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Literature summary extracted from

  • Maresso, A.W.; Wu, R.; Kern, J.W.; Zhang, R.; Janik, D.; Missiakas, D.M.; Duban, M.; Joachimiak, A.; Schneewind, O.
    Activation of inhibitors by sortase triggers irreversible modification of the active site (2007), J. Biol. Chem., 282, 23129-23139.
    View publication on PubMedView publication on EuropePMC

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
3.4.22.71 SrtB in complex with aryl (beta-amino)ethyl ketone inhibitors. Analysis of the three-dimensional structure ofBacillusanthracissortaseBwithandwithoutinhibitorprovidesinsights into the mechanism of inhibition Bacillus anthracis

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.22.70 1-(3,4-dichlorophenyl)-3-(dimethylamino)propan-1-one
-
Staphylococcus aureus
3.4.22.70 1-(4-bromophenyl)-3-(3-methylpiperidin-1-yl)propan-1-one
-
Staphylococcus aureus
3.4.22.70 1-(4-chlorophenyl)-3-morpholin-4-ylpropan-1-one
-
Staphylococcus aureus
3.4.22.70 1-(4-fluorophenyl)-3-morpholin-4-ylpropan-1-one
-
Staphylococcus aureus
3.4.22.70 1-(4-methylphenyl)-3-morpholin-4-ylpropan-1-one
-
Staphylococcus aureus
3.4.22.70 3-(dimethylamino)-1-(2-thienyl)propan-1-one
-
Staphylococcus aureus
3.4.22.70 3-(dimethylamino)-1-(3-nitrophenyl)propan-1-one
-
Staphylococcus aureus
3.4.22.70 3-anilino-1-(3-nitrophenyl)propan-1-one
-
Staphylococcus aureus
3.4.22.70 ethyl 4-[3-(4-bromophenyl)-3-oxopropyl]piperazine-1-carboxylate
-
Staphylococcus aureus
3.4.22.70 methyl 4-[3-(dimethylamino)propanoyl]benzenesulfinate
-
Staphylococcus aureus
3.4.22.70 additional information aryl (beta-amino)ethyl ketones inhibit sortase enzymes. Inhibition of sortases occurs through an irreversible, covalent modification of their active site cysteine. Sortases specifically activate this class of molecules via beta-elimination, generating a reactive olefin intermediate that covalently modifies the cysteine thiol Bacillus anthracis
3.4.22.70 additional information aryl (beta-amino)ethyl ketones inhibit sortase enzymes. Inhibition of sortases occurs through an irreversible, covalent modification of their active site cysteine. Sortases specifically activate this class of molecules via beta-elimination, generating a reactive olefin intermediate that covalently modifies the cysteine thiol Staphylococcus aureus
3.4.22.71 additional information aryl (beta-amino)ethyl ketones inhibit sortase enzymes. Inhibition of sortases occurs through an irreversible, covalent modification of their active site cysteine. Sortases specifically activate this class of molecules via beta-elimination, generating a reactive olefin intermediate that covalently modifies the cysteine thiol Bacillus anthracis

Organism

EC Number Organism UniProt Comment Textmining
3.4.22.70 Bacillus anthracis
-
-
-
3.4.22.70 Staphylococcus aureus
-
-
-
3.4.22.71 Bacillus anthracis
-
-
-

Synonyms

EC Number Synonyms Comment Organism
3.4.22.70 SrtA
-
Staphylococcus aureus
3.4.22.70 SrtA
-
Bacillus anthracis
3.4.22.71 SrtB
-
Bacillus anthracis

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.22.70 0.0472
-
-
Staphylococcus aureus 1-(4-fluorophenyl)-3-morpholin-4-ylpropan-1-one
3.4.22.70 0.0543
-
-
Staphylococcus aureus 3-(dimethylamino)-1-(3-nitrophenyl)propan-1-one
3.4.22.70 0.0548
-
-
Staphylococcus aureus 3-(dimethylamino)-1-(2-thienyl)propan-1-one
3.4.22.70 0.0569
-
-
Staphylococcus aureus 1-(4-bromophenyl)-3-(3-methylpiperidin-1-yl)propan-1-one
3.4.22.70 0.0569
-
-
Staphylococcus aureus 1-(4-methylphenyl)-3-morpholin-4-ylpropan-1-one
3.4.22.70 0.066
-
-
Staphylococcus aureus 3-anilino-1-(3-nitrophenyl)propan-1-one
3.4.22.70 0.0698
-
-
Staphylococcus aureus methyl 4-[3-(dimethylamino)propanoyl]benzenesulfinate
3.4.22.70 0.0802
-
-
Staphylococcus aureus ethyl 4-[3-(4-bromophenyl)-3-oxopropyl]piperazine-1-carboxylate
3.4.22.70 0.0837
-
-
Staphylococcus aureus 1-(4-bromophenyl)-3-(3-methylpiperidin-1-yl)propan-1-one
3.4.22.70 0.0844
-
-
Staphylococcus aureus 1-(4-chlorophenyl)-3-morpholin-4-ylpropan-1-one
3.4.22.70 0.0873
-
-
Staphylococcus aureus 3-anilino-1-(3-nitrophenyl)propan-1-one
3.4.22.70 0.0889
-
-
Staphylococcus aureus 1-(4-methylphenyl)-3-morpholin-4-ylpropan-1-one
3.4.22.70 0.0891
-
-
Staphylococcus aureus 1-(4-fluorophenyl)-3-morpholin-4-ylpropan-1-one
3.4.22.70 0.0896
-
-
Staphylococcus aureus 1-(3,4-dichlorophenyl)-3-(dimethylamino)propan-1-one
3.4.22.70 0.0902
-
-
Staphylococcus aureus 3-(dimethylamino)-1-(3-nitrophenyl)propan-1-one
3.4.22.70 0.0904
-
-
Staphylococcus aureus 1-(3,4-dichlorophenyl)-3-(dimethylamino)propan-1-one
3.4.22.70 0.0906
-
-
Staphylococcus aureus 1-(4-chlorophenyl)-3-morpholin-4-ylpropan-1-one
3.4.22.70 0.0907
-
-
Staphylococcus aureus 3-(dimethylamino)-1-(2-thienyl)propan-1-one
3.4.22.70 0.0907
-
-
Staphylococcus aureus ethyl 4-[3-(4-bromophenyl)-3-oxopropyl]piperazine-1-carboxylate
3.4.22.70 0.0913
-
-
Staphylococcus aureus methyl 4-[3-(dimethylamino)propanoyl]benzenesulfinate