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Literature summary for 1.8.1.9 extracted from

  • Lo, Y.C.; Ko, T.P.; Su, W.C.; Su, T.L.; Wang, A.H.
    Terpyridine-platinum(II) complexes are effective inhibitors of mammalian topoisomerases and human thioredoxin reductase 1 (2009), J. Inorg. Biochem., 103, 1082-1092.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with FAD, NADPH and/or (N-acetyl-4-aminothiophenolato)(2,2':6',2''-terpyridine)platinum(II) chloride, sitting drop vapor diffusion method, using 5 mM MgSO4, 5% (w/v) PEG 3350, 50 mM MES pH 6.0 and 20% (w/v) 1,6-hexanediol Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(4-ammoniothiophenolato)(2,2':6',2''-terpyridine)platinum(II) chloride
-
Homo sapiens
(4-ammoniothiophenolato)(4'-toyl-2,2':6',2''-terpyridine)platinum(II) nitrate
-
Homo sapiens
(4-hydroxylthiophenolato)(2,2':6',2''-terpyridine)platinum(II) chloride
-
Homo sapiens
(4-hydroxylthiophenolato)(4'-toyl-2,2':6',2''-terpyridine)platinum(II) chloride
-
Homo sapiens
(N-acetyl-4-aminothiophenolato)(2,2':6',2''-terpyridine)platinum(II) chloride
-
Homo sapiens
(N-acetyl-4-aminothiophenolato)(4'-toyl-2,2':6',2''-terpyridine)platinum(II) nitrate
-
Homo sapiens
cisplatin
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q16881
-
-

Purification (Commentary)

Purification (Comment) Organism
Ni2+ affinity column chromatography Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
HeLa cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5,5'-dithiobis(2-nitrobenzoic acid) + NADPH + H+
-
Homo sapiens 2-nitro-5-thiobenzoate + NADP+
-
?

Synonyms

Synonyms Comment Organism
thioredoxin reductase 1
-
Homo sapiens
TrxR1
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
FAD
-
Homo sapiens
NADPH
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00005826
-
in 50 mM Tris-HCl, pH 8.0, at 37°C Homo sapiens (4-hydroxylthiophenolato)(4'-toyl-2,2':6',2''-terpyridine)platinum(II) chloride
0.00006977
-
in 50 mM Tris-HCl, pH 8.0, at 37°C Homo sapiens (4-hydroxylthiophenolato)(2,2':6',2''-terpyridine)platinum(II) chloride
0.00007002
-
in 50 mM Tris-HCl, pH 8.0, at 37°C Homo sapiens (4-ammoniothiophenolato)(4'-toyl-2,2':6',2''-terpyridine)platinum(II) nitrate
0.00007426
-
in 50 mM Tris-HCl, pH 8.0, at 37°C Homo sapiens (N-acetyl-4-aminothiophenolato)(2,2':6',2''-terpyridine)platinum(II) chloride
0.00007442
-
in 50 mM Tris-HCl, pH 8.0, at 37°C Homo sapiens (4-ammoniothiophenolato)(2,2':6',2''-terpyridine)platinum(II) chloride
0.00007786
-
in 50 mM Tris-HCl, pH 8.0, at 37°C Homo sapiens (N-acetyl-4-aminothiophenolato)(4'-toyl-2,2':6',2''-terpyridine)platinum(II) nitrate