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Literature summary for 2.5.1.15 extracted from

  • Zhao, Y.; Shadrick, W.R.; Wallace, M.J.; Wu, Y.; Griffith, E.C.; Qi, J.; Yun, M.K.; White, S.W.; Lee, R.E.
    Pterin-sulfa conjugates as dihydropteroate synthase inhibitors and antibacterial agents (2016), Bioorg. Med. Chem. Lett., 26, 3950-3954 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.5.1.15

Crystallization (Commentary)

Crystallization (Comment) Organism
an inhibitor is soaked into the apo crystals of the enzyme and the structure of the complex is determined to 2.1 A resolution. Thed inhibitor occupies both the pterin and 4-aminobenzoate binding pocket of the enzyme Yersinia pestis

Inhibitors

Inhibitors Comment Organism Structure
2-amino-6-[[4-(4-aminobenzene-1-sulfonyl)anilino]methyl]pteridin-4(1H)-one
-
 Bacillus anthracis
4-[[(2-amino-4-oxo-1,4-dihydropteridin-6-yl)methyl]amino]-N-(2,6-dimethoxypyrimidin-4-yl)benzene-1-sulfonamide
-
 Bacillus anthracis
4-[[(2-amino-4-oxo-1,4-dihydropteridin-6-yl)methyl]amino]-N-(3,4-dimethyl-1,2-oxazol-5-yl)benzene-1-sulfonamide
-
 Bacillus anthracis
4-[[(2-amino-4-oxo-1,4-dihydropteridin-6-yl)methyl]amino]-N-(5,6-dimethoxypyrimidin-4-yl)benzene-1-sulfonamide
-
 Bacillus anthracis
4-[[(2-amino-4-oxo-1,4-dihydropteridin-6-yl)methyl]amino]-N-(5-methyl-1,2-oxazol-3-yl)benzene-1-sulfonamide
-
 Bacillus anthracis
4-[[(2-amino-4-oxo-1,4-dihydropteridin-6-yl)methyl]amino]-N-(pyridin-2-yl)benzene-1-sulfonamide
-
 Bacillus anthracis
4-[[(2-amino-4-oxo-1,4-dihydropteridin-6-yl)methyl]amino]-N-(pyrimidin-2-yl)benzene-1-sulfonamide
-
 Bacillus anthracis
ampicillin
-
 Bacillus anthracis
chloramphenicol
-
 Bacillus anthracis
N-(4-[[(2-amino-4-oxo-1,4-dihydropteridin-6-yl)methyl]amino]benzene-1-sulfonyl)acetamide
-
 Bacillus anthracis
trimethroprim
-
 Bacillus anthracis

Organism

Organism UniProt Comment Textmining
Bacillus anthracis Q81VW8
-
-
Yersinia pestis A0A384KP04
-
-

