Synopsis
Histone deacetylases (HDACs) regulate gene expression mainly by deacetylating the histone substrates. They play a crucial role in regulating cell processes including cell-cycle progression and apoptosis. Aberrant expression of HDACs plays an active role in tumor onset and progression, making them candidate targets for anticancer drugs and therapy. Class I HDACs being ubiquitous in distribution are mainly involved in cancer. Pharmacological intervention using histone deacetylase inhibitors (HDACi) often targets all the members of Class I HDACs culminating in disastrous side effects. Thus, there is an escalating need to design target-specific inhibitors. Many approaches have been taken to modulate the HDACi to address such challenges. This entry provides intricate details about the in silico approaches taken by the scientific community for designing selective inhibitors against Class I HDAC isoforms. The methods discussed in this entry will open novel avenues for pharmacists and...
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Ganai, S.A. (2015). In Silico Approaches Towards Safe Targeting of Class I Histone Deacetylases. In: Wells, R., Bond, J., Klinman, J., Masters, B., Bell, E. (eds) Molecular Life Sciences. Springer, New York, NY. https://doi.org/10.1007/978-1-4614-6436-5_459-1
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DOI: https://doi.org/10.1007/978-1-4614-6436-5_459-1
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