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Literature summary for 1.8.1.12 extracted from

  • Salmon-Chemin, L.; Buisine, E.; Yardley, V.; Kohler, S.; Debreu, M.A.; Landry, V.; Sergheraert, C.; Croft, S.L.; Krauth-Siegel, R.L.; Davioud-Charvet, E.
    2- And 3-substituted 1,4-naphthoquinone derivatives as subversive substrates of trypanothione reductase and lipoamide dehydrogenase from Trypanosoma cruzi: Synthesis and correlation between redox cycling activities and in vitro cytotoxicity (2001), J. Med. Chem., 44, 548-565.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
additional information activity is dependent on a redox-active cysteine at the active centre Trypanosoma brucei
additional information activity is dependent on a redox-active cysteine at the active centre Leishmania donovani
additional information activity is dependent on a redox-active cysteine at the active centre Trypanosoma cruzi

Application

Application Comment Organism
medicine
-
Trypanosoma brucei
medicine good target for structure/function studies and trypanicidal inhibitor design Trypanosoma cruzi
medicine potential target for drug design against trypanosomiasis Trypanosoma cruzi
medicine target for rational approach to design new anti-leishmanial chemotherapeutic agents Leishmania donovani

Inhibitors

Inhibitors Comment Organism Structure
3,3'-[polyaminobis(carbonylalkyl)]bis(1,4-naphthoquinone) derivatives
-
Trypanosoma cruzi
juglone
-
Leishmania donovani
juglone
-
Trypanosoma brucei
juglone
-
Trypanosoma cruzi
juglone derivatives
-
Leishmania donovani
juglone derivatives
-
Trypanosoma brucei
juglone derivatives
-
Trypanosoma cruzi
menadione
-
Trypanosoma cruzi
menadione derivatives
-
Leishmania donovani
menadione derivatives
-
Leishmania infantum
menadione derivatives
-
Trypanosoma brucei
menadione derivatives
-
Trypanosoma cruzi
Plumbagin
-
Trypanosoma brucei
Plumbagin
-
Trypanosoma cruzi
plumbagin derivatives
-
Leishmania donovani
plumbagin derivatives
-
Leishmania infantum
plumbagin derivatives
-
Trypanosoma brucei
plumbagin derivatives
-
Trypanosoma cruzi

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
trypanothione disulfide + NADPH Trypanosoma brucei
-
trypanothione + NADP+
-
?
trypanothione disulfide + NADPH Leishmania donovani
-
trypanothione + NADP+
-
?
trypanothione disulfide + NADPH Leishmania infantum
-
trypanothione + NADP+
-
?
trypanothione disulfide + NADPH Trypanosoma cruzi
-
trypanothione + NADP+
-
?

Organism

Organism UniProt Comment Textmining
Leishmania donovani
-
-
-
Leishmania infantum
-
-
-
Trypanosoma brucei
-
-
-
Trypanosoma cruzi P28593
-
-

Reaction

Reaction Comment Organism Reaction ID
trypanothione + NADP+ = trypanothione disulfide + NADPH + H+ molecular modeling of inhibitor binding using X-ray data Trypanosoma cruzi

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
glutathionylspermidine disulfide + NADPH
-
Leishmania donovani 2-glutathionylspermidine + NADP+
-
?
glutathionylspermidine disulfide + NADPH
-
Trypanosoma cruzi 2-glutathionylspermidine + NADP+
-
?
additional information serve as subversive substrates in redox cycling activity: 3,3'-[polyaminobis(carbonylalkyl)]bis(1,4-naphthoquinone) derivatives, inhibitory and substrate activity depending on spacer length Trypanosoma cruzi ?
-
?
trypanothione disulfide + NADPH
-
Trypanosoma brucei trypanothione + NADP+
-
?
trypanothione disulfide + NADPH
-
Leishmania donovani trypanothione + NADP+
-
?
trypanothione disulfide + NADPH
-
Leishmania infantum trypanothione + NADP+
-
?
trypanothione disulfide + NADPH
-
Trypanosoma cruzi trypanothione + NADP+
-
?

Synonyms

Synonyms Comment Organism
TR
-
Leishmania donovani
TR
-
Trypanosoma cruzi

Cofactor

Cofactor Comment Organism Structure
FAD
-
Trypanosoma brucei
FAD
-
Leishmania donovani
FAD
-
Leishmania infantum
FAD
-
Trypanosoma cruzi
NADPH
-
Trypanosoma brucei
NADPH
-
Leishmania donovani
NADPH
-
Leishmania infantum
NADPH
-
Trypanosoma cruzi