科研之友
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摘要
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 IC50 of 28 mu M for HDAC8 and is found to inhibit the deacetylation of H4 but not alpha-tubulin in SH-SY5Y cell line.
- 出版日期2012-11-1
