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Dipeptidyl nitroalkenes as potent reversible inhibitors of cysteine proteases rhodesain and cruzain

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 s...

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Main Authors: Latorre, Antonio (Author) , Schirmeister, Tanja (Author) , Kesselring, Jochen (Author) , Jung, Sascha (Author) , Johé, Patrick (Author) , Hellmich, Ute A. (Author) , Heilos, Anna (Author) , Engels, Bernd (Author) , Krauth-Siegel, Renate (Author) , Dirdjaja, Natalie (Author) , Bou-Iserte, Lledó (Author) , Rodríguez, Santiago (Author) , González, Florenci V. (Author)
Format: Article (Journal)
Language:English
Published: September 21, 2016
In: ACS medicinal chemistry letters
Year: 2016, Volume: 7, Issue: 12, Pages: 1073-1076
ISSN:1948-5875
DOI:10.1021/acsmedchemlett.6b00276
Online Access:Verlag, lizenzpflichtig, Volltext: https://doi.org/10.1021/acsmedchemlett.6b00276
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Author Notes:Antonio Latorre, Tanja Schirmeister, Jochen Kesselring, Sascha Jung, Patrick Johé, Ute A. Hellmich, Anna Heilos, Bernd Engels, R. Luise Krauth-Siegel, Natalie Dirdjaja, Lledó Bou-Iserte, Santiago Rodríguez, and Florenci V. González
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Summary: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.
Item Description:Gesehen am 15.06.2020
Physical Description:Online Resource
ISSN:1948-5875
DOI:10.1021/acsmedchemlett.6b00276

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