Information on EC 3.4.22.70 - sortase A

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The expected taxonomic range for this enzyme is: Bacteria

EC NUMBER
COMMENTARY hide
3.4.22.70
-
RECOMMENDED NAME
GeneOntology No.
sortase A
-
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
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.
show the reaction diagram
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of peptide bond
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CAS REGISTRY NUMBER
COMMENTARY hide
9033-39-0
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ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
-
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Manually annotated by BRENDA team
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-
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Manually annotated by BRENDA team
-
-
-
Manually annotated by BRENDA team
strain ATCC25923
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Manually annotated by BRENDA team
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-
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Manually annotated by BRENDA team
strain Newman
-
-
Manually annotated by BRENDA team
Staphylococcus aureus Newman D2C
gene srtA
-
-
Manually annotated by BRENDA team
-
-
-
Manually annotated by BRENDA team
gene srtA
UniProt
Manually annotated by BRENDA team
gene srtA
UniProt
Manually annotated by BRENDA team
(serotype 2)
-
-
Manually annotated by BRENDA team
(serotype 4)
-
-
Manually annotated by BRENDA team
strain SF370
UniProt
Manually annotated by BRENDA team
strain SF370
UniProt
Manually annotated by BRENDA team
serotype 2
-
-
Manually annotated by BRENDA team
ATCC BAA-854/0140J
UniProt
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
physiological function
additional information
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
2-aminobenzoyl-LPATG-diaminopropionic acid + H2O
2-aminobenzoyl-LPAT + G-diaminopropionic acid
show the reaction diagram
-
efficient cleavage
-
-
?
2-aminobenzoyl-LPETG-diaminopropionic acid +
?
show the reaction diagram
-
-
-
-
?
2-aminobenzoyl-LPETG-diaminopropionic acid + Gly5
?
show the reaction diagram
-
-
-
-
?
2-aminobenzoyl-LPETG-diaminopropionic acid + H2O
2-aminobenzoyl-LPET + G-diaminopropionic acid
show the reaction diagram
-
cleavage between the threonine and the glycine residues, efficient cleavage
-
-
?
2-aminobenzoyl-LPETG-diaminopropionic acid + H2O
?
show the reaction diagram
-
evidence for a reverse protonation catalytic mechanism
-
-
?
2-aminobenzoyl-LPNTA-diaminopropionic acid + H2O
2-aminobenzoyl-LPNT + A-diaminopropionic acid
show the reaction diagram
-
small amount of cleavage
-
-
?
4-([4-(dimethylamino)phenyl]-azo)-benzoyl-QALPETGEE-((2-aminoethyl)-amino)naphthalene-1-sulfonic acid + H2O
?
show the reaction diagram
-
a catalytically important and conserved binding surface is formed by residues A118, T180 and I182. R197 is also required for catalysis
-
-
?
4-[[4'-(dimethylamino)phenyl]azo]-benzoyl-Gln-Ala-Leu-Pro-Glu-Thr-Gly-Glu-Glu-5-[(2'-aminoethyl)-amino]naphthalenesulfonic acid + H2O
4-[[4'-(dimethylamino)phenyl]azo]-benzoyl-Gln-Ala-Leu-Pro-Glu-Thr + Gly-Glu-Glu-5-[(2'-aminoethyl)-amino]naphthalenesulfonic acid
show the reaction diagram
-
-
-
-
?
4-[[4'-(dimethylamino)phenyl]azo]-benzoyl-Leu-Pro-Glu-Thr-Gly-5-[(2'-aminoethyl)-amino]naphthalenesulfonic acid + H2O
4-[[4'-(dimethylamino)phenyl]azo]-benzoyl-Leu-Pro-Glu-Thr + Gly-5-[(2'-aminoethyl)-amino]naphthalenesulfonic acid
show the reaction diagram
-
-
-
-
?
5(6)-carboxyfluorescein-6-aminohexanoic acid-LPKTGGRR-NH2 + H2O
?
show the reaction diagram
-
-
-
-
?
A33-LPETG-His6 + H2O
?
show the reaction diagram
-
A33 antigen extracellular domain bearing a His6 tag
-
-
?
Abz-KVENPQTNAGT-Dap(Dnp)-NH2 + GGGGG
Abz-KVENPQTGGGGG + Gly-Dap(DNP)-NH2
show the reaction diagram
-
-
-
-
?
Abz-LPETG-Dap(Dnp)-NH2 + GGGGG
Abz-LPETGGGGGG + Gly-Dap(Dnp)-NH2
show the reaction diagram
-
-
-
-
?
Abz-LPETG-Dap(Dnp)-NH2 + Gly5
?
show the reaction diagram
-
transpeptidation of LPXTG-containing peptides to the cell-wall precursor mimic NH2-Ala2
-
-
?
Abz-LPETG-Dap(Dnp)-NH2 + Gly5
Abz-LPETGGGGG-OH + Gly-Dap(Dnp)-NH2
show the reaction diagram
-
-
-
-
?
Abz-LPETG-Dap(Dnp)-NH2 + H2O
?
show the reaction diagram
-
-
-
-
?
