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Literature summary for 2.7.4.4 extracted from

  • El Amri, C.; Martin, A.; Vasseur, J.; Smietana, M.
    Borononucleotides as substrates/binders for human NMP kinases: Enzymatic and spectroscopic evaluation (2012), ChemBioChem, 13, 1605-1612.
    View publication on PubMed
Search for more literature for 2.7.4.4

Inhibitors

Inhibitors Comment Organism Structure
(E)-1-(5'-deoxy-thymidin-5'-yl)-vinyl boronic acid about 30% inhibition at 1 mM Homo sapiens
3-(thymin-1-yl)propylboronic acid about 10% inhibition at 1 mM Homo sapiens
[(E)-2-[(2R,3S,5R)-5-(6-amino-9H-purin-9-yl)-3-hydroxytetrahydrofuran-2-yl]ethenyl]boronic acid about 15% inhibition at 1 mM Homo sapiens
[2-[(2R,3S,5R)-3-hydroxy-5-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-2-yl]ethyl]boronic acid about 45% inhibition at 1 mM Homo sapiens
[2-[(2R,3S,5R)-5-(2-amino-6-oxo-1,6-dihydro-9H-purin-9-yl)-3-hydroxytetrahydrofuran-2-yl]ethyl]boronic acid about 25% inhibition at 1 mM Homo sapiens
[2-[(2R,3S,5R)-5-(4-amino-2-oxopyrimidin-1(2H)-yl)-3-hydroxytetrahydrofuran-2-yl]ethyl]boronic acid about 55% inhibition at 1 mM Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.119
-
 [2-[(2R,3S,5R)-3-hydroxy-5-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-2-yl]ethyl]boronic acid in Tris-HCl (50 mM, pH 7.4), KCl (50 mM), MgCl2 (5 mM), at 37°C Homo sapiens
0.23
-
 TMP in Tris-HCl (50 mM, pH 7.4), KCl (50 mM), MgCl2 (5 mM), at 37°C Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + TMP
-
 Homo sapiens ADP + TDP
-
 ?
ATP + [2-[(2R,3S,5R)-3-hydroxy-5-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-2-yl]ethyl]boronic acid
-
 Homo sapiens ADP + (2-((2R,3S,5R)-3-hydroxy-5-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-2-yl)ethyl)boronic phosphoric anhydride
-
 ?
additional information no activity with 3-(thymin-1-yl)propylboronic acid, (E)-3-(thymin-1-yl)prop-1-enylboronic acid, and (E)-1-(5'-deoxy-thymidin-5'-yl)-vinyl boronic acid Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
NMP kinase
-
 Homo sapiens
thymidylate kinase
-
 Homo sapiens
TMPK
-
 Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.014
-
 [2-[(2R,3S,5R)-3-hydroxy-5-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-2-yl]ethyl]boronic acid in Tris-HCl (50 mM, pH 7.4), KCl (50 mM), MgCl2 (5 mM), at 37°C Homo sapiens
1.25
-
 TMP in Tris-HCl (50 mM, pH 7.4), KCl (50 mM), MgCl2 (5 mM), at 37°C Homo sapiens

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
0.139
-
 [2-[(2R,3S,5R)-3-hydroxy-5-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-2-yl]ethyl]boronic acid in Tris-HCl (50 mM, pH 7.4), KCl (50 mM), MgCl2 (5 mM), at 37°C Homo sapiens
5400
-
 TMP in Tris-HCl (50 mM, pH 7.4), KCl (50 mM), MgCl2 (5 mM), at 37°C Homo sapiens