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Literature summary extracted from

  • Terrak, M.
    Peptidoglycan glycosyltransferase inhibition: New perspectives for an old target (2008), Anti-Infect. Agents Med. Chem., 7, 180-192.
No PubMed abstract available

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.1.129 (3E,7E,14E)-4,9,9,15,19-pentamethyl-12-methylideneicosa-3,7,14,18-tetraen-1-yl (2R)-3-[[[[(2R,3R,4S,5S,6S)-6-carbamoyl-3-[[(2S,3R,4R,5S,6R)-4,5-dihydroxy-6-(hydroxymethyl)-3-([[3-(trifluoromethyl)phenyl]carbonyl]amino)tetrahydro-2H-pyran-2-yl]oxy]-5-hydroxy-4-([[4-(trifluoromethoxy)-3-(trifluoromethyl)phenyl]carbamoyl]amino)tetrahydro-2H-pyran-2-yl]oxy](hydroxy)phosphoryl]oxy]-2-hydroxypropanoate
-
Aquifex aeolicus
2.4.1.129 (3E,7E,14E)-4,9,9,15,19-pentamethyl-12-methylideneicosa-3,7,14,18-tetraen-1-yl (2R)-3-[[[[(2R,3R,4S,5S,6S)-6-carbamoyl-3-[[(2S,3R,4R,5S,6R)-4,5-dihydroxy-6-(hydroxymethyl)-3-([[3-(trifluoromethyl)phenyl]carbonyl]amino)tetrahydro-2H-pyran-2-yl]oxy]-5-hydroxy-4-([[4-(trifluoromethoxy)-3-(trifluoromethyl)phenyl]carbamoyl]amino)tetrahydro-2H-pyran-2-yl]oxy](hydroxy)phosphoryl]oxy]-2-hydroxypropanoate
-
Enterococcus faecalis
2.4.1.129 (3E,7E,14E)-4,9,9,15,19-pentamethyl-12-methylideneicosa-3,7,14,18-tetraen-1-yl (2R)-3-[[[[(2R,3R,4S,5S,6S)-6-carbamoyl-3-[[(2S,3R,4R,5S,6R)-4,5-dihydroxy-6-(hydroxymethyl)-3-([[3-(trifluoromethyl)phenyl]carbonyl]amino)tetrahydro-2H-pyran-2-yl]oxy]-5-hydroxy-4-([[4-(trifluoromethoxy)-3-(trifluoromethyl)phenyl]carbamoyl]amino)tetrahydro-2H-pyran-2-yl]oxy](hydroxy)phosphoryl]oxy]-2-hydroxypropanoate
-
Escherichia coli
2.4.1.129 (3E,7E,14E)-4,9,9,15,19-pentamethyl-12-methylideneicosa-3,7,14,18-tetraen-1-yl (2R)-3-[[[[(2R,3R,4S,5S,6S)-6-carbamoyl-3-[[(2S,3R,4R,5S,6R)-4,5-dihydroxy-6-(hydroxymethyl)-3-([[3-(trifluoromethyl)phenyl]carbonyl]amino)tetrahydro-2H-pyran-2-yl]oxy]-5-hydroxy-4-([[4-(trifluoromethoxy)-3-(trifluoromethyl)phenyl]carbamoyl]amino)tetrahydro-2H-pyran-2-yl]oxy](hydroxy)phosphoryl]oxy]-2-hydroxypropanoate
-
Helicobacter pylori
2.4.1.129 (3E,7E,14E)-4,9,9,15,19-pentamethyl-12-methylideneicosa-3,7,14,18-tetraen-1-yl (2R)-3-[[[[(2R,3R,4S,5S,6S)-6-carbamoyl-3-[[(2S,3R,4R,5S,6R)-4,5-dihydroxy-6-(hydroxymethyl)-3-([[3-(trifluoromethyl)phenyl]carbonyl]amino)tetrahydro-2H-pyran-2-yl]oxy]-5-hydroxy-4-([[4-(trifluoromethoxy)-3-(trifluoromethyl)phenyl]carbamoyl]amino)tetrahydro-2H-pyran-2-yl]oxy](hydroxy)phosphoryl]oxy]-2-hydroxypropanoate
-
Staphylococcus aureus
2.4.1.129 (3Z)-5-(4-bromophenyl)-3-[(5-nitrofuran-2-yl)methylidene]furan-2(3H)-one
-
Aquifex aeolicus
2.4.1.129 (3Z)-5-(4-bromophenyl)-3-[(5-nitrofuran-2-yl)methylidene]furan-2(3H)-one
-
Enterococcus faecalis
2.4.1.129 (3Z)-5-(4-bromophenyl)-3-[(5-nitrofuran-2-yl)methylidene]furan-2(3H)-one
-
Escherichia coli
