Abstract
Histone deacetylase inhibitors (HDACi) are an emerging class of novel anti-cancer drugs that cause growth arrest, differentiation, and apoptosis of tumor cells. In addition, they have shown promise as anti-parasitic, antineurodegenerative, anti-rheumatologic and immunosuppressant agents. To date, several structurally distinct small molecule HDACi have been reported including aryl hydroxamates, benzamides, short-chain fatty acids, electrophilic ketones, and macrocyclic peptides. Macrocyclic HDACi possess the most complex cap-groups which interact with HDAC enzyme's outer rim and have demonstrated excellent HDAC inhibition potency and isoform selectivity. This review focuses on the recent progress and current state of macrocyclic HDACi.
Keywords: Cyclic tetrapeptide, depsipeptide, peptide mimetic, macrolide, ketolide, macrocycles, histone deacetylase inhibitors, HDAC
Current Topics in Medicinal Chemistry
Title: Macrocyclic Histone Deacetylase Inhibitors
Volume: 10 Issue: 14
Author(s): Sandra C. Mwakwari, Vishal Patil, William Guerrant and Adegboyega K. Oyelere
Affiliation:
Keywords: Cyclic tetrapeptide, depsipeptide, peptide mimetic, macrolide, ketolide, macrocycles, histone deacetylase inhibitors, HDAC
Abstract: Histone deacetylase inhibitors (HDACi) are an emerging class of novel anti-cancer drugs that cause growth arrest, differentiation, and apoptosis of tumor cells. In addition, they have shown promise as anti-parasitic, antineurodegenerative, anti-rheumatologic and immunosuppressant agents. To date, several structurally distinct small molecule HDACi have been reported including aryl hydroxamates, benzamides, short-chain fatty acids, electrophilic ketones, and macrocyclic peptides. Macrocyclic HDACi possess the most complex cap-groups which interact with HDAC enzyme's outer rim and have demonstrated excellent HDAC inhibition potency and isoform selectivity. This review focuses on the recent progress and current state of macrocyclic HDACi.
Export Options
About this article
Cite this article as:
C. Mwakwari Sandra, Patil Vishal, Guerrant William and K. Oyelere Adegboyega, Macrocyclic Histone Deacetylase Inhibitors, Current Topics in Medicinal Chemistry 2010; 10 (14) . https://dx.doi.org/10.2174/156802610792232079
DOI https://dx.doi.org/10.2174/156802610792232079 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...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
- Announcements
Related Articles
-
Biochemical, Molecular and Epigenetic Mechanisms of Valproic Acid Neuroprotection
Current Molecular Pharmacology Molecular Mechanisms Underlying Psychological Stress and Cancer
Current Pharmaceutical Design Signal Transduction Pathways and Transcriptional Mechanisms as Targets for Prevention of Emergence of Multidrug Resistance in Human Cancer Cells
Current Drug Targets Recombinant Rhabdoviruses as Potential Vaccines for HIV-1 and Other Diseases
Current HIV Research Confomational Analysis of Soluble Oligomers of GFP Tagged Prion Protein By Fluorescence Fluctuation Spectroscopy
Current Pharmaceutical Biotechnology Endocannabinoid System in Neurological Disorders
Recent Patents on CNS Drug Discovery (Discontinued) Cellular and Molecular Regulation of Inflammatory Pain, Nociception and Hyperalgesia - The Role of the Transcription Factor NF-κB as the Lynchpin Nocisensor: Hyperalgesic or Analgesic Effect?
Current Immunology Reviews (Discontinued) Antioxidant Effects of Chalcones during the Inflammatory Response: An Overall Review
Current Medicinal Chemistry Renaissance of the Biologically Active Vitamin A Derivatives: Established and Novel Directed Therapies for Cancer and Chemoprevention
Current Pharmaceutical Design Potential Role of Natural Compounds as Anti-Angiogenic Agents in Cancer
Current Vascular Pharmacology Anti-Proliferative Activity of Standardized Methanol Extract of Coscinium fenestratum and Its Major Constituent, Berberine, Against Nasopharyngeal Carcinoma Cells
The Natural Products Journal New Insights in Mast Cell Modulation by Palmitoylethanolamide
CNS & Neurological Disorders - Drug Targets Neuroprotective Role of Nanoparticles Against Alzheimer's Disease
Current Drug Metabolism Biophysical Characterization of the Nucleoside Diphosphate Kinase of Leishmania major and Effect of the P95S Mutation
Protein & Peptide Letters Quantitative Proteomics in the Study of Phosphotyrosine-Mediated Signal Transduction Pathway
Current Proteomics Targets of 3-Bromopyruvate, A New, Energy Depleting, Anticancer Agent
Medicinal Chemistry Survival Signaling Pathways Activated by NMDA Receptors
Current Topics in Medicinal Chemistry Image-Guided Nanoparticle-Based siRNA Delivery for Cancer Therapy
Current Pharmaceutical Design Determining the Relative Gene Expression Level of Hypoxia Related Genes in Different Cancer Cell Lines
Current Molecular Pharmacology Potential Impact of Genetic Variants in Nrf2 Regulated Antioxidant Genes and Risk Prediction of Diabetes and Associated Cardiac Complications
Current Medicinal Chemistry