Abz-LPETGG-Dap(Dnp)-NH2 + Ala-Ala
Abz-LPETAA + GG-Dap(Dnp)-NH2
show the reaction diagram
Abz-LPETGG-Dap(Dnp)-NH2 + GGGGG
Abz-LPETGGGGGG + Gly-Dap(Dnp)-NH2
show the reaction diagram
-
-
-
-
?
Abz-LPKTGK(Dnp)KK + GGGWW
Abz-LPKTGGGWW + GK(Dnp)KK
show the reaction diagram
-
substrate peptide 1 (Abz-LPKTGK(Dnp)KK) and acceptor peptide 2 (GGGWW)
-
-
?
acetyl-ooocctcttacctcagttacaoooLPKTGGR-NH2 + H-GGGKLALKLALKALKAALKLA-NH2
acetyl-ooocctcttacctcagttacaoooLPKTGGGKLALKLALKALKAALKLA-NH2 + H-GGR-NH2
show the reaction diagram
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-
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?
agmatine + YALPETGK
(NH2)2-CN-(CH2)4-NH-(CO)-TEPLAY + ?
show the reaction diagram
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transpeptidase reaction. The initially formed acyl-enzyme intermediate undergoes a hydrolysis followed by intra-molecular transpeptidation
-
-
?
AHLPKTGLR + 5-aminopentan-1-ol
?
show the reaction diagram
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-
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-
?
AHLPKTGLR + 6-aminohexyl 4-O-beta-D-galactopyranosyl-beta-D-glucopyranoside
?
show the reaction diagram
-
-
-
-
?
AHLPKTGLR + N-(2-(2-ethoxyethoxy)ethanamine)biotin amide
?
show the reaction diagram
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-
-
-
?
AHLPKTGLR + N-hexylbiotin amide
?
show the reaction diagram
-
-
-
-
?
AHLPKTGLR-NH2 + triglycine
?
show the reaction diagram
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-
-
-
?
aminobenzoyl-LPETG-diaminopropionic acid + GGGGG
aminobenzoyl-LPETGGGGG + G-diaminopropionic acid
show the reaction diagram
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-
-
-
?
aminobenzoyl-LPETG-diaminopropionic acid + H2O
aminobenzoyl-LPET + G-diaminopropionic acid
show the reaction diagram
-
-
-
-
?
aminobenzoyl-LPETG-diaminopropionyl(dinitrophenyl)-NH2 + GGGGG
?
show the reaction diagram
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-
-
-
?
aminobenzoyl-LPETG-dinitrophenyl ester + Gly-Gly-Gly
aminobenzoyl-LPETGGG + Gly-dinitrophenyl ester
show the reaction diagram
-
HPLC results provide direct evidence for the formation of the kinetically competent acyl enzyme intermediate
-
-
?
Dabcyl-LPETG-EDANS + H2O
Dabcyl-LPET + Gly-EDANS
show the reaction diagram
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-
-
-
?
Dabcyl-QALPETGEE-Edans + H2O
Dabcyl-QALPET + GEE-Edans
show the reaction diagram
Dabcyl-SFLPKTGM-EDANS + H2O
?
show the reaction diagram
Dnp-AQALPETGEE-NH2 + Gly5
?
show the reaction diagram
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-
-
-
?
Dns-LPKTGGRR + GGGWW
Dns-LPKTGGGWW + GGRR
show the reaction diagram
-
dansyl-labeled Dns-LPKTGGRR substrate peptide and acceptor peptide 2 (GGGWW)
-
-
?
GST-LPETG + G-eGFP
?
show the reaction diagram
o-aminobenzoyl-Leu-Pro-Glu-Thr-Gly-2,4-dinitrophenyl ester + Gly-Gly-Gly
o-aminobenzoyl-Leu-Pro-Glu-Thr-Gly-Gly-Gly + Gly-2,4-dinitrophenyl ester
show the reaction diagram
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ping-pong mechanism in which a common acyl-enzyme intermediate is formed in transpeptidation and hydrolysis. The nucleophile binding site of the enzyme is specific for diglycine. The S1' and S2' sites of the sortase both prefer a glycine residue, the S1' site is exclusively selective for glycine
-
-
?
o-aminobenzoyl-Leu-Pro-Glu-Thr-Gly-2,4-dinitrophenyl ester + H2O
o-aminobenzoyl-Leu-Pro-Glu-Thr + Gly-2,4-dinitrophenyl ester
show the reaction diagram
-
ping-pong mechanism in which a common acyl-enzyme intermediate is formed in transpeptidation and hydrolysis. The nucleophile binding site of the enzyme is specific for diglycine. The S1' and S2' sites of the sortase both prefer a glycine residue, the S1' site is exclusively selective for glycine
-
-
?
o-aminobenzoyl-LPETG-2,4-dinitrophenyl + H2O
o-aminobenzoyl-LPETG + 2,4-dinitrophenol
show the reaction diagram
-
-
-
-
?
o-aminobenzoyl-LPETG-2,4-dinitrophenyl ester + H2O
?
show the reaction diagram
-
-
-
-
?
