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Literature summary extracted from

  • Trossini, G.; Chin, C.; de Souza Menezes, C.; Ferreira, E.
    Molecular modeling suggests cruzain specificity for peptide primaquine prodrugs (2010), Lett. Drug Des. Discov., 7, 528-533.
No PubMed abstract available

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.22.51 primaquine active against cruzipain, design of selective prodrugs Lys-Arg-primaquine, Phe-Ala-primaquine, and Phe-Arg-primaquine to be cleaved by the enzyme in vivo and selectively inhibiting it, overview Trypanosoma cruzi

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.4.22.51 Lys-Arg-primaquine + H2O Trypanosoma cruzi
-
 Lys-Arg + primaquine
-
 ?
3.4.22.51 additional information Trypanosoma cruzi design of selective prodrugs of primaquine: Lys-Arg-primaquine, Phe-Ala-primaquine, and Phe-Arg-primaquine, cleaved by the enzyme in vivo and selectively inhibiting it, overview ?
-
 ?
3.4.22.51 Phe-Ala-primaquine + H2O Trypanosoma cruzi
-
 Phe-Ala + primaquine
-
 ?
3.4.22.51 Phe-Arg-primaquine + H2O Trypanosoma cruzi
-
 Phe-Arg + primaquine
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
3.4.22.51 Trypanosoma cruzi
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.22.51 Lys-Arg-primaquine + H2O
-
 Trypanosoma cruzi Lys-Arg + primaquine
-
 ?
3.4.22.51 additional information design of selective prodrugs of primaquine: Lys-Arg-primaquine, Phe-Ala-primaquine, and Phe-Arg-primaquine, cleaved by the enzyme in vivo and selectively inhibiting it, overview Trypanosoma cruzi ?
-
 ?
3.4.22.51 additional information design of selective prodrugs of primaquine: Lys-Arg-primaquine, Phe-Ala-primaquine, and Phe-Arg-primaquine, cleaved by the enzyme in vivo and selectively inhibiting it, overview. The molecular mechanism acts via nucleophilic attack of the catalytic Cys25 residue on the respective prodrug amide carbonyl carbon, releasing primaquine, docking study showing specific interactions between the prodrug and the S1 and S2 pockets of cruzipain with the dipeptides acting as distance holders Trypanosoma cruzi ?
-
 ?
3.4.22.51 Phe-Ala-primaquine + H2O
-
 Trypanosoma cruzi Phe-Ala + primaquine
-
 ?
3.4.22.51 Phe-Arg-primaquine + H2O
-
 Trypanosoma cruzi Phe-Arg + primaquine
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.22.51 cruzain
-
 Trypanosoma cruzi