Literature summary for 3.4.22.70 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.

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Inhibitors

Inhibitors	Comment	Organism
1-(3,4-dichlorophenyl)-3-(dimethylamino)propan-1-one	-	Staphylococcus aureus
1-(4-bromophenyl)-3-(3-methylpiperidin-1-yl)propan-1-one	-	Staphylococcus aureus
1-(4-chlorophenyl)-3-morpholin-4-ylpropan-1-one	-	Staphylococcus aureus
1-(4-fluorophenyl)-3-morpholin-4-ylpropan-1-one	-	Staphylococcus aureus
1-(4-methylphenyl)-3-morpholin-4-ylpropan-1-one	-	Staphylococcus aureus
3-(dimethylamino)-1-(2-thienyl)propan-1-one	-	Staphylococcus aureus
3-(dimethylamino)-1-(3-nitrophenyl)propan-1-one	-	Staphylococcus aureus
3-anilino-1-(3-nitrophenyl)propan-1-one	-	Staphylococcus aureus
ethyl 4-[3-(4-bromophenyl)-3-oxopropyl]piperazine-1-carboxylate	-	Staphylococcus aureus
methyl 4-[3-(dimethylamino)propanoyl]benzenesulfinate	-	Staphylococcus aureus
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
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

Organism

Organism	UniProt	Comment	Textmining
Bacillus anthracis	-	-	-
Staphylococcus aureus	-	-	-

Synonyms

Synonyms	Comment	Organism
SrtA	-	Staphylococcus aureus
SrtA	-	Bacillus anthracis

IC50 Value

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