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Literature summary for 2.3.1.275 extracted from

  • Grimes, K.; Lu, Y.; Zhang, Y.; Luna, V.; Hurdle, J.; Carson, E.; Qi, J.; Kudrimoti, S.; Rock, C.; Lee, R.
    Novel acyl phosphate mimics that target PlsY, an essential acyltransferase in gram-positive bacteria (2008), ChemMedChem, 3, 1936-1945 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.3.1.275

Cloned(Commentary)

Cloned (Comment) Organism
overexpression in Escherichia coli Streptococcus pneumoniae
overexpression in Escherichia coli Bacillus anthracis

Inhibitors

Inhibitors Comment Organism Structure
((Z)-octadec-9-enylcarbamoyl)methylphosphonic acid 0.2 mM, 62% inhibition, pH 7.4, 37°C Bacillus anthracis
((Z)-octadec-9-enylcarbamoyl)methylphosphonic acid 0.2 mM, 49% inhibition, pH 7.4, 37°C Streptococcus pneumoniae
(heptylcarbamoyl)methylphosphonic acid 0.2 mM, 98% inhibition, pH 7.4, 37°C Bacillus anthracis
(N-dodecyl-N-methylcarbamoyl)methylphosphonic acid 0.2 mM,23 % inhibition, pH 7.4, 37°C Bacillus anthracis
(N-dodecyl-N-methylcarbamoyl)methylphosphonic acid 0.2 mM, 64% inhibition, pH 7.4, 37°C Streptococcus pneumoniae
(Z)-1,1-difluoro-2-oxononadec-10-enylphosphonic acid 0.2 mM, 68% inhibition, pH 7.4, 37°C Bacillus anthracis
(Z)-1,1-difluoro-2-oxononadec-10-enylphosphonic acid 0.2 mM, 100% inhibition, pH 7.4, 37°C Streptococcus pneumoniae
(Z)-1-oxooctadec-11-enylphosphoramidic acid 0.2 mM, 93% inhibition, pH 7.4, 37°C Streptococcus pneumoniae
(Z)-2-oxononadec-12-enylphosphonic acid 0.2 mM, 40% inhibition, pH 7.4, 37°C Bacillus anthracis
(Z)-2-oxononadec-12-enylphosphonic acid 0.2 mM, 98% inhibition, pH 7.4, 37°C Streptococcus pneumoniae
1,1-difluoro-2-oxododec-11-enylphosphonic acid 0.2 mM, 29% inhibition, pH 7.4, 37°C Bacillus anthracis
1,1-difluoro-2-oxododec-11-enylphosphonic acid 0.2 mM, 14% inhibition, pH 7.4, 37°C Streptococcus pneumoniae
1,1-difluoro-2-oxoheptadecylphosphonic acid 0.2 mM, 91% inhibition, pH 7.4, 37°C Bacillus anthracis
1,1-difluoro-2-oxoheptadecylphosphonic acid 0.2 mM, 99% inhibition, pH 7.4, 37°C Streptococcus pneumoniae
1,1-difluoro-2-oxotridecylphosphonic acid 0.2 mM, 100% inhibition, pH 7.4, 37°C Bacillus anthracis
1,1-difluoro-2-oxotridecylphosphonic acid 0.2 mM, 48% inhibition, pH 7.4, 37°C Streptococcus pneumoniae
1-oxo-11-phenoxyundecylphosphoramidic acid 0.2 mM, 47% inhibition, pH 7.4, 37°C Streptococcus pneumoniae
1-oxododecylphosphoramidic acid 0.2 mM, 30% inhibition, pH 7.4, 37°C Streptococcus pneumoniae
1-oxohexadecylphosphoramidic acid 0.2 mM, 75% inhibition, pH 7.4, 37°C Streptococcus pneumoniae
2-oxo-12-phenoxydodecylphosphonic acid 0.2 mM, 55% inhibition, pH 7.4, 37°C Bacillus anthracis
2-oxo-12-phenoxydodecylphosphonic acid 0.2 mM, 48% inhibition, pH 7.4, 37°C Streptococcus pneumoniae
2-oxo-6-phenylhexylphosphonic acid 0.2 mM, 6% inhibition, pH 7.4, 37°C Streptococcus pneumoniae
2-oxoheptadecylphosphonic acid 0.2 mM, 67% inhibition, pH 7.4, 37°C Bacillus anthracis
2-oxoheptadecylphosphonic acid 0.2 mM, 28% inhibition, pH 7.4, 37°C Streptococcus pneumoniae
2-oxopentylphosphonic acid 0.2 mM, 18% inhibition, pH 7.4, 37°C Streptococcus pneumoniae
2-oxotridecylphosphonic acid 0.2 mM, 28% inhibition, pH 7.4, 37°C Bacillus anthracis
2-oxotridecylphosphonic acid 0.2 mM, 38% inhibition, pH 7.4, 37°C Streptococcus pneumoniae
4-methoxyphenyl 5-phenylpentanoylsulfamate 0.2 mM, 13% inhibition, pH 7.4, 37°C Bacillus anthracis
4-methoxyphenyl 5-phenylpentanoylsulfamate 0.2 mM, 12% inhibition, pH 7.4, 37°C Streptococcus pneumoniae
4-methoxyphenyl palmitoylsulfamate 0.2 mM, 100% inhibition, pH 7.4, 37°C Bacillus anthracis
4-methoxyphenyl palmitoylsulfamate 0.2 mM, 100% inhibition, pH 7.4, 37°C Streptococcus pneumoniae
5-cyclohexyl-1-oxopentylphosphoramidic acid 0.2 mM, 18% inhibition, pH 7.4, 37°C Streptococcus pneumoniae
6-cyclohexyl-2-oxohexylphosphonic acid 0.2 mM, 9% inhibition, pH 7.4, 37°C Streptococcus pneumoniae
butyl palmitoylsulfamate 0.2 mM, 99% inhibition, pH 7.4, 37°C Bacillus anthracis
butyl palmitoylsulfamate 0.2 mM, 100% inhibition, pH 7.4, 37°C Streptococcus pneumoniae
ethyl palmitoylsulfamate 0.2 mM, 99% inhibition, pH 7.4, 37°C Bacillus anthracis
ethyl palmitoylsulfamate 0.2 mM, 98% inhibition, pH 7.4, 37°C Streptococcus pneumoniae

