Identification of novel chemical scaffolds Inhibiting trypanothione synthetase from pathogenic trypanosomatids

2020-12-222020-12-222016-04-121935-2735http://hdl.handle.net/2133/19536The search for novel chemical entities targeting essential and parasite-specific pathways is considered a priority for neglected diseases such as trypanosomiasis and leishmaniasis. The thiol-dependent redox metabolism of trypanosomatids relies on bis-glutathionylspermidine [trypanothione, T(SH)2], a low molecular mass cosubstrate absent in the host. In pathogenic trypanosomatids, a single enzyme, trypanothione synthetase (TryS), catalyzes trypanothione biosynthesis, which is indispensable for parasite survival. Thus, TryS qualifies as an attractive drug target candidate.Para citar este articulo: Benítez D, Medeiros A, Fiestas L, PanozzoZenere EA, Maiwald F, Prousis KC, et al. (2016) Identification of Novel Chemical Scaffolds Inhibiting Trypanothione Synthetase from Pathogenic Trypanosomatids. PLoS Negl Trop Dis 10(4): e0004617. doi:10.1371/journal.pntd.0004617application/pdf1-25engopenAccessNeglected DiseasesTrypanothione Synthetase InhibitorsPathogenic TrypanosomatidsLeishmaniaTrypanosomaIdentification of novel chemical scaffolds Inhibiting trypanothione synthetase from pathogenic trypanosomatidsarticleUniversidad Nacional de RosarioBenítez, DiegoMedeiros, AndreaFiestas, LucíaPanozzo Zénere, Esteban AndrésMaiwald, FranziskaProusis, Kyriakos C.Roussaki, MarinaCalogeropoulou, TheodoraDetsi, AnastasiaJaeger, TimoŠarlauskas, JonasPeterlin Mašič, LucíjaKunick, ConradLabadie, Guillermo RobertoFlohé, LeopoldComini, Marcelo A.Attribution 4.0 International (CC BY 4.0)