2.4.1.129 (3Z)-5-(4-bromophenyl)-3-[(5-nitrofuran-2-yl)methylidene]furan-2(3H)-one
-
Helicobacter pylori
2.4.1.129 (3Z)-5-(4-bromophenyl)-3-[(5-nitrofuran-2-yl)methylidene]furan-2(3H)-one
-
Staphylococcus aureus
2.4.1.129 (4Z)-2,5-diphenyl-4-[2-(1,3-thiazol-2-yl)hydrazinylidene]-2,4-dihydro-3H-pyrazol-3-one
-
Aquifex aeolicus
2.4.1.129 (4Z)-2,5-diphenyl-4-[2-(1,3-thiazol-2-yl)hydrazinylidene]-2,4-dihydro-3H-pyrazol-3-one
-
Enterococcus faecalis
2.4.1.129 (4Z)-2,5-diphenyl-4-[2-(1,3-thiazol-2-yl)hydrazinylidene]-2,4-dihydro-3H-pyrazol-3-one
-
Escherichia coli
2.4.1.129 (4Z)-2,5-diphenyl-4-[2-(1,3-thiazol-2-yl)hydrazinylidene]-2,4-dihydro-3H-pyrazol-3-one
-
Helicobacter pylori
2.4.1.129 (4Z)-2,5-diphenyl-4-[2-(1,3-thiazol-2-yl)hydrazinylidene]-2,4-dihydro-3H-pyrazol-3-one
-
Staphylococcus aureus
2.4.1.129 4-[(1E)-2-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)prop-1-en-1-yl]benzoic acid
-
Aquifex aeolicus
2.4.1.129 4-[(1E)-2-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)prop-1-en-1-yl]benzoic acid
-
Enterococcus faecalis
2.4.1.129 4-[(1E)-2-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)prop-1-en-1-yl]benzoic acid
-
Escherichia coli
2.4.1.129 4-[(1E)-2-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)prop-1-en-1-yl]benzoic acid
-
Helicobacter pylori
2.4.1.129 4-[(1E)-2-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)prop-1-en-1-yl]benzoic acid
-
Staphylococcus aureus
2.4.1.129 chlorobiphenyl desleucyl vancomycin
-
Aquifex aeolicus
2.4.1.129 chlorobiphenyl desleucyl vancomycin
-
Enterococcus faecalis
2.4.1.129 chlorobiphenyl desleucyl vancomycin
-
Escherichia coli
2.4.1.129 chlorobiphenyl desleucyl vancomycin
-
Helicobacter pylori
2.4.1.129 chlorobiphenyl desleucyl vancomycin
-
Staphylococcus aureus
2.4.1.129 chlorobiphenyl disaccharide
-
Aquifex aeolicus
2.4.1.129 chlorobiphenyl disaccharide
-
Enterococcus faecalis
2.4.1.129 chlorobiphenyl disaccharide
-
Escherichia coli
2.4.1.129 chlorobiphenyl disaccharide
-
Helicobacter pylori
2.4.1.129 chlorobiphenyl disaccharide
-
Staphylococcus aureus
2.4.1.129 chlorobiphenyl vancomycin
-
Aquifex aeolicus
2.4.1.129 chlorobiphenyl vancomycin
-
Enterococcus faecalis
2.4.1.129 chlorobiphenyl vancomycin
-
Escherichia coli
2.4.1.129 chlorobiphenyl vancomycin
-
Helicobacter pylori
2.4.1.129 chlorobiphenyl vancomycin
-
Staphylococcus aureus
2.4.1.129 moenomycin A
-
Aquifex aeolicus
2.4.1.129 moenomycin A
-
Enterococcus faecalis
2.4.1.129 moenomycin A
-
Escherichia coli
2.4.1.129 moenomycin A
-
Helicobacter pylori
2.4.1.129 moenomycin A
-
Staphylococcus aureus
2.4.1.129 moenomycin disaccharide
-
Aquifex aeolicus
2.4.1.129 moenomycin disaccharide
-
Enterococcus faecalis
2.4.1.129 moenomycin disaccharide
-
Escherichia coli
2.4.1.129 moenomycin disaccharide
-
Helicobacter pylori
2.4.1.129 moenomycin disaccharide
-
Staphylococcus aureus
