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Literature summary for 2.7.4.9 extracted from

  • Topalis, D.; Pradere, U.; Roy, V.; Caillat, C.; Azzouzi, A.; Broggi, J.; Snoeck, R.; Andrei, G.; Lin, J.; Eriksson, S.; Alexandre, J.A.; El-Amri, C.; Deville-Bonne, D.; Meyer, P.; Balzarini, J.; Agrofoglio, L.A.
    Novel antiviral C5-substituted pyrimidine acyclic nucleoside phosphonates selected as human thymidylate kinase substrates (2011), J. Med. Chem., 54, 222-232.
    View publication on PubMed
Search for more literature for 2.7.4.9

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with phosphorylated N1-[(E)-4-dihydroxyphosphonyl-but-2-enyl]-thymine and ADP, vapor diffusion method, using 14% (w/v) PEG 3350, 0.1 M HEPES pH 7.5, at 20°C Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.01
-
 5-bromo-dUMP at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
0.02
-
 dTMP at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
0.02
-
 N1-[(E)-4-dihydroxyphosphonyl-but-2-enyl]-5-chlorouracil at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
0.024
-
 N1-[(E)-4-dihydroxyphosphonyl-but-2-enyl]-thymine at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
0.1
-
 N1-[(E)-5-dihydroxyphosphonyl-pent-2-enyl]-thymine at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
0.13
-
 N1-[(E)-4-dihydroxyphosphonyl-but-2-enyl]-5-chlorouracil at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
0.15
-
 N1-[(E)-5-dihydroxyphosphonyl-pent-2-enyl]-5-chlorouracil at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
0.16
-
 N1-[(E)-5-dihydroxyphosphonyl-pent-2-enyl]-5-bromouracil at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
0.17
-
 dUMP at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
1
-
 N1-[(E)-3-dihydroxyphosphonyl-prop-2-enyl]-thymine at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
1
-
 N1-[(E)-4-dihydroxyphosphonyl-but-2-enyl]-5-fluorouracil at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
1.7
-
 N1-[(E)-4-dihydroxyphosphonyl-but-2-enyl]-uracil at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
1.9
-
 N1-[(E)-5-dihydroxyphosphonyl-pent-2-enyl]-5-fluorouracil at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
2.5
-
 N1-[(E)-5-dihydroxyphosphonyl-pent-2-enyl]-uracil at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + dTMP Homo sapiens
-
 ADP + dTDP
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens P23919
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + 3'-azido-2',3'-dideoxythymidine monophosphate
-
 Homo sapiens ADP + 3'-azido-2',3'-dideoxythymidine diphosphate
-
 ?
ATP + 5-bromo-dUMP
-
 Homo sapiens ADP + 5-bromo-dUDP
-
 ?
ATP + dTMP
-
 Homo sapiens ADP + dTDP
-
 ?
ATP + dUMP
-
 Homo sapiens ADP + dUDP
-
 ?
ATP + N1-[(E)-3-dihydroxyphosphonyl-prop-2-enyl]-thymine
-
 Homo sapiens ADP + ?
-
 ?
ATP + N1-[(E)-4-dihydroxyphosphonyl-but-2-enyl]-5-chlorouracil
-
 Homo sapiens ADP + ?
-
 ?
ATP + N1-[(E)-4-dihydroxyphosphonyl-but-2-enyl]-5-fluorouracil
-
 Homo sapiens ADP + ?
-
 ?
ATP + N1-[(E)-4-dihydroxyphosphonyl-but-2-enyl]-thymine
-
 Homo sapiens ADP + ?
-
 ?
ATP + N1-[(E)-4-dihydroxyphosphonyl-but-2-enyl]-uracil
-
 Homo sapiens ADP + ?
-
 ?
ATP + N1-[(E)-5-dihydroxyphosphonyl-pent-2-enyl]-5-bromouracil
-
 Homo sapiens ADP + ?
-
 ?
ATP + N1-[(E)-5-dihydroxyphosphonyl-pent-2-enyl]-5-chlorouracil
-
 Homo sapiens ADP + ?
-
 ?
