Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.7.4.9 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
Search for more literature for 2.7.4.9

Application

Application Comment Organism
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)

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

Inhibitors

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

KM Value [mM]

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

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Mycobacterium tuberculosis
-
-
-

Purification (Commentary)

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

Substrates and Products (Substrate)

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

Ki Value [mM]

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