Development of a Potent and Selective HDAC8 Inhibitor

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.

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Bibliographic Details
Published inACS medicinal chemistry letters Vol. 7; no. 10; pp. 929 - 932
Main Authors Ingham, Oscar J, Paranal, Ronald M, Smith, William B, Escobar, Randolph A, Yueh, Han, Snyder, Tracy, Porco, John A, Bradner, James E, Beeler, Aaron B
Format Journal Article
LanguageEnglish
Published WASHINGTON American Chemical Society 13.10.2016
Amer Chemical Soc
Subjects
Chemistry, Medicinal
Letter
Life Sciences & Biomedicine
Pharmacology & Pharmacy
Science & Technology
Histone deacetylase
HDAC8
epigenetic
histone deacetylase 8
HDAC
triazole
DESIGN
CANCER
DISCOVERY
HISTONE
CYCLOADDITION
CORNELIA
DEACETYLASE INHIBITORS
MUTATIONS
SPECTRUM
BINDING
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Summary: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.
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ISSN:1948-5875
1948-5875
DOI:10.1021/acsmedchemlett.6b00239