3.4.22.70: sortase A
This is an abbreviated version!
For detailed information about sortase A, go to the full flat file.
Word Map on EC 3.4.22.70
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3.4.22.70
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aureus
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staphylococcus
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lpxtg
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streptococcus
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peptidoglycan
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transpeptidation
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sortase-mediated
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a-mediated
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adhesins
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bioconjugation
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antivirulence
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mutans
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anti-infective
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pilins
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transpeptidases
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oligoglycine
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cross-bridges
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pentaglycine
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wall-anchored
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molecular biology
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azide-alkyne
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analysis
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biotechnology
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drug development
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synthesis
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medicine
- 3.4.22.70
- aureus
- staphylococcus
-
lpxtg
- streptococcus
- peptidoglycan
-
transpeptidation
-
sortase-mediated
-
a-mediated
- adhesins
-
bioconjugation
-
antivirulence
- mutans
-
anti-infective
- pilins
- transpeptidases
-
oligoglycine
-
cross-bridges
- pentaglycine
-
wall-anchored
- molecular biology
-
azide-alkyne
- analysis
- biotechnology
- drug development
- synthesis
- medicine
Reaction
The enzyme catalyses a cell wall sorting reaction in which a surface protein with a sorting signal containing a LPXTG motif is cleaved between the Thr and Gly residue. The resulting threonine carboxyl end of the protein is covalently attached to a pentaglycine cross-bridge of peptidoglycan. =
Synonyms
C60.001, sortase A, sortase A transpeptidase, sortase SrtA, sortase transpeptidase, SrtA, SrtA protein, SrtA sortase
ECTree
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Inhibitors
Inhibitors on EC 3.4.22.70 - sortase A
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(1E)-N'-[(1E)-(4-[(E)-[(diaminomethylene)hydrazono]methyl]phenyl)methylene]ethanehydrazonamide
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(2-(trimethylammonium)ethyl)methanethiosulfonate
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inhibition at 5 mM, inhibition is relieved by supplementing the reaction with 10 mM dithiothreitol
(2E)-2-(2-furoyl)-3-[(methyl[4-[(5-nitropyridin-2-yl)oxy]phenyl]oxido-l4-sulfanylidene)amino]acrylonitrile
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(2E)-3-(2-furyl)-N-[3-(hydroxymethyl)-4-morpholin-4-ylphenyl]acrylamide
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(2E)-3-[(methyl[4-[(5-nitropyridin-2-yl)oxy]phenyl]oxido-l4-sulfanylidene)amino]-2-(2-thienylcarbonyl)acrylonitrile
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(2E)-4-([4-[(2-hydroxybenzoyl)amino]phenyl]amino)-4-oxobut-2-enoic acid
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(2E)-N-[3-(hydroxymethyl)-4-morpholin-4-ylphenyl]-3-(2-thienyl)acrylamide
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(2Z)-3-(2,5-dimethoxyphenyl)-2-(4-methoxyphenyl)acrylonitrile
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IC50: 0.009244 mM
(2Z)-3-(2-methoxyphenyl)-2-(4-methoxyphenyl)acrylonitrile
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IC50: 0.0362 mM
(2Z)-3-(3,4-dimethoxyphenyl)-2-(4-methoxyphenyl)acrylonitrile
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IC50: 0.02296 mM
(2Z)-3-(3,5-dimethoxyphenyl)-2-(4-methoxyphenyl)acrylonitrile
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IC50: 0.025463 mM
(2Z)-3-(3-methoxyphenyl)-2-(4-methoxyphenyl)acrylonitrile
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IC50: 0.0174 mM
(4E)-5-methyl-4-[[(4-nitrophenyl)amino]methylidene]-2-phenyl-2,4-dihydro-3H-pyrazole-3-thione
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(5R)-3,5-bis(6-bromo-1H-indol-3-yl)-5,6-dihydropyrazin-2(1H)-one
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IC50: 68.98 mg/L
(5Z)-3-(2,4-dimethylphenyl)-5-(3-nitrobenzylidene)-2-thioxo-1,3-thiazolidin-4-one
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(5Z)-3-(3-chlorophenyl)-5-(4-methyl-3-nitrobenzylidene)-2-thioxo-1,3-thiazolidin-4-one
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(5Z)-5-(3-bromo-2-hydroxy-5-nitrobenzylidene)-3-(2,4-dimethylphenyl)-2-thioxo-1,3-thiazolidin-4-one
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(5Z)-5-(3-bromo-2-hydroxy-5-nitrobenzylidene)-3-(3-chlorophenyl)-2-thioxo-1,3-thiazolidin-4-one
