Abstract
Chromatin-regulating proteins modulate nucleosome structure by either modifying histones covalently or disrupting DNA-protein interaction directly with ATP hydrolysis. Evidence has shown that chromatin-regulating proteins play critical roles in regulation of molecular processes using DNA as template, including gene expression, DNA replication, DNA damage repair, and chromosome integrity. In most of human malignancies, chromatin-regulating proteins have been shown as functional oncogenes. In some scenarios, chromatin-regulating proteins also could have tumor suppressive functions. Thereby, small molecular inhibitors targeting chromatin-regulating proteins could be used for cancer therapies. Numerous small molecular inhibitors against chromatin-regulating proteins are recently developed by academic and industrial groups. These compounds are evaluated for antitumor effects in vitro and in vivo. Some of them have shown great potential to become a therapeutic drug for cancer, and is currently evaluated in clinical trials. A few compounds have been approved for clinical use in cancer treatment. In this review, we will focus on the recent progress on the development of small inhibitors of chromatin-regulating proteins for cancer therapy.
Keywords: Chromatin regulator, chromatin regulating protein, inhibitor, cancer, therapy.
Current Protein & Peptide Science
Title:Small Molecular Inhibitors Targeting Chromatin Regulating Proteins for Cancer
Volume: 17 Issue: 5
Author(s): Jie Luan, Zhiyong Chu, Joya Chandra and Pingyu Zhang
Affiliation:
Keywords: Chromatin regulator, chromatin regulating protein, inhibitor, cancer, therapy.
Abstract: Chromatin-regulating proteins modulate nucleosome structure by either modifying histones covalently or disrupting DNA-protein interaction directly with ATP hydrolysis. Evidence has shown that chromatin-regulating proteins play critical roles in regulation of molecular processes using DNA as template, including gene expression, DNA replication, DNA damage repair, and chromosome integrity. In most of human malignancies, chromatin-regulating proteins have been shown as functional oncogenes. In some scenarios, chromatin-regulating proteins also could have tumor suppressive functions. Thereby, small molecular inhibitors targeting chromatin-regulating proteins could be used for cancer therapies. Numerous small molecular inhibitors against chromatin-regulating proteins are recently developed by academic and industrial groups. These compounds are evaluated for antitumor effects in vitro and in vivo. Some of them have shown great potential to become a therapeutic drug for cancer, and is currently evaluated in clinical trials. A few compounds have been approved for clinical use in cancer treatment. In this review, we will focus on the recent progress on the development of small inhibitors of chromatin-regulating proteins for cancer therapy.
Export Options
About this article
Cite this article as:
Luan Jie, Chu Zhiyong, Chandra Joya and Zhang Pingyu, Small Molecular Inhibitors Targeting Chromatin Regulating Proteins for Cancer, Current Protein & Peptide Science 2016; 17 (5) . https://dx.doi.org/10.2174/1389203717666160122121340
DOI https://dx.doi.org/10.2174/1389203717666160122121340 |
Print ISSN 1389-2037 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5550 |
Call for Papers in Thematic Issues
Advancements in Proteomic and Peptidomic Approaches in Cancer Immunotherapy: Unveiling the Immune Microenvironment
The scope of this thematic issue centers on the integration of proteomic and peptidomic technologies into the field of cancer immunotherapy, with a particular emphasis on exploring the tumor immune microenvironment. This issue aims to gather contributions that illustrate the application of these advanced methodologies in unveiling the complex interplay ...read more
Nutrition and Metabolism in Musculoskeletal Diseases
The musculoskeletal system consists mainly of cartilage, bone, muscles, tendons, connective tissue and ligaments. Balanced metabolism is of vital importance for the homeostasis of the musculoskeletal system. A series of musculoskeletal diseases (for example, sarcopenia, osteoporosis) are resulted from the dysregulated metabolism of the musculoskeletal system. Furthermore, metabolic diseases (such ...read more
Protein Folding, Aggregation and Liquid-Liquid Phase Separation
Protein folding, misfolding and aggregation remain one of the main problems of interdisciplinary science not only because many questions are still open, but also because they are important from the point of view of practical application. Protein aggregation and formation of fibrillar structures, for example, is a hallmark of a ...read more
Related Journals
- 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
-
Prostaglandin E<sub>2</sub> Receptor 4 (EP4): A Promising Therapeutic Target for the Treatment of Cancer and Inflammatory Diseases
Current Chemical Biology RING-, HECT-, and RBR-type E3 Ubiquitin Ligases: Involvement in Human Cancer
Current Cancer Drug Targets New Molecular Targets of Anticancer Therapy – Current Status and Perspectives
Current Medicinal Chemistry <i>Uncaria tomentosa</i> (Willd. ex Schult.): Focus on Nutraceutical Aspects
Current Bioactive Compounds Sphingolipid Signaling and Hematopoietic Malignancies: To the Rheostat and Beyond
Anti-Cancer Agents in Medicinal Chemistry The Role of Angiogenesis as a Prognostic Factor of Breast Cancer: Recent Review
Current Women`s Health Reviews Choline Kinase Alpha Depletion Selectively Kills Tumoral Cells
Current Cancer Drug Targets Overview of Angiogenesis and the use of Bevacizumab in Patients with Malignant Gliomas
Current Signal Transduction Therapy Nitrogen-Containing Heterocycles as Anticancer Agents: An Overview
Anti-Cancer Agents in Medicinal Chemistry Aqueous Extracts of Selected Potentilla Species Modulate Biological Activity of Human Normal Colon Cells
Current Drug Targets A Review of Natural and Modified Betulinic, Ursolic and Echinocystic Acid Derivatives as Potential Antitumor and Anti-HIV Agents
Mini-Reviews in Medicinal Chemistry Trans-Platinum Complexes as Anticancer Drugs: Recent Developments and Future Prospects
Current Medicinal Chemistry Oncolytic HSV-1 Virotherapy: Clinical Experience and Opportunities for Progress
Current Pharmaceutical Biotechnology Radiopharmaceuticals Labelled with Copper Radionuclides: Clinical Results in Human Beings
Current Radiopharmaceuticals Hollow Inorganic Nanoparticles as Efficient Carriers for siRNA Delivery: A Comprehensive Review
Current Pharmaceutical Design Assessment of the Health Effects of Chemicals in Humans: II. Construction of an Adverse Effects Database for QSAR Modeling
Current Drug Discovery Technologies Microarrays and Colon Cancer in the Road for Translational Medicine
Current Bioinformatics Angiogenesis: A Target for Cancer Therapy
Current Pharmaceutical Design Treatment Related Morbidity in Cervical Cancer
Current Women`s Health Reviews Fc-fusion Proteins in Therapy: An Updated View
Current Medicinal Chemistry