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Literature summary for 2.7.8.35 extracted from

  • Ishizaki, Y.; Hayashi, C.; Inoue, K.; Igarashi, M.; Takahashi, Y.; Pujari, V.; Crick, D.C.; Brennan, P.J.; Nomoto, A.
    Inhibition of the first step in synthesis of the mycobacterial cell wall core, catalyzed by the GlcNAc-1-phosphate transferase WecA, by the novel caprazamycin derivative CPZEN-45 (2013), J. Biol. Chem., 288, 30309-30319.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
drug development enzyme WecA is a promising target for the development of antituberculous drugs as a countermeasure of drug resistant tuberculosis Mycobacterium tuberculosis

Cloned(Commentary)

Cloned (Comment) Organism
gene wecA, recombinant expression in Mycobacterium smegmatis strain 8a10 Mycobacterium tuberculosis

Inhibitors

Inhibitors Comment Organism Structure
CPZEN-45 a caprazamycin derivative, CPZEN-45 shows excellent antitubercular activity against not only drug-sensitive strains but also some multidrug-resistant tuberculosis and extensively drug-resistant tuberculosis strains Mycobacterium tuberculosis
additional information poor inhibition by caprazamycin B Mycobacterium tuberculosis
tunicamycin
-
Mycobacterium tuberculosis
Vancomycin weak inhibition Mycobacterium tuberculosis

Organism

Organism UniProt Comment Textmining
Mycobacterium tuberculosis P9WMW5 gene wecA or Rv1302 or Rfe
-
Mycobacterium tuberculosis H37Rv P9WMW5 gene wecA or Rv1302 or Rfe
-

Synonyms

Synonyms Comment Organism
decaprenyl-phosphate N-acetylglucosaminephosphotransferase UniProt Mycobacterium tuberculosis
GlcNAc-1-phosphate transferase
-
Mycobacterium tuberculosis
WecA
-
Mycobacterium tuberculosis

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00004
-
pH and temperature not specified in the publication Mycobacterium tuberculosis CPZEN-45
0.004
-
pH and temperature not specified in the publication Mycobacterium tuberculosis Vancomycin

General Information

General Information Comment Organism
metabolism the enzyme is involved in the biosynthesis of the mycolylarabinogalactan of the cell wall of Mycobacterium tuberculosis Mycobacterium tuberculosis