Inhibitors | Comment | Organism | Structure |
---|---|---|---|
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 | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
Lys-Arg-primaquine + H2O | Trypanosoma cruzi | - |
Lys-Arg + primaquine | - |
? | |
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 | ? | - |
? | |
Phe-Ala-primaquine + H2O | Trypanosoma cruzi | - |
Phe-Ala + primaquine | - |
? | |
Phe-Arg-primaquine + H2O | Trypanosoma cruzi | - |
Phe-Arg + primaquine | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Trypanosoma cruzi | - |
- |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
Lys-Arg-primaquine + H2O | - |
Trypanosoma cruzi | Lys-Arg + primaquine | - |
? | |
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 | ? | - |
? | |
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 | ? | - |
? | |
Phe-Ala-primaquine + H2O | - |
Trypanosoma cruzi | Phe-Ala + primaquine | - |
? | |
Phe-Arg-primaquine + H2O | - |
Trypanosoma cruzi | Phe-Arg + primaquine | - |
? |
Synonyms | Comment | Organism |
---|---|---|
cruzain | - |
Trypanosoma cruzi |