PrtP protein + H2O
?
show the reaction diagram
recombinant Helicobacter pylori R1,3-fucosyltransferase + triglycine
?
show the reaction diagram
-
-
-
-
?
recombinant human beta1,4-galactosyltransferase + N-(2-(2-ethoxyethoxy)ethanamine)biotin amide
?
show the reaction diagram
-
-
-
-
?
recombinant human beta1,4-galactosyltransferase + N-hexylbiotin amide
?
show the reaction diagram
-
-
-
-
?
YALPETGK + H2O
YALPET + Gly-Lys
show the reaction diagram
-
-
-
-
?
YbeF protein + H2O
?
show the reaction diagram
YhgE protein + H2O
?
show the reaction diagram
YndF protein + H2O
?
show the reaction diagram
YwfG protein + H2O
?
show the reaction diagram
[4-(4-dimethylaminophenylazo)benzoic acid]-QALPETGEE-[5-[2'-(aminoethyl)amino]-naphthalenesulfonic acid] + H2O
?
show the reaction diagram
-
-
-
-
?
additional information
?
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NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
additional information
?
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METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Mg2+
-
can substitute in part for Ca2+
Mn2+
-
can substitute in part for Ca2+
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(1E)-N'-[(1E)-(4-[(E)-[(diaminomethylene)hydrazono]methyl]phenyl)methylene]ethanehydrazonamide
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-
(2-(trimethylammonium)ethyl)methanethiosulfonate
-
inibition at 5 mM, inhibition is relieved by supplementing the reaction with 10 mM dithiothreitol
(2-methyl-1H-indol-3-yl)(oxo)acetic acid
-
-
(2-sulfonatoethyl)methanethiosulfonate
-
-
(2E)-2,3-bis(4-methoxyphenyl)acrylamide
-
IC50: 0.476 mM
(2E)-2,3-bis(4-methoxyphenyl)acrylonitrile
-
IC50: 0.187 mM
(2E)-2-(2-furoyl)-3-[(methyl[4-[(5-nitropyridin-2-yl)oxy]phenyl]oxido-l4-sulfanylidene)amino]acrylonitrile
-
-
(2E)-3-(2-furyl)-N-[3-(hydroxymethyl)-4-morpholin-4-ylphenyl]acrylamide
-
-
(2E)-3-[(methyl[4-[(5-nitropyridin-2-yl)oxy]phenyl]oxido-l4-sulfanylidene)amino]-2-(2-thienylcarbonyl)acrylonitrile
-
-
(2E)-4-([4-[(2-hydroxybenzoyl)amino]phenyl]amino)-4-oxobut-2-enoic acid
-
-
(2E)-N-(3-formyl-4-morpholin-4-ylphenyl)-3-(2-furyl)acrylamide
-
-
(2E)-N-(3-formyl-4-morpholin-4-ylphenyl)-3-(2-thienyl)acrylamide
-
-
(2E)-N-[3-(hydroxymethyl)-4-morpholin-4-ylphenyl]-3-(2-thienyl)acrylamide
-
-
(2Z)-2,3-bis(4-methoxyphenyl)acrylonitrile
-
IC50: 0.0279mM
(2Z)-3-(2,5-dimethoxyphenyl)-2-(4-methoxyphenyl)acrylonitrile
-
IC50: 0.009244 mM
(2Z)-3-(2-methoxyphenyl)-2-(4-methoxyphenyl)acrylonitrile
-
IC50: 0.0362 mM
(2Z)-3-(3,4-dimethoxyphenyl)-2-(4-methoxyphenyl)acrylonitrile
-
IC50: 0.02296 mM
(2Z)-3-(3,5-dimethoxyphenyl)-2-(4-methoxyphenyl)acrylonitrile
-
IC50: 0.025463 mM
(2Z)-3-(3-methoxyphenyl)-2-(4-methoxyphenyl)acrylonitrile
-
IC50: 0.0174 mM
(4E)-5-methyl-4-[[(4-nitrophenyl)amino]methylidene]-2-phenyl-2,4-dihydro-3H-pyrazole-3-thione
-
-
(5R)-3,5-bis(6-bromo-1H-indol-3-yl)-5,6-dihydropyrazin-2(1H)-one
-
IC50: 68.98 mg/L
(5Z)-3-(2,4-dimethylphenyl)-5-(3-nitrobenzylidene)-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-3-(3-chlorophenyl)-5-(4-methyl-3-nitrobenzylidene)-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-3-benzyl-5-benzylidene-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-3-ethyl-5-(2-nitrobenzylidene)-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-5-(3-bromo-2-hydroxy-5-nitrobenzylidene)-3-(2,4-dimethylphenyl)-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-5-(3-bromo-2-hydroxy-5-nitrobenzylidene)-3-(3-chlorophenyl)-