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(5Z)-5-(3-bromo-2-hydroxy-5-nitrobenzylidene)-3-(3-methylphenyl)-2-thioxo-1,3-thiazolidin-4-one
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(5Z)-5-(3-bromo-2-hydroxy-5-nitrobenzylidene)-3-(4-nitrophenyl)-2-thioxo-1,3-thiazolidin-4-one
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(5Z)-5-(3-bromo-2-hydroxy-5-nitrobenzylidene)-3-phenyl-2-thioxo-1,3-thiazolidin-4-one
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(5Z)-5-(3-bromo-4-hydroxy-5-nitrobenzylidene)-3-(2,4-dimethylphenyl)-2-thioxo-1,3-thiazolidin-4-one
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(5Z)-5-(3-chlorobenzylidene)-3-ethyl-2-thioxo-1,3-thiazolidin-4-one
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(5Z)-5-benzylidene-3-(prop-2-en-1-yl)-2-thioxo-1,3-thiazolidin-4-one
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(6-methyl-1H-inden-3-yl)[4-(6-methyl-1H-indol-3-yl)-1H-imidazol-2-yl]methanone
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IC50: 15.67 mg/Ll
(6R)-3,6-bis(6-bromo-1H-indol-3-yl)-5,6-dihydropyrazin-2(1H)-one
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IC50: 86.34 mg/L
(6R)-6-(6-bromo-1H-indol-3-yl)-3-(1H-indol-3-yl)-5,6-dihydropyrazin-2(1H)-one
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IC50: 34.04 mg/L
(Z)-3-(2,5-dimethoxyphenyl)-2-(4-methoxyphenyl) acrylonitrile
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potential of this inhibitor for the treatment of Staphylococcus aureus infections
2-(3,5-dichlorophenyl)-4-(ethylsulfanyl)-5-sulfanylpyridazin-3(2H)-one
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2-(3-oxo-1,2-benzothiazol-2(3H)-yl)-N-(tricyclo[3.3.1.13,7]dec-1-yl)acetamide
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2-hydroxy-N-[4-[([[(4-methylphenyl)sulfonyl]amino]carbonyl)amino]phenyl]benzamide
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2-morpholin-4-yl-5-[[(2E)-3-(2-thienyl)prop-2-enoyl]amino]benzamide
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3,3,3-trifluoro-1-(phenylsulfonyl)-1-propene
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IC50: 0.19 mM, irreversible
3,5-bis[[2-(4-nitrophenyl)-2-oxoethyl]thio]isothiazole-4-carbonitrile
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5-[[(2E)-3-(2-furyl)prop-2-enoyl]amino]-2-morpholin-4-ylbenzoic acid
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benzyloxycarbonyl-Leu-Pro-Ala-Thr-CH2Cl
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irreversible inhibitor of recombinant enzyme
benzyloxycarbonyl-Leu-Pro-Ala-Thr-CHN2
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irreversible inhibitor of recombinant enzyme
galangin
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IC50 for recombinant SrtA(DELTA24): 0.123 mM, no antibacterial activity against Staphylococcus aureus
galangin-3-methyl ether
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IC50 for recombinant SrtA(DELTA24): 0.1179 mM, no antibacterial activity against Staphylococcus aureus
iodoacetamide
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active site Cys184 of sortase A can be alkylated by iodoacetamide resulting in irreversible modified enzyme. The selenol and thiol of mutant Sec-sortase and mutant Hcy-sortase are sensitive to alkylation as well
isoaaptamine
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the suppression of fibronectin-binding activity by isoaaptamine highlights its potential for the treatment of Staphylococcus aureus infections via inhibition of SrtA activity
isorhamnetin
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IC50 for recombinant SrtA(DELTA24): 0.05886 mM, no antibacterial activity against Staphylococcus aureus
kaempferol
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IC50 for recombinant SrtA(DELTA24): 0.07794 mM, no antibacterial activity against Staphylococcus aureus
maltol 3-O-(4'-O-p-coumaroyl-6'-O-(3-hydroxy-3-methylglutaroyl))-beta-glucopyranoside
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maltol-3-O-(4'-O-cis-p-coumaroyl-6'-O-(3-hydroxy-3-methylglutaroyl))-beta-glucopyranoside
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methyl (2S,3S,7aS)-2-ethenesulfonyl-5-oxo-3-phenyltetrahydropyrrolizine-7a-carboxylate
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methyl (2S,3S,7aS)-2-ethenesulfonyl-5-oxo-3-pyridin-3-yl-tetrahydropyrrolizine-7a-carboxylate
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methyl (2S,3S,7aS)-3-(3,4-dimethoxyphenyl)-2-ethenesulfonyl-5-oxotetrahydropyrrolizine-7a-carboxylate
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methyl (2S,4S,5S)-4-ethenesulfonyl-2-(2-methoxycarbonylethyl)-5-pyridin-3-yl-pyrrolidine-2-carboxylate
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methyl 2-morpholin-4-yl-5-[[(2E)-3-(2-thienyl)prop-2-enoyl]amino]benzoate
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methyl 3-(3-(3-oxobenzo[d]isothiazol-2(3H)-yl)propanamido)adamantane-1-carboxylate
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methyl 3-(3-(4-fluoro-3-oxobenzo[d]isothiazol-2(3H)-yl)propanamido)adamantane-1-carboxylate
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methyl 5-[[(2E)-3-(2-furyl)prop-2-enoyl]amino]-2-morpholin-4-ylbenzoate
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morin
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IC50 for recombinant SrtA(DELTA24): 0.03739 mM, no antibacterial activity against Staphylococcus aureus
