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Literature summary extracted from

  • Felczak, K.; Miazga, A.; Poznanski, J.; Bretner, M.; Kulikowski, T.; Dzik, J.M.; Golos, B.; Zielinski, Z.; Ciesla, J.; Rode, W.
    5-Substituted N4-hydroxy-2'-deoxycytidines and their 5'-monophosphates: Synthesis, conformation, interaction with tumor thymidylate synthase, and in vitro antitumor activity (2000), J. Med. Chem., 43, 4647-4656.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.1.1.45
-
 Rattus norvegicus

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.1.1.45 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-bromopyrimidin-2(1H)-one 5'-monophosphate
-
 Mus musculus
2.1.1.45 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-chloropyrimidin-2(1H)-one 5'-monophosphate
-
 Mus musculus
2.1.1.45 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-fluoropyrimidin-2(1H)-one 5'-monophosphate
-
 Mus musculus
2.1.1.45 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-hydroxymethylpyrimidin-2(1H)-one 5'-monophosphate
-
 Mus musculus
2.1.1.45 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-iodopyrimidin-2(1H)-one 5'-monophosphate
-
 Mus musculus
2.1.1.45 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyaminopyrimidin-2(1H)-one 5'-monophosphate
-
 Mus musculus
2.1.1.45 5-bromo-N4-hydroxy-2'-deoxycytidine
-
 Mus musculus
2.1.1.45 5-chloro-N4-hydroxy-2'-deoxycytidine
-
 Mus musculus
2.1.1.45 5-fluoro-2'-deoxyuridylic acid
-
 Mus musculus
2.1.1.45 bromo-2'-deoxyuridine
-
 Mus musculus
2.1.1.45 chloro-2'-deoxyuridine
-
 Mus musculus
2.1.1.45 hydroxymethyl-2'-deoxyuridine
-
 Mus musculus
2.1.1.45 iodo-2'-deoxyuridine
-
 Mus musculus
2.1.1.45 N4-hydroxy-2'-deoxycytidine
-
 Mus musculus
2.1.1.45 N4-hydroxy-5-methyl-2'-deoxycytidine
-
 Mus musculus
2.1.1.45 thymidine phosphate
-
 Mus musculus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP Mus musculus
-
 dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP Rattus norvegicus
-
 dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP Lacticaseibacillus casei
-
 dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP Trichinella spiralis
-
 dihydrofolate + dTMP
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.1.1.45 Lacticaseibacillus casei
-
-
-
2.1.1.45 Mus musculus
-
 L5178 murine leukemia cell line
-
2.1.1.45 Rattus norvegicus
-
-
-
2.1.1.45 Trichinella spiralis
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.1.1.45 liver
-
 Mus musculus
-
2.1.1.45 liver
-
 Rattus norvegicus
-

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
2.1.1.45 0.6
-
-
 Rattus norvegicus

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Mus musculus dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Mus musculus dihydrofolate + dTMP
-
 r
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Rattus norvegicus dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Rattus norvegicus dihydrofolate + dTMP
-
 r
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Lacticaseibacillus casei dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Lacticaseibacillus casei dihydrofolate + dTMP
-
 r
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Trichinella spiralis dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Trichinella spiralis dihydrofolate + dTMP
-
 r
2.1.1.45 5-bromo-2'-deoxyuridine 5'-monophosphate + ? dehalogenation Mus musculus ?
-
 ?
2.1.1.45 5-bromo-2'-deoxyuridine 5'-monophosphate + ? dehalogenation Lacticaseibacillus casei ?
-
 ?
2.1.1.45 5-bromo-2'-deoxyuridine 5'-monophosphate + ? dehalogenated by recombinant rat hepatoma enzyme Rattus norvegicus ?
-
 ?
2.1.1.45 5-iodo-2'-deoxyuridine 5'-monophosphate + ? dehalogenation Mus musculus ?
-
 ?
2.1.1.45 5-iodo-2'-deoxyuridine 5'-monophosphate + ? dehalogenated by recombinant rat hepatoma enzyme Rattus norvegicus ?
-
 ?

Cofactor

EC Number Cofactor Comment Organism Structure
2.1.1.45 N5,N10-methylenetetrahydrofolate
-
 Mus musculus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.1.1.45 0.00002
-
 5-fluoro-2'-deoxyuridylic acid L1210 parental enzyme Mus musculus
2.1.1.45 0.0003
-
 chloro-2'-deoxyuridine L1210 parental enzyme Mus musculus
2.1.1.45 0.0008
-
 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-fluoropyrimidin-2(1H)-one 5'-monophosphate L1210 parental enzyme Mus musculus
2.1.1.45 0.0013
-
 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-hydroxymethylpyrimidin-2(1H)-one 5'-monophosphate L1210 recombinant enzyme Mus musculus
2.1.1.45 0.0014
-
 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-fluoropyrimidin-2(1H)-one 5'-monophosphate L1210 recombinant enzyme Mus musculus
2.1.1.45 0.0015
-
 bromo-2'-deoxyuridine L1210 parental enzyme Mus musculus
2.1.1.45 0.0017
-
 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyaminopyrimidin-2(1H)-one 5'-monophosphate L1210 parental enzyme Mus musculus
2.1.1.45 0.00191
-
 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-hydroxymethylpyrimidin-2(1H)-one 5'-monophosphate L1210 parental enzyme Mus musculus
2.1.1.45 0.0034
-
 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-iodopyrimidin-2(1H)-one 5'-monophosphate L1210 recombinant enzyme Mus musculus
2.1.1.45 0.0037
-
 hydroxymethyl-2'-deoxyuridine L1210 parental enzyme Mus musculus
2.1.1.45 0.0049
-
 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-chloropyrimidin-2(1H)-one 5'-monophosphate L1210 recombinant enzyme Mus musculus
2.1.1.45 0.0073
-
 thymidine phosphate L1210 parental enzyme Mus musculus
2.1.1.45 0.00746
-
 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-iodopyrimidin-2(1H)-one 5'-monophosphate L1210 parental enzyme Mus musculus
2.1.1.45 0.00768
-
 iodo-2'-deoxyuridine L1210 parental enzyme Mus musculus
2.1.1.45 0.0085
-
 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-chloropyrimidin-2(1H)-one 5'-monophosphate L1210 parental enzyme Mus musculus
2.1.1.45 0.0093
-
 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyaminopyrimidin-2(1H)-one 5'-monophosphate L1210 recombinant enzyme Mus musculus
2.1.1.45 0.022
-
 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-bromopyrimidin-2(1H)-one 5'-monophosphate L1210 recombinant enzyme Mus musculus
2.1.1.45 0.0321
-
 1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-bromopyrimidin-2(1H)-one 5'-monophosphate L1210 parental enzyme Mus musculus