Abstract
Histone deacetylases (HDACs) play a significant role in the proliferation and dissemination of cancer and represent promising epigenetic drug targets. The HDAC inhibitor vorinostat featuring a zinc-binding hydroxamate fragment was already clinically approved. However, HDAC inhibitors containing hydroxamic acids are often hampered by acquired or intrinsic drug resistance and may lead to enhanced tumor aggressiveness. In order to overcome these drawbacks of hydroxamate HDAC inhibitors, a series of multimodal derivatives of this compound class, including such with different zinc-binding groups, was recently developed and showed promising anticancer activity. This review provides an overview of the chemistry and pleiotropic anticancer modes of action of these conceptually new HDAC inhibitors.
Keywords: Anticancer drugs, epigenetics, histone deacetylases, kinases, DNA targeting, HDAC inhibitors, hybrid molecules.
Current Cancer Drug Targets
Title:Multimodal HDAC Inhibitors with Improved Anticancer Activity
Volume: 18 Issue: 1
Author(s): Rainer Schobert and Bernhard Biersack*
Affiliation:
- Organic Chemistry Laboratory, Faculty of Biology, Chemistry and Earth Sciences, University of Bayreuth, Universitatsstrasse 30, 95440 Bayreuth,Germany
Keywords: Anticancer drugs, epigenetics, histone deacetylases, kinases, DNA targeting, HDAC inhibitors, hybrid molecules.
Abstract: Histone deacetylases (HDACs) play a significant role in the proliferation and dissemination of cancer and represent promising epigenetic drug targets. The HDAC inhibitor vorinostat featuring a zinc-binding hydroxamate fragment was already clinically approved. However, HDAC inhibitors containing hydroxamic acids are often hampered by acquired or intrinsic drug resistance and may lead to enhanced tumor aggressiveness. In order to overcome these drawbacks of hydroxamate HDAC inhibitors, a series of multimodal derivatives of this compound class, including such with different zinc-binding groups, was recently developed and showed promising anticancer activity. This review provides an overview of the chemistry and pleiotropic anticancer modes of action of these conceptually new HDAC inhibitors.
Export Options
About this article
Cite this article as:
Schobert Rainer and Biersack Bernhard*, Multimodal HDAC Inhibitors with Improved Anticancer Activity, Current Cancer Drug Targets 2018; 18 (1) . https://dx.doi.org/10.2174/1568009617666170206102613
DOI https://dx.doi.org/10.2174/1568009617666170206102613 |
Print ISSN 1568-0096 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5576 |
Call for Papers in Thematic Issues
Innovative Cancer Drug Targets: A New Horizon in Oncology
Cancer remains one of the most challenging diseases, with its complexity and adaptability necessitating continuous research efforts into more effective and targeted therapeutic approaches. Recent years have witnessed significant progress in understanding the molecular and genetic basis of cancer, leading to the identification of novel drug targets. These include, but ...read more
Role of Immune and Genotoxic Response Biomarkers in Tumor Microenvironment in Cancer Diagnosis and Treatment
Biological biomarkers have been used in medical research as an indicator of a normal or abnormal process inside the body, or of a disease. Nowadays, various researchers are in process of exploring and investigating the biological markers for the early assessment of cancer. DNA Damage response (DDR) pathways and immune ...read more
Unraveling the Tumor Microenvironment and Potential Therapeutic Targets: Insights from Single-Cell Sequencing and Spatial Transcriptomics
This special issue will focus on unraveling the complexities of the tumor microenvironment (TME) and identifying key biomarkers for potential therapeutic targets using advanced multi-omics techniques, such as single-cell sequencing and spatial transcriptomics. We seek original research and comprehensive reviews that investigate the heterogeneity and dynamics of the TME, emphasizing ...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
-
Epigenetic Aberrations and Targeted Epigenetic Therapy of Esophageal Cancer
Current Cancer Drug Targets Role of the Receptor Tyrosine Kinase Axl and its Targeting in Cancer Cells
Current Medicinal Chemistry Safety of Nanoparticles in Medicine
Current Drug Targets Novel Antibody Therapeutics Targeting Mesothelin In Solid Tumors
Clinical Cancer Drugs Metal Complexes, their Cellular Targets and Potential for Cancer Therapy
Current Pharmaceutical Design Epigenetic Regulation of Gene Expression as an Anticancer Drug Target
Current Cancer Drug Targets High Therapeutic Potential for Systemic Delivery of a Liposomeconjugated Herpes Simplex Virus
Current Cancer Drug Targets The Cell-Type Specificity and Endosomal Escape of Cell-Penetrating Peptides
Current Pharmaceutical Design The Use of Therapeutic Peptides to Target and to Kill Cancer Cells
Current Medicinal Chemistry The Role of Pemetrexed Combined with Targeted Agents for Non-Small Cell Lung Cancer
Current Drug Targets Facile Synthetic Protocols for the Preparation of New Impurities in Pemetrexed Disodium Heptahydrate as an Anti-cancer Drug
Current Organic Synthesis Editorial: (Thematic Issue: Occupational Exposure: An Undermined Risk Factor of Lung Diseases in the Informal Sectors of Developing Economy)
Current Respiratory Medicine Reviews Poly (ADP-Ribosyl) Polymerase 1 Inhibitors: A Patent Review
Recent Patents on Anti-Cancer Drug Discovery How Safe are Nanoparticles? A Review
Pharmaceutical Nanotechnology MicroRNA-dependent Regulation of Telomere Maintenance Mechanisms: A Field as Much Unexplored as Potentially Promising
Current Pharmaceutical Design Recent Advances in Small Molecule Inhibitors of VEGFR and EGFR Signaling Pathways
Current Topics in Medicinal Chemistry Electronic Noses in Medical Diagnostics
Current Medicinal Chemistry MicroRNAs and Long Non-coding RNAs as Novel Targets in Anti-cancer Drug Development
Current Pharmaceutical Biotechnology Phytotherapeutics in Cancer: From Potential Drug Candidates to Clinical Translation
Current Topics in Medicinal Chemistry Bacteria and Bacterial Toxins as Therapeutic Agents for Solid Tumors
Current Cancer Drug Targets