4.5 Article

Development of a Potent and Selective HDAC8 Inhibitor

期刊

ACS MEDICINAL CHEMISTRY LETTERS
卷 7, 期 10, 页码 929-932

出版社

AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.6b00239

关键词

Histone deacetylase; HDAC; histone deacetylase 8; HDAC8; triazole; epigenetic

资金

  1. Boston University
  2. Center for Chemical Methodology and Library Development at Boston University [GM-067041]
  3. NSF [CHE-0619339, CHE- 0443618]
  4. [R24-GM111625]

向作者/读者索取更多资源

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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