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Literature summary for 2.7.8.13 extracted from

  • Yamamoto, K.; Sato, T.; Hikiji, Y.; Katsuyama, A.; Matsumaru, T.; Yakushiji, F.; Yokota, S.; Ichikawa, S.
    Synthesis and biological evaluation of a MraY selective analogue of tunicamycins (2020), Nucleosides Nucleotides Nucleic Acids, 39, 349-364 .
    View publication on PubMed
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Crystallization (Commentary)

Crystallization (Comment) Organism
molecular modeling of complex with inhibitor 3'-O-(2R)-1-(methylamino-1-oxopropan-2-yl)-tunicamycin V, the compound generates a steric clash between the N-methylpropanamide moiety introduced in the place of the GlcNAc moiety of 2 and loop E Enterocloster bolteae
molecular modeling of complex with inhibitor 3'-O-(2R)-1-(methylamino-1-oxopropan-2-yl)-tunicamycin V, the compound generates a steric clash between the N-methylpropanamide moiety introduced in the place of the GlcNAc moiety of 2 and loop E Staphylococcus aureus

Inhibitors

Inhibitors Comment Organism Structure
3'-O-(2R)-1-(methylamino-1-oxopropan-2-yl)-tunicamycin V MurNAc analogue of tunicamycin. The inhibitor does not show toxicity against HepG2 cells up to 100 microM, and is a non-toxic selective MraY inhibitor Enterocloster bolteae
3'-O-(2R)-1-(methylamino-1-oxopropan-2-yl)-tunicamycin V MurNAc analogue of tunicamycin. The inhibitordoes not show toxicity against HepG2 cells up to 100 microM, and is a non-toxic selective MraY inhibitor.The inhibitor retains weak antibacterial activity against Staphylococcus aureus, the MIC value is reduced compared to tunicamycin Staphylococcus aureus
tunicamycin V
-
 Enterocloster bolteae
tunicamycin V
-
 Staphylococcus aureus

Organism

Organism UniProt Comment Textmining
Enterocloster bolteae R0BTE9
-
-
Enterocloster bolteae 90A9 R0BTE9
-
-
Staphylococcus aureus R0BTE9
-
-
Staphylococcus aureus ATCC 25923 R0BTE9
-
-

Synonyms

Synonyms Comment Organism
MraY
-
 Enterocloster bolteae
MraY
-
 Staphylococcus aureus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000087
-
 pH 7.6, 23°C Staphylococcus aureus 3'-O-(2R)-1-(methylamino-1-oxopropan-2-yl)-tunicamycin V
0.00025
-
 pH 7.6, 23°C Staphylococcus aureus tunicamycin V