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Literature summary extracted from

  • Pochet, S.; Dugue, L.; Labesse, G.; Delepierre, M.; Munier-Lehmann, H.
    Comparative study of purine and pyrimidine nucleoside analogues acting on the thymidylate kinases of Mycobacterium tuberculosis and of humans (2003), ChemBioChem, 4, 742-747.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.7.4.9 drug development potential target for the development of new antituberculosis drugs due to the low sequence similarity with the human enzyme Mycobacterium tuberculosis

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.4.9 expressed as His-tag fusion protein in Escherichia coli BL21(DE3) Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.4.9 5-bromo-2'-deoxyuridine
-
 Homo sapiens
2.7.4.9 5-bromo-2'-deoxyuridine potential inhibitor with high selectivity between bacterial and human enzyme Mycobacterium tuberculosis
2.7.4.9 5-chloro-2'-deoxyuridine
-
 Homo sapiens
2.7.4.9 5-chloro-2'-deoxyuridine potential inhibitor with high selectivity between bacterial and human enzyme Mycobacterium tuberculosis
2.7.4.9 5-fluoro-2'-deoxyuridine not inhibitory at 4 mM Homo sapiens
2.7.4.9 5-fluoro-2'-deoxyuridine potential inhibitor with high selectivity between bacterial and human enzyme Mycobacterium tuberculosis
2.7.4.9 5-iodo-2'-deoxyuridine
-
 Homo sapiens
2.7.4.9 5-iodo-2'-deoxyuridine potential inhibitor with high selectivity between bacterial and human enzyme Mycobacterium tuberculosis
2.7.4.9 deoxythymidine
-
 Homo sapiens
2.7.4.9 deoxythymidine potential inhibitor with high selectivity between bacterial and human enzyme Mycobacterium tuberculosis
2.7.4.9 dGMP competitive Mycobacterium tuberculosis

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.7.4.9 0.005
-
 dTMP pH 7.4, 30°C Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.4.9 ATP + dTMP Homo sapiens involved in dTTP metabolism, essential for cell proliferation ADP + dTDP
-
 ?
2.7.4.9 ATP + dTMP Mycobacterium tuberculosis involved in dTTP metabolism, essential for cell proliferation ADP + dTDP
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.4.9 Homo sapiens
-
-
-
2.7.4.9 Mycobacterium tuberculosis
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.7.4.9 recombinant protein using His-tag Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.4.9 ATP + dTMP
-
 Homo sapiens ADP + dTDP
-
 ?
2.7.4.9 ATP + dTMP
-
 Mycobacterium tuberculosis ADP + dTDP
-
 ?
2.7.4.9 ATP + dTMP involved in dTTP metabolism, essential for cell proliferation Homo sapiens ADP + dTDP
-
 ?
2.7.4.9 ATP + dTMP involved in dTTP metabolism, essential for cell proliferation Mycobacterium tuberculosis ADP + dTDP
-
 ?

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.7.4.9 0.005
-
 5-bromo-2'-deoxyuridine pH 7.4, 30°C Mycobacterium tuberculosis
2.7.4.9 0.01
-
 5-chloro-2'-deoxyuridine pH 7.4, 30°C Mycobacterium tuberculosis
2.7.4.9 0.027
-
 deoxythymidine pH 7.4, 30°C Mycobacterium tuberculosis
2.7.4.9 0.033
-
 5-iodo-2'-deoxyuridine pH 7.4, 30°C Mycobacterium tuberculosis
2.7.4.9 0.117
-
 dGMP pH 7.4, 30°C Mycobacterium tuberculosis
2.7.4.9 0.18
-
 deoxythymidine pH 7.4, 30°C Homo sapiens
2.7.4.9 0.212
-
 5-fluoro-2'-deoxyuridine pH 7.4, 30°C Mycobacterium tuberculosis
2.7.4.9 0.214
-
 5-bromo-2'-deoxyuridine pH 7.4, 30°C Homo sapiens
2.7.4.9 0.35
-
 5-iodo-2'-deoxyuridine pH 7.4, 30°C Homo sapiens
2.7.4.9 0.375
-
 5-chloro-2'-deoxyuridine pH 7.4, 30°C Homo sapiens