Abstract
Interdependent genetic and epigenetic events control the initiation and progression of tumors. Genetic amplification and overexpression of the GASC1 (gene amplified in squamous cell carcinoma 1) gene has been found in various tumor types and this upregulation correlates with a poor prognosis for cancer patients. Gain- and loss-of –function approaches demonstrate the importance of GASC1 for the maintenance of cancer phenotypes. The GASC1 gene encodes a Jumonji C domain-containing protein, a newly identified histone lysine demethylase, that mainly catalyzes demethylation of tri- and di-methylated forms of histone H3 lysine 9 (H3K9me3/me2) epigenetic repressive marks. Recent studies indicated that over-production of GASC1 may induce alterations in epigenetic histone methylation and affects the expression of key genes that are implicated in carcinogenesis and stem cell properties in human cancer. Furthermore, histone demethylases, such as GASC1, represent highly promising anti-cancer therapeutic targets; a number of GASC1 inhibitors have been identified and reported. This review provides an overview of the current findings on genetic alterations and the biological function of GASC1 in cancer, together with a summary of recent advances in GASC1 inhibitor discovery.
Keywords: Breast cancer, esophageal cancer, GASC1, gene amplification, histone demethylase, histone methylation, therapeutic target.
Current Cancer Therapy Reviews
Title:The Role of Histone Demethylase GASC1 in Cancer and its Therapeutic Potential
Volume: 9 Issue: 1
Author(s): Andreana Holowatyj and Zeng-Quan Yang
Affiliation:
Keywords: Breast cancer, esophageal cancer, GASC1, gene amplification, histone demethylase, histone methylation, therapeutic target.
Abstract: Interdependent genetic and epigenetic events control the initiation and progression of tumors. Genetic amplification and overexpression of the GASC1 (gene amplified in squamous cell carcinoma 1) gene has been found in various tumor types and this upregulation correlates with a poor prognosis for cancer patients. Gain- and loss-of –function approaches demonstrate the importance of GASC1 for the maintenance of cancer phenotypes. The GASC1 gene encodes a Jumonji C domain-containing protein, a newly identified histone lysine demethylase, that mainly catalyzes demethylation of tri- and di-methylated forms of histone H3 lysine 9 (H3K9me3/me2) epigenetic repressive marks. Recent studies indicated that over-production of GASC1 may induce alterations in epigenetic histone methylation and affects the expression of key genes that are implicated in carcinogenesis and stem cell properties in human cancer. Furthermore, histone demethylases, such as GASC1, represent highly promising anti-cancer therapeutic targets; a number of GASC1 inhibitors have been identified and reported. This review provides an overview of the current findings on genetic alterations and the biological function of GASC1 in cancer, together with a summary of recent advances in GASC1 inhibitor discovery.
Export Options
About this article
Cite this article as:
Holowatyj Andreana and Yang Zeng-Quan, The Role of Histone Demethylase GASC1 in Cancer and its Therapeutic Potential, Current Cancer Therapy Reviews 2013; 9 (1) . https://dx.doi.org/10.2174/1573394711309010007
DOI https://dx.doi.org/10.2174/1573394711309010007 |
Print ISSN 1573-3947 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6301 |
Call for Papers in Thematic Issues
Current progress in Protein Degradation and Cancer Therapy
argeted Protein Degradation is gaining momentum in cancer therapy, it facilitate targeting undruggable proteins, it overcome cancer resistance and avoid undesirable side effects. Thus small molecules degraders have emerged as novel therapeutic strategy. Targeted protein degradation (TPD), the process of eliminating a protein of interest hold a great promise for ...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
-
Protective Effects of Corticosteroids and Neurosteroids on Cochlear injury
Medicinal Chemistry Genetic Surgery - A Right Strategy to Attack Cancer
Current Gene Therapy Redox Homeostasis, Bioactive Agents and Transduction Therapy
Current Signal Transduction Therapy Properties of Cell Sources in Tissue-Engineered Three-dimensional Oral Mucosa Model: A Review
Current Stem Cell Research & Therapy Pharmacological Strategies to Overcome HER2 Cross-Talk and Trastuzumab Resistance
Current Medicinal Chemistry A Proteomics Study of the Subacute Toxicity of Rat Brain after Long- Term Exposure of <i>Gelsemium elegans</i>
Current Molecular Pharmacology Biomarkers of Aging with Prognostic and Predictive Value in Non-Oncological Diseases
Current Medicinal Chemistry Exfoliated Epithelial Cells: A Non-Invasive way to Evaluate the Physiological State of Gastrointestinal Epithelium
Recent Patents on Biomedical Engineering (Discontinued) Hypomagnesaemia/Hypokalemia Associated with the Use of Esomeprazole
Current Drug Safety New Pharmacological Approaches Using Polyphenols on the Physiopathology of Neuropathic Pain
Current Drug Targets Mixed Connective Tissue Disease (MCTD) – A Coming of Age
Current Rheumatology Reviews Inhibition of Cyclin-Dependent Kinases - A Review of the Recent Patent Literature
Recent Patents on Anti-Cancer Drug Discovery TRPV1 Function in Health and Disease
Current Pharmaceutical Biotechnology Research Advances in the Treatment of Melanoma by Treat Melanoma
Current Topics in Medicinal Chemistry Challenges and Strategies in Precision Medicine for Non-Small-Cell Lung Cancer
Current Pharmaceutical Design Chemoprotective and Carcinogenic Effects of tert-Butylhydroquinone and Its Metabolites
Current Drug Metabolism Evaluation of Current Pharmacological Treatment Options in the Management of Rett Syndrome: From the Present to Future Therapeutic Alternatives.
Current Clinical Pharmacology Recent Advances in PUVA Photochemotherapy and PDT for the Treatment of Cancer
Current Pharmaceutical Design Topical Use of Sucralfate in Epithelial Wound Healing: Clinical Evidence and Molecular Mechanisms of Action
Recent Patents on Inflammation & Allergy Drug Discovery New Agents to Treat Life-Threatening Fungal Infections
Current Topics in Medicinal Chemistry