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Development of a Potent and Selective HDAC8 Inhibitor.


ABSTRACT: A novel, isoform-selective inhibitor of histone deacetylase 8 (HDAC8) has been discovered by the repurposing of a diverse compound collection. Medicinal chemistry optimization led to the identification of a highly potent (0.8 nM) and selective inhibitor of HDAC8.

SUBMITTER: Ingham OJ 

PROVIDER: S-EPMC5066159 | biostudies-literature | 2016 Oct

REPOSITORIES: biostudies-literature

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Development of a Potent and Selective HDAC8 Inhibitor.

Ingham Oscar J OJ   Paranal Ronald M RM   Smith William B WB   Escobar Randolph A RA   Yueh Han H   Snyder Tracy T   Porco John A JA   Bradner James E JE   Beeler Aaron B AB  

ACS medicinal chemistry letters 20160901 10


A novel, isoform-selective inhibitor of histone deacetylase 8 (HDAC8) has been discovered by the repurposing of a diverse compound collection. Medicinal chemistry optimization led to the identification of a highly potent (0.8 nM) and selective inhibitor of HDAC8. ...[more]

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