| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1370664 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
The FDA-approved drug suberoylanilide hydroxamic acid (SAHA, Vorinostat) was modified to improve its selectivity for a single histone deaetylase (HDAC) isoform. We show that attaching an ethyl group at the C3 position transforms SAHA from nonselective to an HDAC6-selective inhibitor. Theses results indicate that small structural changes in SAHA can significantly influence selectivity, which will lead future anti-cancer design efforts targeting HDAC proteins.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Sun Ea Choi, Sujith V.W. Weerasinghe, Mary Kay H. Pflum,