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-5-(3-bromo-2-hydroxy-5-nitrobenzylidene)-3-(3-methylphenyl)-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-5-(3-bromo-2-hydroxy-5-nitrobenzylidene)-3-(4-nitrophenyl)-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-5-(3-bromo-2-hydroxy-5-nitrobenzylidene)-3-phenyl-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-5-(3-bromo-4-hydroxy-5-nitrobenzylidene)-3-(2,4-dimethylphenyl)-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-5-(3-chlorobenzylidene)-3-ethyl-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-5-benzylidene-3-(prop-2-en-1-yl)-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-5-benzylidene-3-methyl-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-5-benzylidene-3-propyl-2-thioxo-1,3-thiazolidin-4-one
-
-
(6-hydroxy-1H-indol-3-yl)(oxo)acetic acid
-
-
(6-methoxy-1H-indol-3-yl)(oxo)acetic acid
-
-
(6-methyl-1H-inden-3-yl)[4-(6-methyl-1H-indol-3-yl)-1H-imidazol-2-yl]methanone
-
IC50: 15.67 mg/Ll
(6R)-3,6-bis(6-bromo-1H-indol-3-yl)-5,6-dihydropyrazin-2(1H)-one
-
IC50: 86.34 mg/L
(6R)-6-(6-bromo-1H-indol-3-yl)-3-(1H-indol-3-yl)-5,6-dihydropyrazin-2(1H)-one
-
IC50: 34.04 mg/L
(Z)-3-(2,5-dimethoxyphenyl)-2-(4-methoxyphenyl) acrylonitrile
-
potential of this inhibitor for the treatment of Staphylococcus aureus infections
1,2-bis(5-hydroxy-1H-indol-3-yl)ethane-1,2-dione
-
-
1-(3,4-dichlorophenyl)-3-(dimethylamino)propan-1-one
-
-
1-(3-methoxyphenyl)-2,3,4,9-tetrahydro-1H-beta-carboline
-
-
1-(4-bromophenyl)-3-(3-methylpiperidin-1-yl)propan-1-one
-
-
1-(4-chlorophenyl)-3-morpholin-4-ylpropan-1-one
-
-
1-(4-fluorophenyl)-3-morpholin-4-ylpropan-1-one
-
-
1-(4-methoxyphenyl)-2,3,4,9-tetrahydro-1H-beta-carboline
-
-
1-(4-methylphenyl)-3-morpholin-4-ylpropan-1-one
-
-
1-(naphthalen-2-yl)-2,3,4,9-tetrahydro-1H-beta-carboline
-
-
1-pentyl-2,3,4,9-tetrahydro-1H-beta-carboline
-
-
1-phenyl-2,3,4,9-tetrahydro-1H-beta-carbolin-7-ol
-
-
1-phenyl-2,3,4,9-tetrahydro-1H-beta-carboline
-
-
1-phenyl-4,9-dihydro-3H-beta-carboline
-
-
1-[4-(2-aminopyrimidin-4-yl)phenyl]-3-(4-chlorophenyl)urea
-
-
1H-indol-3-yl(oxo)acetic acid
-
-
2,3,4,9-tetrahydro-1H-beta-carboline-1-carboxylic acid
-
-
2-(1-oxoisoindolin-2-yl)acetic acid
-
-
2-(1H-indol-3-yl)-2-oxo-N-phenylacetamide
-
-
2-(2-methyl-1H-indol-3-yl)-2-oxo-N-phenylacetamide
-
-
2-(3,5-dichlorophenyl)-4-(ethylsulfanyl)-5-sulfanylpyridazin-3(2H)-one
-
-
2-(3,5-dichlorophenyl)-5-ethoxy-4-sulfanylpyridazin-3(2H)-one
-
-
2-(3-bromophenyl)-4,5-dichloropyridazin-3(2H)-one
-
-
2-(3-bromophenyl)-4-(ethylsulfanyl)-5-sulfanylpyridazin-3(2H)-one
-
-
2-(3-bromophenyl)-4-chloro-5-ethoxypyridazin-3(2H)-one
-
-
2-(3-bromophenyl)-5-chloro-4-ethoxypyridazin-3(2H)-one
-
-
2-(3-bromophenyl)-5-chloro-4-methoxypyridazin-3(2H)-one
-
-
2-(3-chlorophenyl)-4-methoxy-5-sulfanylpyridazin-3(2H)-one
-
-
2-(3-oxo-1,2-benzothiazol-2(3H)-yl)-N-(tricyclo[3.3.1.13,7]dec-1-yl)acetamide
-
-
2-(4-nitrophenyl)-4,5-dichloropyridazin-3-one
-
-
2-(6-hydroxy-1H-indol-3-yl)-2-oxo-N-phenylacetamide
-
-
2-(6-methoxy-1H-indol-3-yl)-2-oxo-N-phenylacetamide
-
-
2-cyclohexyl-4-(ethylsulfanyl)-5-sulfanylpyridazin-3(2H)-one
-
-
2-ethyl-4-hydroxy-5-(methylsulfanyl)pyridazin-3(2H)-one
-
-
2-hydroxy-1-(5-hydroxy-1H-indol-3-yl)ethanone
-
-
2-hydroxy-N-[4-[([[(4-methylphenyl)sulfonyl]amino]carbonyl)amino]phenyl]benzamide
-
-
2-morpholin-4-yl-5-[[(2E)-3-(2-thienyl)prop-2-enoyl]amino]benzamide
-
-
2-phenyl-4,5-dichloro-pyridazin-3-one
-
-
3,3,3-trifluoro-1-(phenylsulfonyl)-1-propene