Organism

Organism UniProt Comment Textmining
Bacillus anthracis Q81QF8
-
-
Bacillus anthracis Sterne 34F2 Q81QF8
-
-
Streptococcus pneumoniae
-
-
-
Streptococcus pneumoniae DAW30
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Streptococcus pneumoniae
-
 Bacillus anthracis

Synonyms

Synonyms Comment Organism
BaPlsY1
-
 Bacillus anthracis
SpPlsY
-
 Streptococcus pneumoniae

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.011
-
 pH 7.4, 37°C Streptococcus pneumoniae (Z)-1-oxooctadec-11-enylphosphoramidic acid
0.02
-
 pH 7.4, 37°C Streptococcus pneumoniae (Z)-1,1-difluoro-2-oxononadec-10-enylphosphonic acid
0.025
-
 pH 7.4, 37°C Bacillus anthracis 1,1-difluoro-2-oxotridecylphosphonic acid
0.035
-
 pH 7.4, 37°C Bacillus anthracis 4-methoxyphenyl palmitoylsulfamate
0.039
-
 pH 7.4, 37°C Streptococcus pneumoniae 1,1-difluoro-2-oxoheptadecylphosphonic acid
0.048
-
 pH 7.4, 37°C Streptococcus pneumoniae (Z)-2-oxononadec-12-enylphosphonic acid
0.05
-
 pH 7.4, 37°C Bacillus anthracis 1,1-difluoro-2-oxoheptadecylphosphonic acid
0.05
-
 pH 7.4, 37°C Bacillus anthracis butyl palmitoylsulfamate
0.06
-
 pH 7.4, 37°C Streptococcus pneumoniae 4-methoxyphenyl palmitoylsulfamate
0.07
-
 pH 7.4, 37°C Streptococcus pneumoniae butyl palmitoylsulfamate
0.08
-
 pH 7.4, 37°C Bacillus anthracis (heptylcarbamoyl)methylphosphonic acid
0.082
-
 pH 7.4, 37°C Streptococcus pneumoniae 1-oxohexadecylphosphoramidic acid
0.085
-
 pH 7.4, 37°C Streptococcus pneumoniae ethyl palmitoylsulfamate
0.09
-
 pH 7.4, 37°C Bacillus anthracis 2-oxoheptadecylphosphonic acid
0.14
-
 pH 7.4, 37°C Bacillus anthracis (Z)-1,1-difluoro-2-oxononadec-10-enylphosphonic acid
0.15
-
 pH 7.4, 37°C Streptococcus pneumoniae (N-dodecyl-N-methylcarbamoyl)methylphosphonic acid
0.2
-
 pH 7.4, 37°C Bacillus anthracis 2-oxo-12-phenoxydodecylphosphonic acid
0.99
-
 pH 7.4, 37°C Bacillus anthracis ethyl palmitoylsulfamate

General Information

General Information Comment Organism
metabolism the enzyme executes an essential step in membrane phospholipid biosynthesis in Gram-positive bacteria Streptococcus pneumoniae
metabolism the enzyme executes an essential step in membrane phospholipid biosynthesis in Gram-positive bacteria Bacillus anthracis