| Literature DB >> 21353783 |
Silviya D Furdas1, Suhaib Shekfeh, Elisabeth-Maria Bissinger, Julia M Wagner, Sonja Schlimme, Vassil Valkov, Michael Hendzel, Manfred Jung, Wolfgang Sippl.
Abstract
We present a combination of database screening, synthesis and in vitro testing to identify novel histone acetyltransferase (HAT) inhibitors. The National Cancer Institute compound collection (NCI) and several commercial databases were filtered by similarity-based virtual screening to find new HAT inhibitors. Employing the recombinant HAT p300/CBP-associated factor (PCAF) and two different histone substrates for screening, pyridoisothiazolones were identified as inhibitors of human PCAF. Due to the limited solubility of the initial hits, we synthesized and tested them on PCAF. The compounds inhibit the proliferation of cancer cells. In summary, valuable chemical tools and potential lead candidates for new anticancer agents directed against HATs as new targets have been identified.Entities:
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Year: 2011 PMID： 21353783 DOI： 10.1016/j.bmc.2011.01.063
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641