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Literature summary extracted from

  • Agarwal, H.K.; McElroy, C.A.; Sjuvarsson, E.; Eriksson, S.; Darby, M.V.; Tjarks, W.
    Synthesis of N3-substituted carboranyl thymidine bioconjugates and their evaluation as substrates of recombinant human thymidine kinase 1 (2013), Eur. J. Med. Chem., 60, 456-468.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.1.21 expressed in Escherichia coli BL21(DE3)pLysS cells Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.7.1.21 0.0049
-
 thymidine in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37°C Homo sapiens
2.7.1.21 0.0174
-
 3-[1(2)-closo-1,7-carboranylbutyltetrazol-5-yl]thymidine in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37°C Homo sapiens
2.7.1.21 0.0318
-
 3-[1(2)-closo-1,7-carboranylethyltetrazol-5-ylmethyl]thymidine in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37°C Homo sapiens
2.7.1.21 0.0356
-
 3-[1(2)-closo-1,7-carboranylethyltetrazol-5-yl]thymidine in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37°C Homo sapiens
2.7.1.21 0.0373
-
 3-[1(2)-propyltetrazol-5-ylmethyl]thymidine in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37°C Homo sapiens
2.7.1.21 0.0552
-
 3-[1(2)-closo-1,7-carboranylpropyltetrazol-5-ylmethyl]thymidine in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37°C Homo sapiens
2.7.1.21 0.0552
-
 3-[1(2)-propyltetrazol-5-yl]thymidine in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37°C Homo sapiens
2.7.1.21 0.0563
-
 3-[1(2)-closo-1,7-carboranylbutyltetrazol-5-ylmethyl]thymidine in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37°C Homo sapiens
2.7.1.21 0.0799
-
 3-[1(2)-closo-1,7-carboranylpropyltetrazol-5-yl]thymidine in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37°C Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
2.7.1.21 Homo sapiens
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.1.21 ATP + 3-(benzylcarbamimidoyl)thymidine 14.9% activity compared to thymidine Homo sapiens ADP + 3-(benzylcarbamimidoyl)thymidine 5'-phosphate
-
 ?
2.7.1.21 ATP + 3-(butylcarbamimidoyl)thymidine 1.2% activity compared to thymidine Homo sapiens ADP + 3-(butylcarbamimidoyl)thymidine 5'-phosphate
-
 ?
2.7.1.21 ATP + 3-(phenylcarbamimidoyl)thymidine 1.9% activity compared to thymidine Homo sapiens ADP + 3-(phenylcarbamimidoyl)thymidine 5'-phosphate
-
 ?
2.7.1.21 ATP + 3-(tetrazol-5-ylmethyl)thymidine 39.5% activity compared to thymidine Homo sapiens ADP + 3-(tetrazol-5-ylmethyl)thymidine 5'-phosphate
-
 ?
2.7.1.21 ATP + 3-[1(2)-closo-1,7-carboranylbutyltetrazol-5-ylmethyl]thymidine 63.7% activity compared to thymidine Homo sapiens ADP + 3-[1(2)-closo-1,7-carboranylbutyltetrazol-5-ylmethyl]thymidine 5'-phosphate
-
 ?
2.7.1.21 ATP + 3-[1(2)-closo-1,7-carboranylbutyltetrazol-5-yl]thymidine 42.5% activity compared to thymidine Homo sapiens ADP + 3-[1(2)-closo-1,7-carboranylbutyltetrazol-5-yl]thymidine 5'-phosphate
-
 ?
2.7.1.21 ATP + 3-[1(2)-closo-1,7-carboranylethyltetrazol-5-ylmethyl]thymidine 52.4% activity compared to thymidine Homo sapiens ADP + 3-[1(2)-closo-1,7-carboranylethyltetrazol-5-ylmethyl]thymidine 5'-phosphate
-
 ?
2.7.1.21 ATP + 3-[1(2)-closo-1,7-carboranylethyltetrazol-5-yl]thymidine 55.6% activity compared to thymidine Homo sapiens ADP + 3-[1(2)-closo-1,7-carboranylethyltetrazol-5-yl]thymidine 5'-phosphate
-
 ?
2.7.1.21 ATP + 3-[1(2)-closo-1,7-carboranylpropyltetrazol-5-ylmethyl]thymidine 58.2% activity compared to thymidine Homo sapiens ADP + 3-[1(2)-closo-1,7-carboranylpropyltetrazol-5-ylmethyl]thymidine 5'-phosphate
-
 ?
2.7.1.21 ATP + 3-[1(2)-closo-1,7-carboranylpropyltetrazol-5-yl]thymidine 42.9% activity compared to thymidine Homo sapiens ADP + 3-[1(2)-closo-1,7-carboranylpropyltetrazol-5-yl]thymidine 5'-phosphate
-
 ?
