Journal
CURRENT DRUG TARGETS
Volume 19, Issue 7, Pages 815-824Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1389450118666170112130151
Keywords
HATs; HDACs; HDACi; isoform-selective inhibitors; anticancer therapy; gene expression
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Funding
- DST-SERB, Government of India [YSS/2015/001267]
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Histone deacetylase inhibitors, the small molecules modulating the biological activity of histone deacetylases are emerging as potent chemotherapeutic agents. Despite their considerable therapeutic benefits in disease models, the lack of isoform specificity culminates in debilitating off target effects, raising serious concerns regarding their applicability. This emphasizes the pressing and unmet medical need of designing isoform selective inhibitors for safe and effective anticancer therapy. Keeping these grim facts in view, the current article sheds light on structural basis of off-targeting. Furthermore, the article discusses extensively the role of in silico strategies such as Molecular Docking, Molecular Dynamics Simulation and Energetically-optimized structure based pharmacophore approach in designing on-target inhibitors against classical HDACs.
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