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

ABSTRACT: 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.

SUBMITTER: Latorre A

PROVIDER: S-EPMC5150692 | biostudies-literature | 2016 Dec

REPOSITORIES: biostudies-literature

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

Latorre Antonio A Schirmeister Tanja T Kesselring Jochen J Jung Sascha S Johé Patrick P Hellmich Ute A UA Heilos Anna A Engels Bernd B Krauth-Siegel R Luise RL Dirdjaja Natalie N Bou-Iserte Lledó L Rodríguez Santiago S González Florenci V FV

ACS medicinal chemistry letters 20160921 12

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. ...[more]

PMID: 27994740

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