2.4.1.129 moenomycin trisaccharide
-
Aquifex aeolicus
2.4.1.129 moenomycin trisaccharide
-
Enterococcus faecalis
2.4.1.129 moenomycin trisaccharide
-
Escherichia coli
2.4.1.129 moenomycin trisaccharide
-
Helicobacter pylori
2.4.1.129 moenomycin trisaccharide
-
Staphylococcus aureus
2.4.1.129 Vancomycin
-
Aquifex aeolicus
2.4.1.129 Vancomycin
-
Enterococcus faecalis
2.4.1.129 Vancomycin
-
Escherichia coli
2.4.1.129 Vancomycin
-
Helicobacter pylori
2.4.1.129 Vancomycin
-
Staphylococcus aureus

Organism

EC Number Organism UniProt Comment Textmining
2.4.1.129 Aquifex aeolicus
-
-
-
2.4.1.129 Enterococcus faecalis
-
-
-
2.4.1.129 Escherichia coli
-
-
-
2.4.1.129 Escherichia coli BAS849
-
-
-
2.4.1.129 Helicobacter pylori
-
-
-
2.4.1.129 Staphylococcus aureus
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.1.129 additional information while isoform PBP1a is able to convert lipid IV (heptaprenyl-tetrasaccharide) to peptidoglycan in the absence of lipid II, isoform PBP1b does not use lipid IV as substrate unless lipid II is also present Staphylococcus aureus ?
-
?
2.4.1.129 additional information while isoform PBP1a is able to convert lipid IV (heptaprenyl-tetrasaccharide) to peptidoglycan in the absence of lipid II, isoform PBP1b does not use lipid IV as substrate unless lipid II is also present Escherichia coli ?
-
?
2.4.1.129 additional information while isoform PBP1a is able to convert lipid IV (heptaprenyl-tetrasaccharide) to peptidoglycan in the absence of lipid II, isoform PBP1b does not use lipid IV as substrate unless lipid II is also present Enterococcus faecalis ?
-
?
2.4.1.129 additional information while isoform PBP1a is able to convert lipid IV (heptaprenyl-tetrasaccharide) to peptidoglycan in the absence of lipid II, isoform PBP1b does not use lipid IV as substrate unless lipid II is also present Helicobacter pylori ?
-
?
2.4.1.129 additional information while isoform PBP1a is able to convert lipid IV (heptaprenyl-tetrasaccharide) to peptidoglycan in the absence of lipid II, isoform PBP1b does not use lipid IV as substrate unless lipid II is also present Aquifex aeolicus ?
-
?
2.4.1.129 additional information while isoform PBP1a is able to convert lipid IV (heptaprenyl-tetrasaccharide) to peptidoglycan in the absence of lipid II, isoform PBP1b does not use lipid IV as substrate unless lipid II is also present Escherichia coli BAS849 ?
-
?
2.4.1.129 [GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-(L)-meso-diaminopimelic acid-(L)-D-Ala-D-Ala)]n-diphosphoundecaprenol + GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-(L)-meso-diaminopimelic acid-(L)-D-Ala-D-Ala)-diphosphoundecaprenol
-
Staphylococcus aureus [GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-(L)-meso-diaminopimelic acid-(L)-D-Ala-D-Ala)]n+1-diphosphoundecaprenol + undecaprenyl diphosphate
-
?