2.7.1.21 ATP + 3-[1(2)-propyltetrazol-5-ylmethyl]thymidine 55.7% activity compared to thymidine Homo sapiens ADP + 3-[1(2)-propyltetrazol-5-ylmethyl]thymidine 5'-phosphate
-
 ?
2.7.1.21 ATP + 3-[1(2)-propyltetrazol-5-yl]thymidine 57.6% activity compared to thymidine Homo sapiens ADP + 3-[1(2)-propyltetrazol-5-yl]thymidine 5'-phosphate
-
 ?
2.7.1.21 ATP + 3-[2-(closo-1,7-carboranyl)ethylcarbamimidoyl]thymidine 16.3% activity compared to thymidine Homo sapiens ADP + 3-[2-(closo-1,7-carboranyl)ethylcarbamimidoyl]thymidine 5'-phosphate
-
 ?
2.7.1.21 ATP + 3-[2-imino-2-(benzylamino)ethyl]thymidine 16.8% activity compared to thymidine Homo sapiens ADP + 3-[2-imino-2-(benzylamino)ethyl]thymidine 5'-phosphate
-
 ?
2.7.1.21 ATP + 3-[2-imino-2-(butylamino)ethyl]thymidine 2.3% activity compared to thymidine Homo sapiens ADP + 3-[2-imino-2-(butylamino)ethyl]thymidine 5'-phosphate
-
 ?
2.7.1.21 ATP + 3-[2-imino-2-(phenylamino)ethyl]thymidine 11.3% activity compared to thymidine Homo sapiens ADP + 3-[2-imino-2-(phenylamino)ethyl]thymidine 5'-phosphate
-
 ?
2.7.1.21 ATP + 3-[2-imino-2-(propylamino)ethyl]thymidine 1.9% activity compared to thymidine Homo sapiens ADP + 3-[2-imino-2-(propylamino)ethyl]thymidine 5'-phosphate
-
 ?
2.7.1.21 ATP + 3-[2-imino-2-[2-(closo-1,7-carboranyl)ethylamino]ethyl]thymidine 3.0% activity compared to thymidine Homo sapiens ADP + 3-[2-imino-2-[2-(closo-1,7-carboranyl)ethylamino]ethyl]thymidine 5'-phosphate
-
 ?
2.7.1.21 ATP + 3-[2-imino-2-[2-(closo-1,7-carboranyl)propylamino]ethyl]thymidine 5.6% activity compared to thymidine Homo sapiens ADP + 3-[2-imino-2-[2-(closo-1,7-carboranyl)propylamino]ethyl]thymidine 5'-phosphate
-
 ?
2.7.1.21 ATP + 3-[3-(closo-1,7-carboranyl)propylcarbamimidoyl]thymidine 15.5% activity compared to thymidine Homo sapiens ADP + 3-[3-(closo-1,7-carboranyl)propylcarbamimidoyl]thymidine 5'-phosphate
-
 ?
2.7.1.21 ATP + 3-[4-(closo-1,7-carboranyl)butylcarbamimidoyl]thymidine 27.3% activity compared to thymidine Homo sapiens ADP + 3-[4-(closo-1,7-carboranyl)butylcarbamimidoyl]thymidine 5'-phosphate
-
 ?
2.7.1.21 ATP + thymidine 100% activity Homo sapiens ADP + dTMP
-
 ?
2.7.1.21 additional information no activity with 3-(propylcarbamimidoyl)thymidine and 3-(tetrazol-5-yl)thymidine Homo sapiens ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.1.21 thymidine kinase 1
-
 Homo sapiens
2.7.1.21 TK1
-
 Homo sapiens

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2.7.1.21 0.32
-
 3-[1(2)-closo-1,7-carboranylbutyltetrazol-5-yl]thymidine in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37°C Homo sapiens
2.7.1.21 0.34
-
 3-[1(2)-propyltetrazol-5-yl]thymidine in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37°C Homo sapiens
2.7.1.21 0.35
-
 3-[1(2)-closo-1,7-carboranylethyltetrazol-5-yl]thymidine in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37°C Homo sapiens
2.7.1.21 0.37
-
 3-[1(2)-closo-1,7-carboranylpropyltetrazol-5-yl]thymidine in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37°C Homo sapiens
2.7.1.21 0.39
-
 3-[1(2)-closo-1,7-carboranylpropyltetrazol-5-ylmethyl]thymidine in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37°C Homo sapiens
2.7.1.21 0.44
-
 3-[1(2)-closo-1,7-carboranylethyltetrazol-5-ylmethyl]thymidine in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37°C Homo sapiens
2.7.1.21 0.45
-
 3-[1(2)-propyltetrazol-5-ylmethyl]thymidine in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37°C Homo sapiens
2.7.1.21 0.46
-
 thymidine in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37°C Homo sapiens
2.7.1.21 0.47
-
 3-[1(2)-closo-1,7-carboranylbutyltetrazol-5-ylmethyl]thymidine in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37°C Homo sapiens