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Literature summary extracted from

  • Haouz, A.; Vanheusden, V.; Munier-Lehmann, H.; Froeyen, M.; Herdewijn, P.; Van Calenbergh, S.; Delarue, M.
    Enzymatic and structural analysis of inhibitors designed against Mycobacterium tuberculosis thymidylate kinase. New insights into the phosphoryl transfer mechanism (2003), J. Biol. Chem., 278, 4963-4971.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.7.4.9 drug development potential target for antituberculosis drugs Mycobacterium tuberculosis

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.4.9 expressed in Escherichia coli Mycobacterium tuberculosis

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
2.7.4.9 cocrystallization with TMP and potential inhibitors Mycobacterium tuberculosis

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.4.9 3'-azido-3'-deoxythymidine 5'-monophosphate potential inhibitor Mycobacterium tuberculosis
2.7.4.9 azido-TMP
-
 Mycobacterium tuberculosis
2.7.4.9 additional information several different TMP analogues tested and found to be inhibitory Mycobacterium tuberculosis
2.7.4.9 P1,P5-di(adenosine-5')pentaphosphate potential inhibitor Mycobacterium tuberculosis

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.7.4.9 0.04
-
 TMP pH 7.5 Mycobacterium tuberculosis
2.7.4.9 0.1
-
 ATP pH 7.5 Mycobacterium tuberculosis

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.7.4.9 Mg2+ bound to enzyme, displacement of Mg2+ might be responsible for inhibitory effect of the enzyme inhibitors Mycobacterium tuberculosis

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.4.9 ATP + TMP Mycobacterium tuberculosis involved in TTP metabolism ADP + TDP
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.4.9 Mycobacterium tuberculosis P9WKE1
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.7.4.9
-
 Mycobacterium tuberculosis

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.4.9 ATP + TMP
-
 Mycobacterium tuberculosis ADP + TDP
-
 ?
2.7.4.9 ATP + TMP involved in TTP metabolism Mycobacterium tuberculosis ADP + TDP
-
 ?

Subunits

EC Number Subunits Comment Organism
2.7.4.9 dimer homodimer Mycobacterium tuberculosis

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.7.4.9 0.03
-
 P1,P5-di(adenosine-5')pentaphosphate pH 7.5 Mycobacterium tuberculosis
2.7.4.9 0.05
-
 3'-azido-3'-deoxythymidine 5'-monophosphate pH 7.5 Mycobacterium tuberculosis