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Showing posts with label HDAC. Show all posts
Showing posts with label HDAC. Show all posts

Saturday, March 17, 2012

Future Science - abstract: Targeted cancer therapy: giving histone deacetylase inhibitors



Future Science - Future Medicinal Chemistry - 4(4):505 - Summary

Review
Abstract

Targeted cancer therapy: giving histone deacetylase inhibitors


"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™) and FK228 (romidepsin, Istodax™). 

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."

Friday, August 13, 2010

Expert Opinion on Investigational Drugs - Summary: Histone deacetylase (HDAC) inhibitors



Take home message: There are extensive preclinical studies with transformed cells in culture and tumor-bearing animal models, as well as limited clinical studies reported to date, which indicate that HDAC inhibitors will be most useful when used in combination with cytotoxic or other targeted anticancer agents.