Synonyms

Synonyms Comment Organism
DHPS
-
 Bacillus anthracis
DHPS
-
 Yersinia pestis

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0019
-
 pH and temperature not specified in the publication, fluorescence polarization based competition binding assay, in presence of 2 mM sodium diphosphate Bacillus anthracis 4-[[(2-amino-4-oxo-1,4-dihydropteridin-6-yl)methyl]amino]-N-(2,6-dimethoxypyrimidin-4-yl)benzene-1-sulfonamide
0.0025
-
 pH and temperature not specified in the publication, fluorescence polarization based competition binding assay, in presence of 2 mM sodium diphosphate Bacillus anthracis 4-[[(2-amino-4-oxo-1,4-dihydropteridin-6-yl)methyl]amino]-N-(pyridin-2-yl)benzene-1-sulfonamide
0.0034
-
 pH and temperature not specified in the publication, fluorescence polarization based competition binding assay, in presence of 2 mM sodium diphosphate Bacillus anthracis 4-[[(2-amino-4-oxo-1,4-dihydropteridin-6-yl)methyl]amino]-N-(5-methyl-1,2-oxazol-3-yl)benzene-1-sulfonamide
0.0081
-
 pH and temperature not specified in the publication, fluorescence polarization based competition binding assay Bacillus anthracis 4-[[(2-amino-4-oxo-1,4-dihydropteridin-6-yl)methyl]amino]-N-(3,4-dimethyl-1,2-oxazol-5-yl)benzene-1-sulfonamide
0.0094
-
 pH and temperature not specified in the publication, fluorescence polarization based competition binding assay, in presence of 2 mM sodium diphosphate Bacillus anthracis 4-[[(2-amino-4-oxo-1,4-dihydropteridin-6-yl)methyl]amino]-N-(pyrimidin-2-yl)benzene-1-sulfonamide
0.0113
-
 pH and temperature not specified in the publication, fluorescence polarization based competition binding assay, in presence of 2 mM sodium diphosphate Bacillus anthracis 2-amino-6-[[4-(4-aminobenzene-1-sulfonyl)anilino]methyl]pteridin-4(1H)-one
0.0115
-
 pH and temperature not specified in the publication, fluorescence polarization based competition binding assay, in presence of 2 mM sodium diphosphate Bacillus anthracis 4-[[(2-amino-4-oxo-1,4-dihydropteridin-6-yl)methyl]amino]-N-(5,6-dimethoxypyrimidin-4-yl)benzene-1-sulfonamide
0.0152
-
 pH and temperature not specified in the publication, fluorescence polarization based competition binding assay Bacillus anthracis 4-[[(2-amino-4-oxo-1,4-dihydropteridin-6-yl)methyl]amino]-N-(5,6-dimethoxypyrimidin-4-yl)benzene-1-sulfonamide
0.0171
-
 pH and temperature not specified in the publication, fluorescence polarization based competition binding assay, in presence of 2 mM sodium diphosphate Bacillus anthracis N-(4-[[(2-amino-4-oxo-1,4-dihydropteridin-6-yl)methyl]amino]benzene-1-sulfonyl)acetamide
0.0178
-
 pH and temperature not specified in the publication, fluorescence polarization based competition binding assay, without sodium diphosphate Bacillus anthracis 2-amino-6-[[4-(4-aminobenzene-1-sulfonyl)anilino]methyl]pteridin-4(1H)-one
0.0186
-
 pH and temperature not specified in the publication, fluorescence polarization based competition binding assay Bacillus anthracis N-(4-[[(2-amino-4-oxo-1,4-dihydropteridin-6-yl)methyl]amino]benzene-1-sulfonyl)acetamide
0.0193
-
 pH and temperature not specified in the publication, fluorescence polarization based competition binding assay, without sodium diphosphate Bacillus anthracis 4-[[(2-amino-4-oxo-1,4-dihydropteridin-6-yl)methyl]amino]-N-(pyrimidin-2-yl)benzene-1-sulfonamide
0.0206
-
 pH and temperature not specified in the publication, fluorescence polarization based competition binding assay, without sodium diphosphate Bacillus anthracis 4-[[(2-amino-4-oxo-1,4-dihydropteridin-6-yl)methyl]amino]-N-(5-methyl-1,2-oxazol-3-yl)benzene-1-sulfonamide
0.0225
-
 pH and temperature not specified in the publication, fluorescence polarization based competition binding assay Bacillus anthracis 4-[[(2-amino-4-oxo-1,4-dihydropteridin-6-yl)methyl]amino]-N-(3,4-dimethyl-1,2-oxazol-5-yl)benzene-1-sulfonamide
0.0268
-
 pH and temperature not specified in the publication, fluorescence polarization based competition binding assay, without sodium diphosphate Bacillus anthracis 4-[[(2-amino-4-oxo-1,4-dihydropteridin-6-yl)methyl]amino]-N-(2,6-dimethoxypyrimidin-4-yl)benzene-1-sulfonamide