myricetin
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IC50 for recombinant SrtA(DELTA24): 0.04403 mM, no antibacterial activity against Staphylococcus aureus
N'-(2-(3-oxobenzo[d]isothiazol-2(3H)-yl)acetyl)adamantane-1-carbohydrazide
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N'-(3-(3-oxobenzo[d]isothiazol-2(3H)-yl)propanoyl)adamantane-1-carbohydrazide
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N'-(3-(4-fluoro-3-oxobenzo[d]isothiazol-2(3H)-yl)propanoyl)adamantane-1-carbohydrazide
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N-(3,5-dimethyladamantan-1-yl)-3-(3-oxobenzo[d]isothiazol-2(3H)-yl)acetamide
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N-(3,5-dimethyladamantan-1-yl)-3-(3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
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N-(3,5-dimethyladamantan-1-yl)-3-(4-fluoro-3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
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N-(3-hydroxy-5,7-dimethyladamantan-1-yl)-2-(3-oxobenzo[d]isothiazol-2(3H)-yl)acetamide
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N-(3-hydroxy-5,7-dimethyladamantan-1-yl)-3-(3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
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N-(3-hydroxy-5,7-dimethyladamantan-1-yl)-3-(4-fluoro-3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
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N-(3-hydroxyadamantan-1-yl)-3-(3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
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N-(3-ydroxyadamantan-1-yl)-3-(4-fluoro-3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
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N-(adamantan-1-yl)-3-(4-fluoro-3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
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NH2-YALPE-AlaPsi(PO2H-CH2)Gly-EE-NH2
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nonhydrolyzable phosphinic peptidomimetic inhibitor of SrtA derived from the LPXTG substrate sequence, simple reversible competitive inhibitor
psammaplin A1
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potential of this inhibitor for the treatment of Staphylococcus aureus infections
quercetin
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IC50 for recombinant SrtA(DELTA24): 0.0527 mM, no antibacterial activity against Staphylococcus aureus
quercetin-3,3'-dimethyl ether
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IC50 for recombinant SrtA(DELTA24): 0.05361 mM, no antibacterial activity against Staphylococcus aureus
[2-(trimethylammonium)ethyl]methanethiosulfonate
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the inhibitor interferes with the cleavage of sorting signals at the LPXTG motif
[4-(6-bromo-1H-indol-3-yl)-1H-imidazol-2-yl](1H-indol-3-yl)methanone
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IC50: 19.44 mg/L
[4-(6-bromo-1H-indol-3-yl)-1H-imidazol-2-yl](6-hydroxy-1H-indol-3-yl)methanone
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IC50: 16.7 mg/L
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potential of this inhibitor for the treatment of Staphylococcus aureus infections
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potential of this inhibitor for the treatment of Staphylococcus aureus infections
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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
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additional information
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SrtA activity is a prime target for inhibition of Staphylococcus aureus colonization
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additional information
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no inhibition by (3R,6S)-3,6-bis(6-bromo-1H-indol-3-yl)piperazin-2-one and (3R,6S)-3,6-bis(6-bromo-1H-indol-3-yl)piperazin-2-one
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additional information
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no inhibition by phenyl trans-styryl sulfone
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additional information
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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
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additional information
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anti-SrtA serum inhibits Staphylococcus aureus biofilm formation
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additional information
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small molecule library screening, synthesis and analysis of irreversible benzisothiazolinone-based inhibitors of the enzyme, structure-activity relationship, overview. No inhibition by aminoadamantan, methyl 1-aminoadamantan-3-carboxylate, and 2-(1-oxoisoindolin-2-yl)acetic acid. Structure determination of inhibitor 1-SrtA complex using purified recombinant nontagged truncated enzyme mutant variant SrtADELTA59, NMR structure determination and analysis
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additional information
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sortase A inhibitory metabolites from the flowers of Sophora japonica, overview
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