The structural requirements of histone deacetylase inhibitors: Suberoylanilide hydroxamic acid analogs modified at the C3 position display isoform selectivity |
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Authors: | Choi Sun Ea Weerasinghe Sujith V W Pflum Mary Kay H |
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Institution: | Department of Chemistry, Wayne State University, Detroit, MI 48202, USA. |
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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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Keywords: | Histone deaceylases HDAC inhibitors Vorinostat Isoform selectivity |
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