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Dipeptidyl Nitroalkenes as Potent Reversible Inhibitors of Cysteine Proteases Rhodesain and Cruzain

dc.contributor.authorLatorre, Antonio
dc.contributor.authorSchirmeister, Tanja
dc.contributor.authorKesselring, Jochen
dc.contributor.authorJung, Sascha
dc.contributor.authorJohé, Patrick
dc.contributor.authorHellmich, Ute A.
dc.contributor.authorHeilos, Anna
dc.contributor.authorEngels, Bernd
dc.contributor.authorKrauth-Siegel, R. Luise
dc.contributor.authorDirdjaja, Natalie
dc.contributor.authorBou Iserte, Lledó
dc.contributor.authorRodríguez, Santiago
dc.contributor.authorGonzález, Florenci
dc.date.accessioned2017-06-27T06:55:02Z
dc.date.available2017-06-27T06:55:02Z
dc.date.issued2016
dc.identifier.citationLATORRE, Antonio, et al. Dipeptidyl Nitroalkenes as Potent Reversible Inhibitors of Cysteine Proteases Rhodesain and Cruzain. ACS medicinal chemistry letters, 2016, vol. 7, no 12, p. 1073-1076.ca_CA
dc.identifier.issn1948-5875
dc.identifier.urihttp://hdl.handle.net/10234/168102
dc.description.abstractDipeptidyl nitroalkenes are potent reversible inhibitors of cysteine proteases. Inhibitor 11 resulted to be the most potent one with Ki values of 0.49 and 0.44 nM against rhodesain and cruzain, respectively. According to enzymatic dilution and dialysis experiments, as well as computational and NMR studies, dipeptidyl nitroalkenes are tightly binding covalent reversible inhibitors.ca_CA
dc.description.sponsorShipWe thank Fundacion Española para la Ciencia y la Tecnología (Fecyt) and Generalitat Valenciana (AICO/2016/32) for financial support. T S. and B.E. thank the DFG (Deutsche Forschungsgemeinschaft) in the framework of the SFB630 for financial support. We thank Universitat Jaume I for technical suppport and funding. U.A.H. acknowledges support by the Carl-Zeiss foundation as well as the Center of Biomolecular Magnetic Resonance (BMRZ) funded by the state of Hesse.ca_CA
dc.format.extent4 p.ca_CA
dc.language.isoengca_CA
dc.publisherAmerican Chemical Societyca_CA
dc.relation.isPartOfACS medicinal chemistry letters, 2016, vol. 7, no 12ca_CA
dc.rightsCopyright © American Chemical Societyca_CA
dc.rights.urihttp://rightsstatements.org/vocab/InC/1.0/*
dc.subjectChagas’ diseaseca_CA
dc.subjectcruzainca_CA
dc.subjectinhibitorsca_CA
dc.subjectRhodesainca_CA
dc.subjectsleeping sicknessca_CA
dc.titleDipeptidyl Nitroalkenes as Potent Reversible Inhibitors of Cysteine Proteases Rhodesain and Cruzainca_CA
dc.typeinfo:eu-repo/semantics/articleca_CA
dc.identifier.doihttp://dx.doi.org/10.1021/acsmedchemlett.6b00276
dc.rights.accessRightsinfo:eu-repo/semantics/restrictedAccessca_CA
dc.relation.publisherVersionhttp://pubs.acs.org/doi/abs/10.1021/acsmedchemlett.6b00276#cor1ca_CA


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