ATP + N1-[(E)-5-dihydroxyphosphonyl-pent-2-enyl]-5-fluorouracil
-
 Homo sapiens ADP + ?
-
 ?
ATP + N1-[(E)-5-dihydroxyphosphonyl-pent-2-enyl]-thymine
-
 Homo sapiens ADP + ?
-
 ?
ATP + N1-[(E)-5-dihydroxyphosphonyl-pent-2-enyl]-uracil
-
 Homo sapiens ADP + ?
-
 ?
additional information no activity with cidofovir, N1-[(E)-3-dihydroxyphosphonyl-prop-2-enyl]-uracil, N1-[(E)-3-dihydroxyphosphonyl-prop-2-enyl]-5-chlorouracil, N1-[(E)-3-dihydroxyphosphonyl-prop-2-enyl]-5-bromouracil, N1-[(E)-3-dihydroxyphosphonyl-prop-2-enyl]-5-fluoro-uracil, and N1-[(E)-3-dihydroxyphosphonyl-prop-2-enyl]-thymine Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
thymidine monophosphate kinase
-
 Homo sapiens
thymidylate kinase
-
 Homo sapiens
TMP kinase
-
 Homo sapiens
TMPK
-
 Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.058
-
 N1-[(E)-5-dihydroxyphosphonyl-pent-2-enyl]-5-bromouracil at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
0.074
-
 N1-[(E)-5-dihydroxyphosphonyl-pent-2-enyl]-uracil at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
0.09
-
 N1-[(E)-5-dihydroxyphosphonyl-pent-2-enyl]-5-fluorouracil at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
0.1
-
 N1-[(E)-5-dihydroxyphosphonyl-pent-2-enyl]-5-chlorouracil at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
0.32
-
 N1-[(E)-5-dihydroxyphosphonyl-pent-2-enyl]-thymine at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
0.48
-
 N1-[(E)-4-dihydroxyphosphonyl-but-2-enyl]-uracil at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
0.5
-
 N1-[(E)-4-dihydroxyphosphonyl-but-2-enyl]-5-chlorouracil at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
0.6
-
 N1-[(E)-3-dihydroxyphosphonyl-prop-2-enyl]-thymine at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
0.73
-
 N1-[(E)-4-dihydroxyphosphonyl-but-2-enyl]-5-fluorouracil at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
0.84
-
 N1-[(E)-4-dihydroxyphosphonyl-but-2-enyl]-thymine at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
0.9
-
 N1-[(E)-4-dihydroxyphosphonyl-but-2-enyl]-5-chlorouracil at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
1.2
-
 5-bromo-dUMP at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
3
-
 dTMP at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
4.8
-
 dUMP at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
0.03
-
 N1-[(E)-5-dihydroxyphosphonyl-pent-2-enyl]-uracil at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
0.047
-
 N1-[(E)-5-dihydroxyphosphonyl-pent-2-enyl]-5-fluorouracil at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
0.28
-
 N1-[(E)-4-dihydroxyphosphonyl-but-2-enyl]-uracil at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
0.36
-
 N1-[(E)-5-dihydroxyphosphonyl-pent-2-enyl]-5-bromouracil at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
0.6
-
 N1-[(E)-3-dihydroxyphosphonyl-prop-2-enyl]-thymine at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
0.66
-
 N1-[(E)-5-dihydroxyphosphonyl-pent-2-enyl]-5-chlorouracil at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
0.73
-
 N1-[(E)-4-dihydroxyphosphonyl-but-2-enyl]-5-fluorouracil at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
3.2
-
 N1-[(E)-5-dihydroxyphosphonyl-pent-2-enyl]-thymine at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
4.1
-
 N1-[(E)-4-dihydroxyphosphonyl-but-2-enyl]-5-chlorouracil at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
28
-
 dUMP at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
35
-
 N1-[(E)-4-dihydroxyphosphonyl-but-2-enyl]-thymine at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
45
-
 N1-[(E)-4-dihydroxyphosphonyl-but-2-enyl]-5-chlorouracil at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
120
-
 5-bromo-dUMP at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens
150
-
 dTMP at 37°C in 50 mM Tris-HCl, pH 7.4, containing 50 mM KCl and 5 mM MgCl2 Homo sapiens