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Bioorg Med Chem Lett. 2012 Nov 1;22(21):6621-7. doi: 10.1016/j.bmcl.2012.08.104. Epub 2012 Sep 7.

Novel histone deacetylase 8 ligands without a zinc chelating group: exploring an 'upside-down' binding pose.

Author information

1
Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL 60612, USA.

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.

PMID:
23010266
PMCID:
PMC3472134
DOI:
10.1016/j.bmcl.2012.08.104
[Indexed for MEDLINE]
Free PMC Article

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