Abstract
The androgen receptor (AR) plays a crucial role in the physiological and pathological functions of androgen. As a transcription factor, the AR modulates androgen activity by regulating the transcription of target genes that are involved in numerous physiological functions and pathological disorders, such as acne vulgaris, androgenetic alopecia, benign prostate hyperplasia (BPH), and prostate cancers. Although many natural and synthetic curcumin analogues have been reported to possess anticancer activity through a common cytotoxic property against proliferating tumor cells, none has been reported to inhibit cancer cell growth through a more specific mechanism or target in the cancer cells. Recently, new curcumin analogues were studied extensively regarding their synthesis, structure-activity (i.e., anticancer activity) relationships, and mechanism of action. These compounds, such as ASC-J9 and its analogues (3 and 4), have now been shown to inhibit prostate cancer proliferation through a novel mechanism of enhancing AR degradation.
Keywords: Androgen receptor (AR), Curcumin analogues, Anti-prostate cancer activity, AR degradation
Anti-Cancer Agents in Medicinal Chemistry
Title: Novel Anti-Prostate Cancer Curcumin Analogues That Enhance Androgen Receptor Degradation Activity
Volume: 9 Issue: 8
Author(s): Q. Shi, C. C.-Y. Shih and K. H. Lee
Affiliation:
Keywords: Androgen receptor (AR), Curcumin analogues, Anti-prostate cancer activity, AR degradation
Abstract: The androgen receptor (AR) plays a crucial role in the physiological and pathological functions of androgen. As a transcription factor, the AR modulates androgen activity by regulating the transcription of target genes that are involved in numerous physiological functions and pathological disorders, such as acne vulgaris, androgenetic alopecia, benign prostate hyperplasia (BPH), and prostate cancers. Although many natural and synthetic curcumin analogues have been reported to possess anticancer activity through a common cytotoxic property against proliferating tumor cells, none has been reported to inhibit cancer cell growth through a more specific mechanism or target in the cancer cells. Recently, new curcumin analogues were studied extensively regarding their synthesis, structure-activity (i.e., anticancer activity) relationships, and mechanism of action. These compounds, such as ASC-J9 and its analogues (3 and 4), have now been shown to inhibit prostate cancer proliferation through a novel mechanism of enhancing AR degradation.
Export Options
About this article
Cite this article as:
Shi Q., Shih C.-Y. C. and Lee H. K., Novel Anti-Prostate Cancer Curcumin Analogues That Enhance Androgen Receptor Degradation Activity, Anti-Cancer Agents in Medicinal Chemistry 2009; 9 (8) . https://dx.doi.org/10.2174/187152009789124655
DOI https://dx.doi.org/10.2174/187152009789124655 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...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
-
Small Molecule Toxins Targeting Tumor Receptors
Current Pharmaceutical Design Evaluation of Multifunctional Hybrid Analogs for Stilbenes, Chalcones and Flavanones
Anti-Cancer Agents in Medicinal Chemistry Oligonucleotides and G-quadruplex Stabilizers: Targeting Telomeres and Telomerase in Cancer Therapy
Current Pharmaceutical Design Contemporary Role of Endocrine Treatment in Patients with Localized or Locally Advanced Prostate Cancer: A Review
Current Cancer Therapy Reviews Expression, Distribution and Regulation of Phosphodiesterase 5
Current Pharmaceutical Design The Autism Candidate Gene Neurobeachin Encodes a Scaffolding Protein Implicated in Membrane Trafficking and Signaling
Current Molecular Medicine Multi-Component Reactions of Cyclohexan-1,3-dione: Synthesis of Fused Pyran, Pyridine, Thiophene and Pyrazole Derivatives with c-Met, Anti-Proliferative Activities
Anti-Cancer Agents in Medicinal Chemistry Neuroimmune Aspects of Sjogren`s Syndrome: Role of VIP/VPAC System in Immune and Salivary Gland Epithelial Cell Function
Current Pharmaceutical Design Prediction by Pharmacogenetics of Safety and Efficacy of Non-Steroidal Anti- Inflammatory Drugs: A Review
Current Drug Metabolism The PKB/AKT Pathway in Cancer
Current Pharmaceutical Design Synthesis, Biological Evaluation and Molecular Docking Studies of New Pyrazolines as an Antitubercular and Cytotoxic Agents
Infectious Disorders - Drug Targets Neuroprotective Effects of Quercetin: From Chemistry to Medicine
CNS & Neurological Disorders - Drug Targets Assessment of the Usefulness of the SEMA5A Concentration Profile Changes as a Molecular Marker in Endometrial Cancer
Current Pharmaceutical Biotechnology Regional Distribution and Kinetics of Inhaled Pharmaceuticals
Current Pharmaceutical Design Aging and DNA Methylation
Current Chemical Biology Negative Regulation of NEDD8 Conjugation Pathway by Novel Molecules and Agents for Anticancer Therapy
Current Pharmaceutical Design Quantitative Structure-Activity Relationship Study of Camptothecin Derivatives as Anticancer Drugs Using Molecular Descriptors
Combinatorial Chemistry & High Throughput Screening Glutamine, Glucose and other Fuels for Cancer
Current Pharmaceutical Design The Effect of Psychological Stress and Social Isolation on Neuroimmunoendocrine Communication
Current Pharmaceutical Design Endothelin-1 and Angiogenesis in Cancer
Current Vascular Pharmacology