title: Dipeptidyl Nitroalkenes as Potent Reversible Inhibitors of Cysteine Proteases Rhodesain and Cruzain.
abstract: Dipeptidyl nitroalkenes are potent reversible inhibitors of cysteine proteases. Inhibitor11resulted to be the most potent one withKivalues 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.
authors.affiliation: Departament de Química Inorgànica i Orgànica, Universitat Jaume I , 12080 Castelló, Spain.
authors.forename: Antonio
authors.initials: A
authors.lastname: Latorre
authors.affiliation: Institute of Pharmacy and Biochemistry, University of Mainz , Staudinger Weg 5, 55099 Mainz, Germany.
authors.forename: Tanja
authors.initials: T
authors.lastname: Schirmeister
authors.affiliation: Institute of Pharmacy and Biochemistry, University of Mainz , Staudinger Weg 5, 55099 Mainz, Germany.
authors.forename: Jochen
authors.initials: J
authors.lastname: Kesselring
authors.affiliation: Institute of Pharmacy and Biochemistry, University of Mainz , Staudinger Weg 5, 55099 Mainz, Germany.
authors.forename: Sascha
authors.initials: S
authors.lastname: Jung
authors.affiliation: Institute of Pharmacy and Biochemistry, University of Mainz , Staudinger Weg 5, 55099 Mainz, Germany.
authors.forename: Patrick
authors.initials: P
authors.lastname: Johé
authors.affiliation: Institute of Pharmacy and Biochemistry, University of Mainz, Staudinger Weg 5, 55099 Mainz, Germany; Institute of Pharmacy and Biochemistry, University of Mainz, Johann-Joachim Becherweg 30, 55128 Mainz, Germany; Center of Biomolecular Magnetic Resonance (BMRZ), Goethe University, 60323 Frankfurt, Germany.
authors.forename: Ute A
authors.initials: UA
authors.lastname: Hellmich
authors.affiliation: Institute of Phys. and Theor. Chemistry, University of Würzburg , Emil-Fischer-Straße 42, 97074 Würzburg, Germany.
authors.forename: Anna
authors.initials: A
authors.lastname: Heilos
authors.affiliation: Institute of Phys. and Theor. Chemistry, University of Würzburg , Emil-Fischer-Straße 42, 97074 Würzburg, Germany.
authors.forename: Bernd
authors.initials: B
authors.lastname: Engels
authors.affiliation: Biochemie-Zentrum Heidelberg (BZH), Universität Heidelberg , Im Neuenheimer Feld 328, 69120 Heidelberg, Germany.
authors.forename: R Luise
authors.initials: RL
authors.lastname: Krauth-Siegel
authors.affiliation: Biochemie-Zentrum Heidelberg (BZH), Universität Heidelberg , Im Neuenheimer Feld 328, 69120 Heidelberg, Germany.
authors.forename: Natalie
authors.initials: N
authors.lastname: Dirdjaja
authors.affiliation: Departament de Química Inorgànica i Orgànica, Universitat Jaume I , 12080 Castelló, Spain.
authors.forename: Lledó
authors.initials: L
authors.lastname: Bou-Iserte
authors.affiliation: Departament de Química Inorgànica i Orgànica, Universitat Jaume I , 12080 Castelló, Spain.
authors.forename: Santiago
authors.initials: S
authors.lastname: Rodríguez
authors.affiliation: Departament de Química Inorgànica i Orgànica, Universitat Jaume I , 12080 Castelló, Spain.
authors.forename: Florenci V
authors.initials: FV
authors.lastname: González
keywords: Chagas’ disease; Rhodesain; cruzain; inhibitors; sleeping sickness