title: 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.
authors: Department of Chemistry and Center for Molecular Discovery (BU-CMD), Boston University , 590 Commonwealth Avenue, Boston, Massachusetts 02215, United States.
authors: Oscar J
authors: OJ
authors: Ingham
authors: Department of Medical Oncology, Dana Farber Cancer Institute , Boston, Massachusetts 02215, United States.
authors: Ronald M
authors: RM
authors: Paranal
authors: Department of Medical Oncology, Dana Farber Cancer Institute , Boston, Massachusetts 02215, United States.
authors: William B
authors: WB
authors: Smith
authors: Department of Chemistry and Center for Molecular Discovery (BU-CMD), Boston University , 590 Commonwealth Avenue, Boston, Massachusetts 02215, United States.
authors: Randolph A
authors: RA
authors: Escobar
authors: Department of Chemistry and Center for Molecular Discovery (BU-CMD), Boston University , 590 Commonwealth Avenue, Boston, Massachusetts 02215, United States.
authors: Han
authors: H
authors: Yueh
authors: Department of Chemistry and Center for Molecular Discovery (BU-CMD), Boston University , 590 Commonwealth Avenue, Boston, Massachusetts 02215, United States.
authors: Tracy
authors: T
authors: Snyder
authors: Department of Chemistry and Center for Molecular Discovery (BU-CMD), Boston University , 590 Commonwealth Avenue, Boston, Massachusetts 02215, United States.
authors: John A
authors: JA
authors: Porco
authors: Department of Medical Oncology, Dana Farber Cancer Institute, Boston, Massachusetts 02215, United States; Department of Medicine, Harvard Medical School, Boston, Massachusetts 02115, United States.
authors: James E
authors: JE
authors: Bradner
authors: Department of Chemistry and Center for Molecular Discovery (BU-CMD), Boston University , 590 Commonwealth Avenue, Boston, Massachusetts 02215, United States.
authors: Aaron B
authors: AB
authors: Beeler
keywords: HDAC; HDAC8; Histone deacetylase; epigenetic; histone deacetylase 8; triazole