-
IC50: 0.19 mM, irreversible
3,5-bis[[2-(4-nitrophenyl)-2-oxoethyl]thio]isothiazole-4-carbonitrile
-
-
3-(2-aminoethyl)-1H-indol-5-ol
-
-
3-(3-oxo-1,2-benzothiazol-2(3H)-yl)propanoic acid
-
-
3-(dimethylamino)-1-(2-thienyl)propan-1-one
-
-
3-(dimethylamino)-1-(3-nitrophenyl)propan-1-one
-
-
3-anilino-1-(3-nitrophenyl)propan-1-one
-
-
4,5-dichloro-2-(3,5-dichlorophenyl)pyridazin-3(2H)-one
-
-
4,5-dichloro-2-(3-fluorophenyl)pyridazin-3(2H)-one
-
-
4,5-dichloro-2-(3-methylphenyl)pyridazin-3(2H)-one
-
-
4,5-dichloro-2-cyclohexylpyridazin-3(2H)-one
-
-
4-(benzyloxy)-5-hydroxy-2-phenylpyridazin-3(2H)-one
-
-
4-(ethylsulfanyl)-2-(3-fluorophenyl)-5-sulfanylpyridazin-3(2H)-one
-
-
4-(ethylsulfanyl)-2-(3-methylphenyl)-5-sulfanylpyridazin-3(2H)-one
-
-
4-(ethylsulfanyl)-2-(4-nitrophenyl)-5-sulfanylpyridazin-3(2H)-one
-
-
4-(ethylsulfanyl)-2-phenyl-5-sulfanylpyridazin-3(2H)-one
-
-
4-(ethylsulfanyl)-5-hydroxy-2-phenylpyridazin-3(2H)-one
-
-
4-chloro-2-(3,5-dichlorophenyl)-5-ethoxypyridazin-3(2H)-one
-
-
4-chloro-2-cyclohexyl-5-ethoxypyridazin-3(2H)-one
-
-
4-chloro-5-(methylsulfanyl)-2-phenylpyridazin-3(2H)-one
-
-
4-chloro-5-ethoxy-2-(3-fluorophenyl)pyridazin-3(2H)-one
-
-
4-chloro-5-ethoxy-2-(3-methylphenyl)pyridazin-3(2H)-one
-
-
4-chloro-5-ethoxy-2-(4-nitrophenyl)pyridazin-3(2H)-one
-
-
4-chloro-5-ethoxy-2-phenylpyridazin-3-one
-
-
4-ethoxy-2-phenyl-5-sulfanylpyridazin-3(2H)-one
-
-
4-ethoxy-5-(2-pyridyldithio)-2-phenylpyridazin-3-one
-
-
4-ethoxy-5-(methyldithio)-2-phenylpyridazin-3-one
-
-
4-ethoxy-5-mercapto-2-phenylpyridazin-3-one
-
-
4-hydroxy-5-(methylsulfanyl)-2-phenylpyridazin-3(2H)-one
-
-
4-hydroxymercuribenzoate
-
-
5-chloro-2-(3,5-dichlorophenyl)-4-ethoxypyridazin-3(2H)-one
-
-
5-chloro-2-(3,5-dichlorophenyl)-4-methoxypyridazin-3(2H)-one
-
-
5-chloro-2-(3-fluorophenyl)-4-methoxypyridazin-3(2H)-one
-
-
5-chloro-2-cyclohexyl-4-ethoxypyridazin-3(2H)-one
-
-
5-chloro-2-cyclohexyl-4-methoxypyridazin-3(2H)-one
-
-
5-chloro-4-ethoxy-2-(3-fluorophenyl)pyridazin-3(2H)-one
-
-
5-chloro-4-ethoxy-2-(3-methylphenyl)pyridazin-3(2H)-one
-
-
5-chloro-4-ethoxy-2-(4-nitrophenyl)pyridazin-3(2H)-one
-
-
5-chloro-4-ethoxy-2-phenylpyridazin-3-one
-
-
5-chloro-4-methoxy-2-(3-methylphenyl)pyridazin-3(2H)-one
-
-
5-chloro-4-methoxy-2-phenylpyridazin-3(2H)-one
-
-
5-ethoxy-2-(3-fluorophenyl)-4-sulfanylpyridazin-3(2H)-one
-
-
5-ethoxy-2-(3-methylphenyl)-4-sulfanylpyridazin-3(2H)-one
-
-
5-ethoxy-2-phenyl-4-sulfanylpyridazin-3(2H)-one
-
-
5-hydroxy-1H-indole-3-carbaldehyde
-
-
5-hydroxy-4-methoxy-2-phenylpyridazin-3(2H)-one
-
-
5-methoxy-2-phenyl-4-sulfanylpyridazin-3(2H)-one
-
-
5-[[(2E)-3-(2-furyl)prop-2-enoyl]amino]-2-morpholin-4-ylbenzoic acid
-
-
6-hydroxy-2,3,4,9-tetrahydro-1H-beta-carbolin-1-one
-
-
6-hydroxydihydro-beta-carboline
-
-
7-hydroxy-2,3,4,9-tetrahydro-1H-beta-carboline-1-carboxylic acid
-
-
7-methoxy-1-pentyl-2,3,4,9-tetrahydro-1H-beta-carboline
-
-
7-methoxy-1-phenyl-2,3,4,9-tetrahydro-1H-beta-carboline
-
-
7-methoxy-1-phenyl-4,9-dihydro-3H-beta-carboline
-
-
7-methoxy-2,3,4,9-tetrahydro-1H-beta-carboline-1-carboxylic acid
-
-
aminoadamantan
-
-
benzyloxycarbonyl-Leu-Pro-Ala-Thr-CH2Cl
-
irreversible inhibitor of recombinant enzyme
benzyloxycarbonyl-Leu-Pro-Ala-Thr-CHN2
-
irreversible inhibitor of recombinant enzyme
berberine chloride
beta-sitosterol-3-O-glucopyranoside
bis(4-ethoxy-2-phenyl-5-pyridazyl)disulfide
-
-
cis-1,2-bis(phenylsulfonyl)ethylene
-
IC50: 0.00113 mM, irreversible
demethylaaptamine
-
-
demethyloxyaaptamine
