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Literature summary for 1.8.1.12 extracted from

  • Hamilton, C.J.; Saravanamuthu, A.; Fairlamb, A.H.; Eggleston, I.M.
    Benzofuranyl 3,5-bis-polyamine derivatives as time-dependent inhibitors of trypanothione reductase (2003), Bioorg. Med. Chem., 11, 3683-3693.
    View publication on PubMed
Search for more literature for 1.8.1.12

Inhibitors

Inhibitors Comment Organism Structure
bis(tetrahydrocinnamoyl)spermine i.e. kukoamine A Trypanosoma cruzi
lunarine Lunaria derived alkaloid with a unusual 3-oxohexahydrodibenzofuranyl tricyclic scaffold, competitive, reversible formation of a covalent adduct between Cys53 and one of the alpha,beta-unsaturated amide groups of lunarine, mechanism, enzyme needs to be in reduced state Trypanosoma cruzi
N-(3-dimethylamino-propyl)-O-[(E)-3-(3-[(E)-3-[N-(3-dimethylamino-propyl)aminooxy]-propenyl]-benzofuran-5-yl)-allyl]-hydroxylamine benzofuranyl-based acyclic bis-polyamine analogue of lunarine with a planar bicyclic benzofuranyl scaffold, inhibition mechanism Trypanosoma cruzi
N-[3-(4-amino-butylamino)-propyl]-O-[(E)-3-[3-((E)-3-[N-[3-(4-amino-butylamino)-propyl]aminooxy]-propenyl)-benzofuran-5-yl]-allyl]-hydroxylamine benzofuranyl-based acyclic bis-polyamine analogue of lunarine with a planar bicyclic benzofuranyl scaffold, inhibition mechanism Trypanosoma cruzi
N-[3-(4-methyl-piperazin-1-yl)-propyl]-O-[(E)-3-[3-((E)-3-[N-[3-(4-methyl-piperazin-1-yl)-propyl]aminooxy]-propenyl)-benzofuran-5-yl]-allyl]-hydroxylamine benzofuranyl-based acyclic bis-polyamine analogue of lunarine with a planar bicyclic benzofuranyl scaffold, inhibition mechanism Trypanosoma cruzi

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Trypanosoma cruzi enzyme is required for maintaining the reducing intracellular environment ?
-
 ?
trypanothione disulfide + NADPH Trypanosoma cruzi
-
 trypanothione + NADP+
-
 ?

Organism

Organism UniProt Comment Textmining
Trypanosoma cruzi
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information enzyme is required for maintaining the reducing intracellular environment Trypanosoma cruzi ?
-
 ?
trypanothione disulfide + NADPH
-
 Trypanosoma cruzi trypanothione + NADP+
-
 ?

Synonyms

Synonyms Comment Organism
trypanothione reductase
-
 Trypanosoma cruzi
TryR
-
 Trypanosoma cruzi

Cofactor

Cofactor Comment Organism Structure
additional information enzyme is a flavoprotein Trypanosoma cruzi
NADPH dependent on Trypanosoma cruzi

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
 additional information inhibition kinetics Trypanosoma cruzi