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Literature summary extracted from

  • Hammoudeh, D.I.; Date, M.; Yun, M.K.; Zhang, W.; Boyd, V.A.; Viacava Follis, A.; Griffith, E.; Lee, R.E.; Bashford, D.; White, S.W.
    Identification and characterization of an allosteric inhibitory site on dihydropteroate synthase (2014), ACS Chem. Biol., 9, 1294-1302.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.5.1.15 2-(7-amino-1-methyl-4,5-dioxo-1,4,5,6-tetrahydropyrimido[4,5-c]pyridazin-3-yl)propanoic acid 86% inhibition at 0.25 mM Bacillus anthracis
2.5.1.15 2-(7-amino-1-methyl-4,5-dioxo-1,4,5,6-tetrahydropyrimido[4,5-c]pyridazin-3-yl)propanoic acid 46% inhibition at 0.25 mM Staphylococcus aureus
2.5.1.15 2-(7-amino-1-methyl-4,5-dioxo-1,4,5,6-tetrahydropyrimido[4,5-c]pyridazin-3-yl)propanoic acid 61% inhibition at 0.25 mM Yersinia pestis
2.5.1.15 N-(4-(trifluoromethyl)-benzylidene)-1-(4-(trifluoromethyl))benzylamine complete inhibition at 0.25 mM Bacillus anthracis
2.5.1.15 N-(4-(trifluoromethyl)-benzylidene)-1-(4-(trifluoromethyl))benzylamine complete inhibition at 0.25 mM Staphylococcus aureus
2.5.1.15 N-(4-(trifluoromethyl)-benzylidene)-1-(4-(trifluoromethyl))benzylamine complete inhibition at 0.25 mM Yersinia pestis

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.5.1.15 (7,8-dihydropterin-6-yl)methyl diphosphate + 4-aminobenzoate Staphylococcus aureus
-
 diphosphate + 7,8-dihydropteroate
-
 ?
2.5.1.15 (7,8-dihydropterin-6-yl)methyl diphosphate + 4-aminobenzoate Yersinia pestis
-
 diphosphate + 7,8-dihydropteroate
-
 ?
2.5.1.15 (7,8-dihydropterin-6-yl)methyl diphosphate + 4-aminobenzoate Bacillus anthracis
-
 diphosphate + 7,8-dihydropteroate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.5.1.15 Bacillus anthracis Q81VW8
-
-
2.5.1.15 Staphylococcus aureus
-
-
-
2.5.1.15 Yersinia pestis
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.5.1.15 (7,8-dihydropterin-6-yl)methyl diphosphate + 4-aminobenzoate
-
 Staphylococcus aureus diphosphate + 7,8-dihydropteroate
-
 ?
2.5.1.15 (7,8-dihydropterin-6-yl)methyl diphosphate + 4-aminobenzoate
-
 Yersinia pestis diphosphate + 7,8-dihydropteroate
-
 ?
2.5.1.15 (7,8-dihydropterin-6-yl)methyl diphosphate + 4-aminobenzoate
-
 Bacillus anthracis diphosphate + 7,8-dihydropteroate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.5.1.15 DHPS
-
 Staphylococcus aureus
2.5.1.15 DHPS
-
 Yersinia pestis
2.5.1.15 DHPS
-
 Bacillus anthracis
2.5.1.15 FolP
-
 Staphylococcus aureus
2.5.1.15 FolP
-
 Yersinia pestis
2.5.1.15 FolP
-
 Bacillus anthracis

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.5.1.15 0.017
-
 at pH 7.6 and 37°C Staphylococcus aureus 2-(7-amino-1-methyl-4,5-dioxo-1,4,5,6-tetrahydropyrimido[4,5-c]pyridazin-3-yl)propanoic acid
2.5.1.15 0.031
-
 at pH 7.6 and 37°C Yersinia pestis 2-(7-amino-1-methyl-4,5-dioxo-1,4,5,6-tetrahydropyrimido[4,5-c]pyridazin-3-yl)propanoic acid
2.5.1.15 0.05
-
 at pH 7.6 and 37°C Bacillus anthracis 2-(7-amino-1-methyl-4,5-dioxo-1,4,5,6-tetrahydropyrimido[4,5-c]pyridazin-3-yl)propanoic acid