Dual Inhibitors Against Topoisomerases and Histone Deacetylases
Journal of Cancer Prevention
;
: 85-91, 2015.
Article
in English
| WPRIM
| ID: wpr-30141
ABSTRACT
Topoisomerases and histone deacetylases (HDACs) are considered as important therapeutic targets for a wide range of cancers, due to their association with the initiation, proliferation and survival of cancer cells. Topoisomerases are involved in the cleavage and religation processes of DNA, while HDACs regulate a dynamic epigenetic modification of the lysine amino acid on various proteins. Extensive studies have been undertaken to discover small molecule inhibitor of each protein and thereby, several drugs have been transpired from this effort and successfully approved for clinical use. However, the inherent heterogeneity and multiple genetic abnormalities of cancers challenge the clinical application of these single targeted drugs. In order to overcome the limitations of a single target approach, a novel approach, simultaneously targeting topoisomerases and HDACs with a single molecule has been recently employed and attracted much attention of medicinal chemists in drug discovery. This review highlights the current studies on the discovery of dual inhibitors against topoisomerases and HDACs, provides their pharmacological aspects and advantages, and discusses the challenges and promise of the dual inhibitors.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Population Characteristics
/
DNA
/
Histones
/
Drug Discovery
/
Epigenomics
/
Histone Deacetylases
/
Lysine
Language:
English
Journal:
Journal of Cancer Prevention
Year:
2015
Type:
Article
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