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

作者：Latorre Antonio; Schirmeister Tanja; Kesselring Jochen; Jung Sascha; Johe Patrick; Hellmich Ute A; Heilos Anna; Engels Bernd; Krauth Siegel R Luise; Dirdjaja Natalie; Bou Iserte Liedo; Rodriguez Santiago; Gonzalez Florenci V

来源：ACS Medicinal Chemistry Letters, 2016, 7(12): 1073-1076.

DOI：10.1021/acsmedchemlett.6b00276

• Rhodesain
• cruzain
• inhibitors
• Chagas' disease
• sleeping sickness

Dipeptidyl nitroalkenes are potent reversible inhibitors of cysteine proteases. Inhibitor 11 resulted to be the most potent one with K-i 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.

• 出版日期2016-12