HDAC inhibitors lead to hyperacetylation of histones, which should, at least partially neutralize the nagetive charge of DNA molecules. In view of this, HDAC inhibitors should lead to chromatin relaxation. Anyone recommend some papers which explain the mechanisms in detail?
Yes - Please see the attached article....page 2 discusses mechanism
Hi Zhiming,
This is the link to an articles we published a while back. Describes the mechanism you're referring to.
http://ac.els-cdn.com/S0163725813001253/1-s2.0-S0163725813001253-main.pdf?_tid=ecb09b96-aadb-11e4-b681-00000aacb35e&acdnat=1422882407_cd78f22f2b9d7530160c8095bea7c45a
Yes, that's why for instance topoisomerases can bind in a better way to DNA and consequently combination with topoisomerase inhibitors gives enhanced anticancer activity.
Kim, M.S.; Blake, M.; Baek, J.H.; Kohlhagen, G.; Pommier, Y.; Carrier, F. Inhibition of histonedeacetylase increases cytotoxicity to anticancer drugs targeting DNA. Cancer Res., 2003, 63, 7291-7300.
Catalano, M.G.; Fortunati, N.; Pugliese, M.; Poli, R.; Bosco, O.; Mastrocola, R.; Aragno, M.; Bocuzzi, G. Valproic acid, a histone deacetylase inhibitor, enhances sensitivity to doxorubicin in anaplastic thyroid cancer cells. J. Endocrinol., 2006, 191, 465-472.
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