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Development of a Potent and Selective HDAC8 Inhibitor.
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.
Afiliação
  • Ingham OJ; Department of Chemistry and Center for Molecular Discovery (BU-CMD), Boston University , 590 Commonwealth Avenue, Boston, Massachusetts 02215, United States.
  • Paranal RM; Department of Medical Oncology, Dana Farber Cancer Institute , Boston, Massachusetts 02215, United States.
  • Smith WB; Department of Medical Oncology, Dana Farber Cancer Institute , Boston, Massachusetts 02215, United States.
  • Escobar RA; Department of Chemistry and Center for Molecular Discovery (BU-CMD), Boston University , 590 Commonwealth Avenue, Boston, Massachusetts 02215, United States.
  • Yueh H; Department of Chemistry and Center for Molecular Discovery (BU-CMD), Boston University , 590 Commonwealth Avenue, Boston, Massachusetts 02215, United States.
  • Snyder T; Department of Chemistry and Center for Molecular Discovery (BU-CMD), Boston University , 590 Commonwealth Avenue, Boston, Massachusetts 02215, United States.
  • Porco JA; Department of Chemistry and Center for Molecular Discovery (BU-CMD), Boston University , 590 Commonwealth Avenue, Boston, Massachusetts 02215, United States.
  • Bradner JE; Department of Medical Oncology, Dana Farber Cancer Institute, Boston, Massachusetts 02215, United States; Department of Medicine, Harvard Medical School, Boston, Massachusetts 02115, United States.
  • Beeler AB; Department of Chemistry and Center for Molecular Discovery (BU-CMD), Boston University , 590 Commonwealth Avenue, Boston, Massachusetts 02215, United States.
ACS Med Chem Lett ; 7(10): 929-932, 2016 Oct 13.
Article em En | MEDLINE | ID: mdl-27774131
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.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2016 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2016 Tipo de documento: Article