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

作者信息

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

机构信息

School of Chemistry and Biochemistry, Parker H. Petit for Bioengineering and Bioscience, Georgia Institute of Technology, Atlanta, GA 30332-0400, USA.

National Center for Natural Products Research, School of Pharmacy, University of Mississippi, University, MS 38677-1848, USA.

出版信息

Bioorg Med Chem Lett. 2014 Oct 15;24(20):4826-30. doi: 10.1016/j.bmcl.2014.08.060. Epub 2014 Sep 4.

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.

摘要

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