-
-
divinyl sulfone
-
IC50: 0.00106 mM, irreversible
ethyl 4-[3-(4-bromophenyl)-3-oxopropyl]piperazine-1-carboxylate
-
-
ethyl vinyl sulfone
-
IC50: 0.00471 mM, irreversible
galangin
-
IC50 for recombinant SrtA(DELTA24): 0.123 mM, no antibacterial activity against Staphylococcus aureus
galangin-3-methyl ether
-
IC50 for recombinant SrtA(DELTA24): 0.1179 mM, no antibacterial activity against Staphylococcus aureus
iodoacetamide
-
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
-
the suppression of fibronectin-binding activity by isoaaptamine highlights its potential for the treatment of Staphylococcus aureus infections via inhibition of SrtA activity
isorhamnetin
-
IC50 for recombinant SrtA(DELTA24): 0.05886 mM, no antibacterial activity against Staphylococcus aureus
isorhamnetin 3-O-beta-D-rutinoside
-
-
-
kaempferol
-
IC50 for recombinant SrtA(DELTA24): 0.07794 mM, no antibacterial activity against Staphylococcus aureus
kaempferol-3-rutinoside
-
-
-
maltol 3-O-(4'-O-p-coumaroyl-6'-O-(3-hydroxy-3-methylglutaroyl))-beta-glucopyranoside
-
-
maltol-3-O-(4'-O-cis-p-coumaroyl-6'-O-(3-hydroxy-3-methylglutaroyl))-beta-glucopyranoside
-
-
methyl (2E)-2,3-bis(4-methoxyphenyl)acrylate
-
IC50: 0.231 mM
methyl (2S,3S,7aS)-2-ethenesulfonyl-5-oxo-3-phenyltetrahydropyrrolizine-7a-carboxylate
-
-
methyl (2S,3S,7aS)-2-ethenesulfonyl-5-oxo-3-pyridin-3-yl-tetrahydropyrrolizine-7a-carboxylate
-
-
methyl (2S,3S,7aS)-3-(3,4-dimethoxyphenyl)-2-ethenesulfonyl-5-oxotetrahydropyrrolizine-7a-carboxylate
-
-
methyl (2S,4S,5S)-4-ethenesulfonyl-2-(2-methoxycarbonylethyl)-5-pyridin-3-yl-pyrrolidine-2-carboxylate
-
-
methyl (2Z)-2,3-bis(4-methoxyphenyl)acrylate
-
IC50: 0.909 mM
methyl (4S,5S)-4-(ethenylsulfonyl)-5-(2-fluorophenyl)-L-prolinate
-
-
methyl (4S,5S)-4-(ethenylsulfonyl)-5-(3-fluorophenyl)-L-prolinate
-
-
methyl (4S,5S)-4-(ethenylsulfonyl)-5-phenyl-L-prolinate
-
-
methyl 1-aminoadamantan-3-carboxylate
-
-
methyl 2-morpholin-4-yl-5-[[(2E)-3-(2-thienyl)prop-2-enoyl]amino]benzoate
-
-
methyl 3-(3-(3-oxobenzo[d]isothiazol-2(3H)-yl)propanamido)adamantane-1-carboxylate
-
-
methyl 3-(3-(4-fluoro-3-oxobenzo[d]isothiazol-2(3H)-yl)propanamido)adamantane-1-carboxylate
-
-
methyl 4-[3-(dimethylamino)propanoyl]benzenesulfinate
-
-
methyl 5-hydroxy-1H-indole-3-carboxylate
-
-
methyl 5-[[(2E)-3-(2-furyl)prop-2-enoyl]amino]-2-morpholin-4-ylbenzoate
-
-
methyl vinyl sulfone
-
IC50: 0.00624 mM, irreversible
morin
-
IC50 for recombinant SrtA(DELTA24): 0.03739 mM, no antibacterial activity against Staphylococcus aureus
myricetin
-
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
-
-
N'-(3-(3-oxobenzo[d]isothiazol-2(3H)-yl)propanoyl)adamantane-1-carbohydrazide
-
-
N'-(3-(4-fluoro-3-oxobenzo[d]isothiazol-2(3H)-yl)propanoyl)adamantane-1-carbohydrazide
-
-
N-(3,5-dimethyladamantan-1-yl)-3-(3-oxobenzo[d]isothiazol-2(3H)-yl)acetamide
-
-
N-(3,5-dimethyladamantan-1-yl)-3-(3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
-
-
N-(3,5-dimethyladamantan-1-yl)-3-(4-fluoro-3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
-
-
N-(3-hydroxy-5,7-dimethyladamantan-1-yl)-2-(3-oxobenzo[d]isothiazol-2(3H)-yl)acetamide
-
-
N-(3-hydroxy-5,7-dimethyladamantan-1-yl)-3-(3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
-
-
N-(3-hydroxy-5,7-dimethyladamantan-1-yl)-3-(4-fluoro-3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
-
-
N-(3-hydroxyadamantan-1-yl)-3-(3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
-
-
