2. Academic Validation
  3. Design and synthesis of a potent histone deacetylase inhibitor

Design and synthesis of a potent histone deacetylase inhibitor

  • J Med Chem. 2007 May 3;50(9):2003-6. doi: 10.1021/jm061082q.
Tao Liu 1,  Galina Kapustin,  Felicia A Etzkorn
Affiliations

Affiliation

  • 1 Virginia Tech, Department of Chemistry MC 0212, Blacksburg, Virginia 24061-0212, USA.
PMID: 17419603 DOI: 10.1021/jm061082q
Abstract

Histone deacetylase (HDAC) inhibitors have potential for Cancer therapy. An HDAC Inhibitor based on a cyclic peptide mimic of known structure, linked by an aliphatic chain to a hydroxamic acid, was designed and synthesized. The chimeric compound showed potent competitive inhibition of nuclear HDACs, with an IC50 value of 46 nM and a Ki value of 13.7 nM. The designed inhibitor showed 4-fold selectivity for HDAC1 (57 nM) over HDAC8 (231 nM).

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