2.4.1.129 [GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-(L)-meso-diaminopimelic acid-(L)-D-Ala-D-Ala)]n-diphosphoundecaprenol + GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-(L)-meso-diaminopimelic acid-(L)-D-Ala-D-Ala)-diphosphoundecaprenol
-
Escherichia coli [GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-(L)-meso-diaminopimelic acid-(L)-D-Ala-D-Ala)]n+1-diphosphoundecaprenol + undecaprenyl diphosphate
-
?
2.4.1.129 [GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-(L)-meso-diaminopimelic acid-(L)-D-Ala-D-Ala)]n-diphosphoundecaprenol + GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-(L)-meso-diaminopimelic acid-(L)-D-Ala-D-Ala)-diphosphoundecaprenol
-
Enterococcus faecalis [GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-(L)-meso-diaminopimelic acid-(L)-D-Ala-D-Ala)]n+1-diphosphoundecaprenol + undecaprenyl diphosphate
-
?
2.4.1.129 [GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-(L)-meso-diaminopimelic acid-(L)-D-Ala-D-Ala)]n-diphosphoundecaprenol + GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-(L)-meso-diaminopimelic acid-(L)-D-Ala-D-Ala)-diphosphoundecaprenol
-
Helicobacter pylori [GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-(L)-meso-diaminopimelic acid-(L)-D-Ala-D-Ala)]n+1-diphosphoundecaprenol + undecaprenyl diphosphate
-
?
2.4.1.129 [GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-(L)-meso-diaminopimelic acid-(L)-D-Ala-D-Ala)]n-diphosphoundecaprenol + GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-(L)-meso-diaminopimelic acid-(L)-D-Ala-D-Ala)-diphosphoundecaprenol
-
Aquifex aeolicus [GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-(L)-meso-diaminopimelic acid-(L)-D-Ala-D-Ala)]n+1-diphosphoundecaprenol + undecaprenyl diphosphate
-
?
2.4.1.129 [GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-(L)-meso-diaminopimelic acid-(L)-D-Ala-D-Ala)]n-diphosphoundecaprenol + GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-(L)-meso-diaminopimelic acid-(L)-D-Ala-D-Ala)-diphosphoundecaprenol
-
Escherichia coli BAS849 [GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-(L)-meso-diaminopimelic acid-(L)-D-Ala-D-Ala)]n+1-diphosphoundecaprenol + undecaprenyl diphosphate
-
?
2.4.1.129 [GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-L-Lys-D-Ala-D-Ala)]n-diphosphoundecaprenol + GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-(L)-meso-diaminopimelic acid-(L)-D-Ala-D-Ala)-diphosphoundecaprenol
-
Staphylococcus aureus [GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-L-Lys-D-Ala-D-Ala)]n+1-diphosphoundecaprenol + undecaprenyl diphosphate
-
?
2.4.1.129 [GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-L-Lys-D-Ala-D-Ala)]n-diphosphoundecaprenol + GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-(L)-meso-diaminopimelic acid-(L)-D-Ala-D-Ala)-diphosphoundecaprenol
-
Escherichia coli [GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-L-Lys-D-Ala-D-Ala)]n+1-diphosphoundecaprenol + undecaprenyl diphosphate
-
?
2.4.1.129 [GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-L-Lys-D-Ala-D-Ala)]n-diphosphoundecaprenol + GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-(L)-meso-diaminopimelic acid-(L)-D-Ala-D-Ala)-diphosphoundecaprenol
-
Enterococcus faecalis [GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-L-Lys-D-Ala-D-Ala)]n+1-diphosphoundecaprenol + undecaprenyl diphosphate
-
?
2.4.1.129 [GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-L-Lys-D-Ala-D-Ala)]n-diphosphoundecaprenol + GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-(L)-meso-diaminopimelic acid-(L)-D-Ala-D-Ala)-diphosphoundecaprenol
-
Helicobacter pylori [GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-L-Lys-D-Ala-D-Ala)]n+1-diphosphoundecaprenol + undecaprenyl diphosphate
-
?
