steroidal Anti-Inflammatory Drugs: From the Bench to the Bedside and Back
Current Drug Targets - Inflammation & Allergy Applications of Artificial Neural Networks in Medical Science
Current Clinical Pharmacology Inhibitors of the Hedgehog Signal Transduction Pathway
Current Cancer Therapy Reviews Applications of Molecular Imaging in Cancer Gene Therapy
Current Gene Therapy Phytochemicals Resveratrol and Sulforaphane as Potential Agents for Enhancing the Anti-Tumor Activities of Conventional Cancer Therapies
Current Pharmaceutical Biotechnology Design, Synthesis and Evaluation of Quinoline-based Small Molecule Inhibitor of STAT3
Letters in Drug Design & Discovery Molecular Phenotype of CXCL12β 3UTR G801A Polymorphism (rs1801157) Associated to HIV-1 Disease Progression
Current HIV Research Immunotherapy for Conformational Diseases
Current Pharmaceutical Design The Potential Role of Claudins in Regulation of Metastasis and Development of Drug Resistance in Breast Cancer
Clinical Cancer Drugs Evaluation of Non-Coding RNAs as Potential Targets in Head and Neck Squamous Cell Carcinoma Cancer Stem Cells
Current Drug Targets The Role of Adenosine in Bone: An Emerging Concept
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Lysophosphatidic Acid and Renal Fibrosis
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery On the Involvement of H2S in Nitroso Signaling and Other Mechanisms of H2S Action
Current Pharmaceutical Biotechnology Prognostic and Predictive Markers in Colorectal Cancer – The Role of New Genomic Technologies
Current Pharmacogenomics The Leptin System: A Potential Target for Sepsis Induced Immune Suppression
Endocrine, Metabolic & Immune Disorders - Drug Targets Curcumin and its Multi-target Function Against Pain and Inflammation: An Update of Pre-clinical Data
Current Drug Targets Comprehensive Quality Management (CQM) in the PLCO Trial
Reviews on Recent Clinical Trials Patent Perspective for Potential Antioxidant Compounds-Rutin and Quercetin
Recent Patents on Nanomedicine Small Heat Shock Proteins and the Endoplasmic Reticulum: Potential Attractive Therapeutic Targets?
Current Molecular Medicine