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Literature summary for 2.7.4.9 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
Search for more literature for 2.7.4.9

Application

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

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli Mycobacterium tuberculosis

Crystallization (Commentary)

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

Inhibitors

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

KM Value [mM]

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

Metals/Ions

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

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Mycobacterium tuberculosis P9WKE1
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Mycobacterium tuberculosis

Substrates and Products (Substrate)

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

Subunits

Subunits Comment Organism
dimer homodimer Mycobacterium tuberculosis

Ki Value [mM]

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