title: The antileishmanial activity of isoforms 6- and 8-selective histone deacetylase inhibitors.
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.
authors.affiliation: School of Chemistry and Biochemistry, Parker H. Petit for Bioengineering and Bioscience, Georgia Institute of Technology, Atlanta, GA 30332-0400, USA.
authors.forename: Quaovi
authors.initials: Q
authors.lastname: Sodji
authors.affiliation: School of Chemistry and Biochemistry, Parker H. Petit for Bioengineering and Bioscience, Georgia Institute of Technology, Atlanta, GA 30332-0400, USA.
authors.forename: Vishal
authors.initials: V
authors.lastname: Patil
authors.affiliation: National Center for Natural Products Research, School of Pharmacy, University of Mississippi, University, MS 38677-1848, USA.
authors.forename: Surendra
authors.initials: S
authors.lastname: Jain
authors.affiliation: Department of Chemistry and Biomedical Engineering, Northwestern University, 2145 Sheridan Rd, Evanston, IL 60208-3113, USA.
authors.forename: James R
authors.initials: JR
authors.lastname: Kornacki
authors.affiliation: Department of Chemistry and Biomedical Engineering, Northwestern University, 2145 Sheridan Rd, Evanston, IL 60208-3113, USA.
authors.forename: Milan
authors.initials: M
authors.lastname: Mrksich
authors.affiliation: National Center for Natural Products Research, School of Pharmacy, University of Mississippi, University, MS 38677-1848, USA. Electronic address: btekwani@olemiss.edu.
authors.forename: Babu L
authors.initials: BL
authors.lastname: Tekwani
authors.affiliation: School of Chemistry and Biochemistry, Parker H. Petit for Bioengineering and Bioscience, Georgia Institute of Technology, Atlanta, GA 30332-0400, USA. Electronic address: aoyelere@gatech.edu.
authors.forename: Adegboyega K
authors.initials: AK
authors.lastname: Oyelere
mesh_terms: D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D056572:Histone Deacetylase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006655:Histone Deacetylases / Q000378:metabolism*; D007527:Isoenzymes / Q000037:antagonists & inhibitors / Q000378:metabolism; D007893:Leishmania donovani / Q000187:drug effects* / Q000201:enzymology; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D013329:Structure-Activity Relationship
chemical_list: D000981:Antiprotozoal Agents; D056572:Histone Deacetylase Inhibitors; D007527:Isoenzymes; D006655:Histone Deacetylases
keywords: 3-Hydroxypyridin-2-thione; Histone deacetylase inhibitors; Leishmania donovani; Trichostatin A; Tubastatin A