N-(3-ydroxyadamantan-1-yl)-3-(4-fluoro-3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
-
-
N-(adamantan-1-yl)-3-(4-fluoro-3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
-
-
N-adamantan-1-yl-3-(3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
-
-
NH2-YALPE-AlaPsi(PO2H-CH2)Gly-EE-NH2
-
nonhydrolyzable phosphinic peptidomimetic inhibitor of SrtA derived from the LPXTG substrate sequence, simple reversible competitive inhibitor
p-hydroxymercuribenzoate
-
-
p-hydroxymercuribenzoic acid
-
-
phenyl vinyl sulfone
psammaplin A1
-
potential of this inhibitor for the treatment of Staphylococcus aureus infections
quercetin
-
IC50 for recombinant SrtA(DELTA24): 0.0527 mM, no antibacterial activity against Staphylococcus aureus
quercetin-3,3'-dimethyl ether
-
IC50 for recombinant SrtA(DELTA24): 0.05361 mM, no antibacterial activity against Staphylococcus aureus
[2-(trimethylammonium)ethyl]methanethiosulfonate
-
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
-
IC50: 19.44 mg/L
[4-(6-bromo-1H-indol-3-yl)-1H-imidazol-2-yl](6-hydroxy-1H-indol-3-yl)methanone
-
IC50: 16.7 mg/L
additional information
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00824 - 0.0168
2-aminobenzoyl-LPETG-diaminopropionic acid
5.5
Abz-LPETG-Dap(Dnp)-NH2
1.18
agmatine
-
at 37C, pH not specified in the publication, transpeptidation reaction
0.79 - 11.2
aminobenzoyl-LPETG-diaminopropionyl(dinitrophenyl)-NH2
4.69 - 13.7
aminobenzoyl-LPETGG-diaminopropionic acid(dinitrophenol)-NH2
0.013 - 0.014
Dabcyl-QALPETGEE-Edans
5.6
Dnp-AQALPETGEE-NH2
-
-
0.041 - 0.2
Gly-Gly-Gly
0.14
Gly5
-
37C, pH 7.5
0.02 - 0.117
o-aminobenzoyl-Leu-Pro-Glu-Thr-Gly-2,4-dinitrophenyl ester
0.035 - 0.038
o-aminobenzoyl-LPETG-2,4-dinitrophenyl
0.00013 - 0.0087
o-aminobenzoyl-LPETG-2,4-dinitrophenyl ester
1.59
YALPETGK
-
at 37C, pH not specified in the publication
additional information
additional information
-
-
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00019 - 0.37
2-aminobenzoyl-LPETG-diaminopropionic acid
0.27
Abz-LPETG-Dap(Dnp)-NH2
0.000019 - 0.78
aminobenzoyl-LPETG-diaminopropionyl(dinitrophenyl)-NH2
0.000628 - 1.13
aminobenzoyl-LPETGG-diaminopropionic acid(dinitrophenol)-NH2
125 - 135
Dabcyl-QALPETGEE-Edans
0.013
Dnp-AQALPETGEE-NH2
Staphylococcus aureus
-
-
0.18
Gly-Gly-Gly
Staphylococcus aureus
-
-
0.0000067 - 0.0000083
o-aminobenzoyl-LPETG-2,4-dinitrophenyl
additional information
additional information
Staphylococcus aureus
-
-
-
kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
9615 - 9642
Dabcyl-QALPETGEE-Edans
0.000183 - 0.000233
o-aminobenzoyl-LPETG-2,4-dinitrophenyl
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00003
4-ethoxy-5-(2-pyridyldithio)-2-phenylpyridazin-3-one
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.0004
4-ethoxy-5-(methyldithio)-2-phenylpyridazin-3-one
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.00000021
benzyloxycarbonyl-Leu-Pro-Ala-Thr-CH2Cl
-
pH 7.5, 37C
0.00000022
benzyloxycarbonyl-Leu-Pro-Ala-Thr-CHN2
-
pH 7.5, 37C
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.275
(1E)-N'-[(1E)-(4-[(E)-[(diaminomethylene)hydrazono]methyl]phenyl)methylene]ethanehydrazonamide
Staphylococcus aureus
-
-
0.133
(2-methyl-1H-indol-3-yl)(oxo)acetic acid
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.476
(2E)-2,3-bis(4-methoxyphenyl)acrylamide
Staphylococcus aureus
-
IC50: 0.476 mM
0.187
(2E)-2,3-bis(4-methoxyphenyl)acrylonitrile
Staphylococcus aureus
-
IC50: 0.187 mM
0.15
(2E)-2-(2-furoyl)-3-[(methyl[4-[(5-nitropyridin-2-yl)oxy]phenyl]oxido-l4-sulfanylidene)amino]acrylonitrile
