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Literature summary for 2.7.4.9 extracted from

  • Van Daele, I.; Munier-Lehmann, H.; Hendrickx, P.M.; Marchal, G.; Chavarot, P.; Froeyen, M.; Qing, L.; Martins, J.C.; Van Calenbergh, S.
    Synthesis and biological evaluation of bicyclic nucleosides as inhibitors of M. tuberculosis thymidylate kinase (2006), ChemMedChem, 1, 1081-1090.
    View publication on PubMed
Search for more literature for 2.7.4.9

Application

Application Comment Organism
additional information Mycobacterium tuberculosis thymidine monophosphate kinase (TMPKmt) recently emerged as a potentially attractive target for the design of a novel class of antituberculosis agents. Mycobacterium tuberculosis variant bovis

Inhibitors

Inhibitors Comment Organism Structure
1-(3-amino-3-deoxy-2-O,3-N-(thiocarbonyl)-beta-D-ribofuranosyl)thymine IC99: 500 microg/ml Mycobacterium tuberculosis variant bovis
1-(3-aminomethyl-3,5-dideoxy-2-O,6-N-(thiocarbonyl)-beta-D-ribofuranosyl)thymine IC99: 100 microg/ml Mycobacterium tuberculosis variant bovis
1-[3-aminomethyl-3,5-dideoxy-2-O,6-N-(thiocarbonyl)-beta-D-ribofuranosyl]thymine
-
 Mycobacterium tuberculosis

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
dTMP + ATP Mycobacterium tuberculosis variant bovis TMPK catalyzes the conversion of dTMP to dTDP, using ATP as its preferred phosphoryl donor. Part of the biosynthetic pathway for deoxythymidine triphosphate (dTTP). dTDP + ADP
-
 ?

Organism

Organism UniProt Comment Textmining
Mycobacterium tuberculosis
-
-
-
Mycobacterium tuberculosis variant bovis
-
 BCG
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
dTMP + ATP TMPK catalyzes the conversion of dTMP to dTDP, using ATP as its preferred phosphoryl donor. Part of the biosynthetic pathway for deoxythymidine triphosphate (dTTP). Mycobacterium tuberculosis variant bovis dTDP + ADP
-
 ?

Synonyms

Synonyms Comment Organism
thymidylate kinase
-
 Mycobacterium tuberculosis
thymidylate kinase
-
 Mycobacterium tuberculosis variant bovis
TMPKmt
-
 Mycobacterium tuberculosis
TMPKmt
-
 Mycobacterium tuberculosis variant bovis

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0023
-
 1-[3-aminomethyl-3,5-dideoxy-2-O,6-N-(thiocarbonyl)-beta-D-ribofuranosyl]thymine
-
 Mycobacterium tuberculosis
0.0023
-
 1-(3-aminomethyl-3,5-dideoxy-2-O,6-N-(thiocarbonyl)-beta-D-ribofuranosyl)thymine
-
 Mycobacterium tuberculosis variant bovis
0.008
-
 1-(3-amino-3-deoxy-2-O,3-N-(thiocarbonyl)-beta-D-ribofuranosyl)thymine
-
 Mycobacterium tuberculosis variant bovis