Search results for "Chagas’ disease"

showing 1 items of 1 documents

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

2016

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. We 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…

Chagas’ diseasechemistry.chemical_classificationChagas diseaseProteasescruzain010405 organic chemistryChemistrysleeping sicknessOrganic Chemistry010402 general chemistrymedicine.disease01 natural sciencesBiochemistry0104 chemical sciencesRhodesainEnzymeBiochemistryCovalent bondinhibitorsDrug DiscoverymedicineDialysis (biochemistry)CysteineACS medicinal chemistry letters
researchProduct