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The Structural Requirements of Histone Deacetylase Inhibitors: Suberoylanilide Hydroxamic Acid Analogues Modified at the C3 Position Display Isoform Selectivity

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 non-selective to an HDAC6-selective inhibitor. Theses results...

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Detalhes bibliográficos
Main Authors: Choi, Sun Ea, Weerasinghe, Sujith V. W., Pflum, Mary Kay H.
Formato: Artigo
Idioma:Inglês
Publicado em: 2011
Assuntos:
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3842171/
https://ncbi.nlm.nih.gov/pubmed/21889343
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2011.08.027
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