The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors

Quaovi Sodji, Vishal Patil, Surendra Jain, James R. Kornacki, Milan Mrksich, Babu L. Tekwani*, Adegboyega K. Oyelere

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

14 Scopus citations

Abstract

Histone deacetylase inhibitors (HDACi) pleiotropy is largely due to their nonselective inhibition of various cellular HDAC isoforms. Connecting inhibition of a specific isoform to biological responses and/or phenotypes is essential toward deconvoluting HDACi pleiotropy. The contribution of classes I and II HDACs to the antileishmanial activity of HDACi was investigated using the amastigote and promastigote forms of Leishmania donovani. We observed that the antileishmanial activities of HDACi are largely due to the inhibition of HDAC6-like activity. This observation could facilitate the development of HDACi as antileishmanial agents.

Original languageEnglish (US)
Pages (from-to)4826-4830
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume24
Issue number20
DOIs
StatePublished - Oct 15 2014

Keywords

  • 3-Hydroxypyridin-2-thione
  • Histone deacetylase inhibitors
  • Leishmania donovani
  • Trichostatin A
  • Tubastatin A

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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