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Literature summary extracted from

  • Hamilton, C.J.; Saravanamuthu, A.; Poupat, C.; Fairlamb, A.H.; Eggleston, I.M.
    Time-dependent inhibitors of trypanothione reductase: analogues of the spermidine alkaloid lunarine and related natural products (2006), Bioorg. Med. Chem., 14, 2266-2278.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.8.1.12 (+/-)-10,11-dihydrolunarine 0.1 mM Lunaria biennis
1.8.1.12 cis-3-(1,3-dioxolan-2-yl)-8-bromo-9b-(trans-acrylic acid)-1,2,3,4,4a,9b-hexahydrodibenzofuran 0.1 mM Lunaria biennis
1.8.1.12 cis-3-oxo-8,9b-bis-(trans-N-(acrylamidospermidyl))-1,2,3,4,4a,9b-hexahydrodibenzofuran IC50: 0.029 mM Lunaria biennis
1.8.1.12 cis-3-oxo-8,9b-bis-(trans-N3-(dimethylamino)propylacrylamido)-1,2,3,4,4a,9b-hexahydrodibenzofuran 0.1 mM Lunaria biennis
1.8.1.12 cis-3-oxo-8-trans-(N-acrylamidospermidyl)-9b-trans-ethylacrylyl-1,2,3,4,4a,9b-hexahydrodibenzofuran IC50: 0.056 mM Lunaria biennis
1.8.1.12 cis-3-oxo-8-trans-(N1-acrylamidospermidyl)-9b-trans-ethylacrylyl-1,2,3,4,4a,9b-hexahydrodibenzofuran
-
Lunaria biennis
1.8.1.12 lunarine IC50: 0.065 mM Lunaria biennis
1.8.1.12 lunarinol 0.1 mM Lunaria biennis
1.8.1.12 additional information no inhibition by 0.1 mM cis-3-(1,3-dioxolan-2-yl)-8,9b-bis-(trans-ethyl-acrylyl)-1,2,3,4,4a,9b-hexahydrodibenzofuran Lunaria biennis
1.8.1.12 numismine 0.1 mM Lunaria biennis
1.8.1.12 tetrahydrolunarine 0.1 mM Lunaria biennis
1.8.1.12 tetrahydrolunarinol 0.1 mM Lunaria biennis

Organism

EC Number Organism UniProt Comment Textmining
1.8.1.12 Lunaria biennis
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.8.1.12 trypanothione disulfide + NADPH
-
Lunaria biennis trypanothione + NADP+
-
?

Synonyms

EC Number Synonyms Comment Organism
1.8.1.12 EC 1.6.4.8 formerly Lunaria biennis
1.8.1.12 trypanothione reductase
-
Lunaria biennis
1.8.1.12 TryR
-
Lunaria biennis

Cofactor

EC Number Cofactor Comment Organism Structure
1.8.1.12 NADPH
-
Lunaria biennis

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.8.1.12 0.049
-
cis-3-oxo-8-trans-(N1-acrylamidospermidyl)-9b-trans-ethylacrylyl-1,2,3,4,4a,9b-hexahydrodibenzofuran
-
Lunaria biennis
1.8.1.12 0.059
-
cis-3-oxo-8,9b-bis-(trans-N1-(acrylamidospermidyl))-1,2,3,4,4a,9b-hexahydrodibenzofuran
-
Lunaria biennis
1.8.1.12 0.079
-
(+/-)-10,11-dihydrolunarine
-
Lunaria biennis
1.8.1.12 0.093
-
cis-3-oxo-8,9b-bis-(trans-N3-(dimethylamino)propylacrylamido)-1,2,3,4,4a,9b-hexahydrodibenzofuran
-
Lunaria biennis
1.8.1.12 0.096
-
tetrahydrolunarine
-
Lunaria biennis
1.8.1.12 0.101
-
cis-3-(1,3-dioxolan-2-yl)-8-bromo-9b-(trans-acrylic acid)-1,2,3,4,4a,9b-hexahydrodibenzofuran
-
Lunaria biennis
1.8.1.12 0.16
-
numismine
-
Lunaria biennis
1.8.1.12 0.218
-
tetrahydrolunarinol
-
Lunaria biennis
1.8.1.12 0.304
-
lunarine
-
Lunaria biennis
1.8.1.12 0.47
-
lunarinol
-
Lunaria biennis

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.8.1.12 0.029
-
IC50: 0.029 mM Lunaria biennis cis-3-oxo-8,9b-bis-(trans-N-(acrylamidospermidyl))-1,2,3,4,4a,9b-hexahydrodibenzofuran
1.8.1.12 0.056
-
IC50: 0.056 mM Lunaria biennis cis-3-oxo-8-trans-(N-acrylamidospermidyl)-9b-trans-ethylacrylyl-1,2,3,4,4a,9b-hexahydrodibenzofuran
1.8.1.12 0.065
-
IC50: 0.065 mM Lunaria biennis lunarine