Dipeptidyl Nitroalkenes as Potent Reversible Inhibitors of Cysteine Proteases Rhodesain and Cruzain
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Scholar |
Otros documentos de la autoría: Latorre, Antonio; Schirmeister, Tanja; Kesselring, Jochen; Jung, Sascha; Johé, Patrick; Hellmich, Ute A.; Heilos, Anna; Engels, Bernd; Krauth-Siegel, R. Luise; Dirdjaja, Natalie; Bou Iserte, Lledó; Rodríguez, Santiago; González, Florenci
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http://dx.doi.org/10.1021/acsmedchemlett.6b00276 |
Metadatos
Título
Dipeptidyl Nitroalkenes as Potent Reversible Inhibitors of Cysteine Proteases Rhodesain and CruzainAutoría
Fecha de publicación
2016Editor
American Chemical SocietyISSN
1948-5875Cita bibliográfica
LATORRE, 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.Tipo de documento
info:eu-repo/semantics/articleVersión de la editorial
http://pubs.acs.org/doi/abs/10.1021/acsmedchemlett.6b00276#cor1Palabras clave / Materias
Resumen
Dipeptidyl 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 ... [+]
Dipeptidyl 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. [-]
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ACS medicinal chemistry letters, 2016, vol. 7, no 12Derechos de acceso
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