| Literature DB >> 23010266 |
Aditya Sudheer Vaidya1, Raghupathi Neelarapu, Antonett Madriaga, He Bai, Emma Mendonca, Hazem Abdelkarim, Richard B van Breemen, Sylvie Y Blond, Pavel A Petukhov.
Abstract
A novel series of HDAC8 inhibitors without a zinc-chelating hydroxamic acid moiety is reported. Photoaffinity labeling and molecular modeling studies suggest that these ligands are likely to bind in an 'upside-down' fashion in a secondary binding site proximal to the main catalytic site. The most potent ligand in the series exhibits an IC(50) of 28 μM for HDAC8 and is found to inhibit the deacetylation of H4 but not α-tubulin in SH-SY5Y cell line.Entities:
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Year: 2012 PMID： 23010266 PMCID： PMC3472134 DOI： 10.1016/j.bmcl.2012.08.104
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823