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De Gomez-Puyou, MT; Perez Montfort, R; GomezPuyou A; Cabrera, N; Cerecetto, H; Gonzalez, M; Di Maio, R; Porcal, W; Lavaggi, ML; Lopez, GV; Merlino, A; Cabrera, M; Varela, J; Aguirre-Lopez, B; Alvarez, G (2010)

MASSIVE SCREENING YIELDS NOVEL AND SELECTIVE TRYPANOSOMA CRUZI TRIOSEPHOSPHATE ISOMERASE DIMER-INTERFACE-IRREVERSIBLE INHIBITORS WITH ANTI-TRYPANOSOMA

EUR J MED CHEM 45(12):5767-5772
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Triosephosphate isomerase from Trypanosoma cruzi (TcTIM), an enzyme in the glycolytic pathway that exhibits high catalytic rates of glyceraldehyde-3-phosphate- and dihydroxyacetone-phosphate-isomerization only in its dimeric form, was screened against an in-house chemical library containing nearly 230 compounds belonging to different chemotypes. After secondary screening, twenty-six compounds from eight different chemotypes were identified as screening positives. Four compounds displayed selectivity for TcTIM over TIM from Homo sapiens and, concomitantly, in vitro activity against T cruzi. (C) 2010 Elsevier Masson SAS. All rights reserved.