2.4.1.129 [GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-L-Lys-D-Ala-D-Ala)]n-diphosphoundecaprenol + GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-(L)-meso-diaminopimelic acid-(L)-D-Ala-D-Ala)-diphosphoundecaprenol
-
Aquifex aeolicus [GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-L-Lys-D-Ala-D-Ala)]n+1-diphosphoundecaprenol + undecaprenyl diphosphate
-
?
2.4.1.129 [GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-L-Lys-D-Ala-D-Ala)]n-diphosphoundecaprenol + GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-(L)-meso-diaminopimelic acid-(L)-D-Ala-D-Ala)-diphosphoundecaprenol
-
Escherichia coli BAS849 [GlcNAc-(1-4)-Mur2Ac(oyl-L-Ala-gamma-D-Glu-L-Lys-D-Ala-D-Ala)]n+1-diphosphoundecaprenol + undecaprenyl diphosphate
-
?

Synonyms

EC Number Synonyms Comment Organism
2.4.1.129 class A penicillin-binding protein
-
Escherichia coli
2.4.1.129 MGT
-
Escherichia coli
2.4.1.129 PBP1a isoform Escherichia coli
2.4.1.129 PBP1a isoform Helicobacter pylori
2.4.1.129 PBP1a isoform Aquifex aeolicus
2.4.1.129 PBP1b isoform Escherichia coli
2.4.1.129 PBP1c isoform Escherichia coli
2.4.1.129 PBP2
-
Staphylococcus aureus
2.4.1.129 penicillin-binding protein
-
Staphylococcus aureus
2.4.1.129 penicillin-binding protein
-
Enterococcus faecalis

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.4.1.129 0.000006
-
-
Escherichia coli moenomycin A
2.4.1.129 0.000006
-
-
Aquifex aeolicus moenomycin A
2.4.1.129 0.000016
-
-
Escherichia coli moenomycin trisaccharide
2.4.1.129 0.000016
-
-
Aquifex aeolicus moenomycin trisaccharide
2.4.1.129 0.000033
-
-
Escherichia coli moenomycin disaccharide
2.4.1.129 0.000033
-
-
Aquifex aeolicus moenomycin disaccharide
2.4.1.129 0.00038
-
-
Escherichia coli Vancomycin
2.4.1.129 0.00038
-
-
Aquifex aeolicus Vancomycin
2.4.1.129 0.0015
-
-
Escherichia coli chlorobiphenyl vancomycin
2.4.1.129 0.0015
-
-
Aquifex aeolicus chlorobiphenyl vancomycin
2.4.1.129 0.0037
-
-
Helicobacter pylori (4Z)-2,5-diphenyl-4-[2-(1,3-thiazol-2-yl)hydrazinylidene]-2,4-dihydro-3H-pyrazol-3-one
2.4.1.129 0.00388
-
-
Escherichia coli chlorobiphenyl desleucyl vancomycin
2.4.1.129 0.00388
-
-
Aquifex aeolicus chlorobiphenyl desleucyl vancomycin
2.4.1.129 0.0093
-
-
Helicobacter pylori 4-[(1E)-2-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)prop-1-en-1-yl]benzoic acid
2.4.1.129 0.0098
-
-
Escherichia coli (3E,7E,14E)-4,9,9,15,19-pentamethyl-12-methylideneicosa-3,7,14,18-tetraen-1-yl (2R)-3-[[[[(2R,3R,4S,5S,6S)-6-carbamoyl-3-[[(2S,3R,4R,5S,6R)-4,5-dihydroxy-6-(hydroxymethyl)-3-([[3-(trifluoromethyl)phenyl]carbonyl]amino)tetrahydro-2H-pyran-2-yl]oxy]-5-hydroxy-4-([[4-(trifluoromethoxy)-3-(trifluoromethyl)phenyl]carbamoyl]amino)tetrahydro-2H-pyran-2-yl]oxy](hydroxy)phosphoryl]oxy]-2-hydroxypropanoate
2.4.1.129 0.034
-
-
Helicobacter pylori (3Z)-5-(4-bromophenyl)-3-[(5-nitrofuran-2-yl)methylidene]furan-2(3H)-one