Abstract
The role of sirtuins in age-related diseases is an area of rapidly expanding investigation. Sirtuins are NAD+ -dependent class III histone deacetylases (HDACs) that share extensive homologies with the yeast HDAC Sir2. Class I and class II HDACs inhibitors have been identified as potential anticancer agents and are in clinical studies, but much less is known about class III HDAC inhibitors. However, inhibitors of sirtuins are currently being targeted as potential therapeutic agents for disease such as cancer, neurodegenerative disease and other disorders as sirtuins are discovered to regulate numerous downstream enzymes. Given the link between sirtuins and cancer, understanding the functionality of these enzymes may ultimately have significant impact in cancer prevention or cancer treatment. This review gives an updated overview regarding the regulation of sirtuin enzymes, their implications in cancer, various sirtuin inhibitor scaffolds and their insights in drug design.
Keywords: Histone deacetylases, sirtuin, inhibitor, epigenetic, cancer.
Anti-Cancer Agents in Medicinal Chemistry
Title:Sirtuin Inhibitors: An Overview from Medicinal Chemistry Perspective
Volume: 16 Issue: 8
Author(s): Yeong Keng Yoon and Chern Ein Oon
Affiliation:
Keywords: Histone deacetylases, sirtuin, inhibitor, epigenetic, cancer.
Abstract: The role of sirtuins in age-related diseases is an area of rapidly expanding investigation. Sirtuins are NAD+ -dependent class III histone deacetylases (HDACs) that share extensive homologies with the yeast HDAC Sir2. Class I and class II HDACs inhibitors have been identified as potential anticancer agents and are in clinical studies, but much less is known about class III HDAC inhibitors. However, inhibitors of sirtuins are currently being targeted as potential therapeutic agents for disease such as cancer, neurodegenerative disease and other disorders as sirtuins are discovered to regulate numerous downstream enzymes. Given the link between sirtuins and cancer, understanding the functionality of these enzymes may ultimately have significant impact in cancer prevention or cancer treatment. This review gives an updated overview regarding the regulation of sirtuin enzymes, their implications in cancer, various sirtuin inhibitor scaffolds and their insights in drug design.
Export Options
About this article
Cite this article as:
Yoon Keng Yeong and Oon Ein Chern, Sirtuin Inhibitors: An Overview from Medicinal Chemistry Perspective, Anti-Cancer Agents in Medicinal Chemistry 2016; 16 (8) . https://dx.doi.org/10.2174/1871520616666160310141622
DOI https://dx.doi.org/10.2174/1871520616666160310141622 |
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
-
Peripartum Cardiomyopathy: Current State of Knowledge, New Developments and Future Directions
Current Cardiology Reviews Stem Cell Therapy for the Treatment of Myocardial Infarction
Current Pharmaceutical Design Natural Products to Anti-trypanosomal Drugs: An Overview of New Drug Prototypes for American Trypanosomiasis
Cardiovascular & Hematological Agents in Medicinal Chemistry Mechanisms of Corticosteroid Resistance in Severe Asthma and Chronic Obstructive Pulmonary Disease (COPD)
Current Pharmaceutical Design p53 Regulation of Energy Metabolism and Mitochondria Regulation of p53 in Cancer Cells: An Insight into the Role of Manganese Superoxide Dismutase
Current Pharmaceutical Biotechnology The Importance of Lost Minerals in Heart Failure
Cardiovascular & Hematological Agents in Medicinal Chemistry RNA Splicing Manipulation: Strategies to Modify Gene Expression for a Variety of Therapeutic Outcomes
Current Gene Therapy Anticancer Drug Combinations, How Far We can Go Through?
Anti-Cancer Agents in Medicinal Chemistry MicroRNAs in Cardiovascular Therapeutics
Current Topics in Medicinal Chemistry Re-Discovering PDE3 Inhibitors - New Opportunities for a Long Neglected Target
Current Topics in Medicinal Chemistry Adenosine Receptors: What We Know and What We are Learning
Current Topics in Medicinal Chemistry Angiotensin-Converting Enzyme Inhibitors: Mechanisms of Action and Implications In Anesthesia Practice
Current Pharmaceutical Design Antioxidant Therapy Against Trypanosome Infections: A Review Update
Current Topics in Medicinal Chemistry Therapeutic Application of Endothelial Progenitor Cells for Treatment of Cardiovascular Diseases
Current Stem Cell Research & Therapy Efficacy and Complications of Subcutaneous <i>versus</i> Conventional Cardioverter Defibrillators: A Systematic Review and Meta-analysis
Current Cardiology Reviews What Does a Pediatrician Need to Know About Chronic Diarrhea?
Current Pediatric Reviews Humoral Immunity in Heart Failure
Cardiovascular & Hematological Disorders-Drug Targets Parathyroid Hormone and Heart Failure: Novel Biomarker Strategy
Endocrine, Metabolic & Immune Disorders - Drug Targets Selective Pharmacological Inhibition of the Pacemaker Channel Isoforms (HCN1-4) as New Possible Therapeutical Targets
Current Medicinal Chemistry Deep Inspiration Breath-hold (DIBH) Technique to Reduce Cardiac Radiation Dose in the Management of Breast Cancer
Current Cancer Therapy Reviews