期刊
FUTURE MEDICINAL CHEMISTRY
卷 4, 期 4, 页码 505-524出版社
FUTURE SCI LTD
DOI: 10.4155/FMC.12.3
关键词
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资金
- Georgia Institute of Technology
- Blanchard fellowship
- NIH [R01CA131217]
- Georgia Tech Center for Drug Design, Development and Delivery
Histone deacetylase inhibitors (HDACis) have now emerged as a powerful new class of small-molecule therapeutics acting through the regulation of the acetylation states of histone proteins (a form of epigenetic modulation) and other non-histone protein targets. Over 490 clinical trials have been initiated in the last 10 years, culminating in the approval of two structurally distinct HDACis SAHA (vorinostat, ZolinzA (TM)) and FK228 (romidepsin, Istodax (TM)). However, the current HDACis have serious limitations, including ineffectively low concentrations in solid tumors and cardiac toxicity, which is hindering their progress in the clinic. Herein, we review the primary paradigms being pursued to overcome these hindrances, including HDAC isoform selectivity, localized administration, and targeting cap groups to achieve selective tissue and cell type distribution.
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