title: Histone deacetylase activators: N-acetylthioureas serve as highly potent and isozyme selective activators for human histone deacetylase-8 on a fluorescent substrate.
abstract: We report, for the first time, that certain N-acetylthiourea derivatives serve as highly potent and isozyme selective activators for the recombinant form of human histone deacetylase-8 in the assay system containing Fluor-de-Lys as a fluorescent substrate. The experimental data reveals that such activating feature is manifested via decrease in the K(m) value of the enzyme's substrate and increase in the catalytic turnover rate of the enzyme.
authors.affiliation: Department of Chemistry and Biochemistry, North Dakota State University, Fargo, ND 58108, USA.
authors.forename: Raushan K
authors.initials: RK
authors.lastname: Singh
authors.forename: Tanmay
authors.initials: T
authors.lastname: Mandal
authors.forename: Narayanaganesh
authors.initials: N
authors.lastname: Balsubramanian
authors.forename: Tajae
authors.initials: T
authors.lastname: Viaene
authors.forename: Travis
authors.initials: T
authors.lastname: Leedahl
authors.forename: Nitesh
authors.initials: N
authors.lastname: Sule
authors.forename: Gregory
authors.initials: G
authors.lastname: Cook
authors.forename: D K
authors.initials: DK
authors.lastname: Srivastava
mesh_terms: D001549:Benzamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001665:Binding Sites; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D055808:Drug Discovery; D004789:Enzyme Activation; D020536:Enzyme Activators / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D005456:Fluorescent Dyes / Q000378:metabolism; D006655:Histone Deacetylases / Q000378:metabolism*; D006801:Humans; D007527:Isoenzymes / Q000378:metabolism; D007700:Kinetics; D008956:Models, Chemical; D058990:Molecular Targeted Therapy; D010670:Phenylthiourea / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D012984:Software; D013329:Structure-Activity Relationship; D013379:Substrate Specificity; D013890:Thiourea / Q000031:analogs & derivatives* / Q000737:chemistry
chemical_list: D001549:Benzamides; D020536:Enzyme Activators; D005456:Fluorescent Dyes; D007527:Isoenzymes; C571363:N-(phenylcarbothiol)benzamide; C062177:acetylthiourea; D010670:Phenylthiourea; D006655:Histone Deacetylases; D013890:Thiourea