pntd.0006180.g003.tif (446.62 kB)
Enzymatic inhibition of TcSir2rp1 by BNIP derivatives.
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posted on 2018-01-22, 18:31 authored by Luís Gaspar, Ross P. Coron, Paul KongThoo Lin, David M. Costa, Begoña Perez-Cabezas, Joana Tavares, Meritxell Roura-Ferrer, Isbaal Ramos, Céline Ronin, Louise L. Major, Fabrice Ciesielski, Iain K. Pemberton, Jane MacDougall, Paola Ciapetti, Terry K. Smith, Anabela Cordeiro-da-SilvaA-B) The percentage of inhibition of the NAD+-dependent deacetylase activity of TcSir2rp1 by BNIP derivatives is represented in the y axis. Positive (no drug) and negative (NAM, nicotinamide at 2 mM) controls are represented. Bars represent the average + standard deviation of at least two independent experiments. Differences between the experimental groups were considered significant as follows: * p<0.05, *** p<0.001 and **** p<0.0001.
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NADprotein 1TcSIR 2rp modelreference drug benznidazolep 53 peptide substrateTcSir 2rp overexpressing epimastigotesTrypanosoma cruzi sirtuinsMedicinal chemistry modificationsparasite sirtuin inhibitorsChagas disease Chagas diseaseanti-parasitic activitycruzi Sir 2sirtuin inhibitor nicotinamideTcSir 2rpSilent information regulator 2Trypanosoma cruzi Sir 2compound BNIP Spermidine
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