Staphylococcus aureus
-
-
0.111
(2E)-3-(2-furyl)-N-[3-(hydroxymethyl)-4-morpholin-4-ylphenyl]acrylamide
Staphylococcus aureus
-
-
0.4
(2E)-3-[(methyl[4-[(5-nitropyridin-2-yl)oxy]phenyl]oxido-l4-sulfanylidene)amino]-2-(2-thienylcarbonyl)acrylonitrile
Staphylococcus aureus
-
-
0.125
(2E)-4-([4-[(2-hydroxybenzoyl)amino]phenyl]amino)-4-oxobut-2-enoic acid
Staphylococcus aureus
-
-
0.107
(2E)-N-(3-formyl-4-morpholin-4-ylphenyl)-3-(2-furyl)acrylamide
Staphylococcus aureus
-
-
0.077
(2E)-N-(3-formyl-4-morpholin-4-ylphenyl)-3-(2-thienyl)acrylamide
Staphylococcus aureus
-
-
0.073
(2E)-N-[3-(hydroxymethyl)-4-morpholin-4-ylphenyl]-3-(2-thienyl)acrylamide
Staphylococcus aureus
-
-
0.0279
(2Z)-2,3-bis(4-methoxyphenyl)acrylonitrile
Staphylococcus aureus
-
IC50: 0.0279mM
0.009244
(2Z)-3-(2,5-dimethoxyphenyl)-2-(4-methoxyphenyl)acrylonitrile
Staphylococcus aureus
-
IC50: 0.009244 mM
0.0362
(2Z)-3-(2-methoxyphenyl)-2-(4-methoxyphenyl)acrylonitrile
Staphylococcus aureus
-
IC50: 0.0362 mM
0.02296
(2Z)-3-(3,4-dimethoxyphenyl)-2-(4-methoxyphenyl)acrylonitrile
Staphylococcus aureus
-
IC50: 0.02296 mM
0.025463
(2Z)-3-(3,5-dimethoxyphenyl)-2-(4-methoxyphenyl)acrylonitrile
Staphylococcus aureus
-
IC50: 0.025463 mM
0.0174
(2Z)-3-(3-methoxyphenyl)-2-(4-methoxyphenyl)acrylonitrile
Staphylococcus aureus
-
IC50: 0.0174 mM
0.0052
(4E)-5-methyl-4-[[(4-nitrophenyl)amino]methylidene]-2-phenyl-2,4-dihydro-3H-pyrazole-3-thione
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.119
(5Z)-3-(2,4-dimethylphenyl)-5-(3-nitrobenzylidene)-2-thioxo-1,3-thiazolidin-4-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
1
(5Z)-3-(3-chlorophenyl)-5-(4-methyl-3-nitrobenzylidene)-2-thioxo-1,3-thiazolidin-4-one
Staphylococcus aureus
-
IC50 above 1.0 mM, in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.492
(5Z)-3-benzyl-5-benzylidene-2-thioxo-1,3-thiazolidin-4-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.104
(5Z)-3-ethyl-5-(2-nitrobenzylidene)-2-thioxo-1,3-thiazolidin-4-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.0037
(5Z)-5-(3-bromo-2-hydroxy-5-nitrobenzylidene)-3-(2,4-dimethylphenyl)-2-thioxo-1,3-thiazolidin-4-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.017
(5Z)-5-(3-bromo-2-hydroxy-5-nitrobenzylidene)-3-(3-chlorophenyl)-2-thioxo-1,3-thiazolidin-4-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.015
(5Z)-5-(3-bromo-2-hydroxy-5-nitrobenzylidene)-3-(3-methylphenyl)-2-thioxo-1,3-thiazolidin-4-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.012
(5Z)-5-(3-bromo-2-hydroxy-5-nitrobenzylidene)-3-(4-nitrophenyl)-2-thioxo-1,3-thiazolidin-4-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.014
(5Z)-5-(3-bromo-2-hydroxy-5-nitrobenzylidene)-3-phenyl-2-thioxo-1,3-thiazolidin-4-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.035
(5Z)-5-(3-bromo-4-hydroxy-5-nitrobenzylidene)-3-(2,4-dimethylphenyl)-2-thioxo-1,3-thiazolidin-4-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.109
(5Z)-5-(3-chlorobenzylidene)-3-ethyl-2-thioxo-1,3-thiazolidin-4-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.199
(5Z)-5-benzylidene-3-(prop-2-en-1-yl)-2-thioxo-1,3-thiazolidin-4-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.405
(5Z)-5-benzylidene-3-methyl-2-thioxo-1,3-thiazolidin-4-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.186
(5Z)-5-benzylidene-3-propyl-2-thioxo-1,3-thiazolidin-4-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.0896 - 0.736
1-(3,4-dichlorophenyl)-3-(dimethylamino)propan-1-one
0.0569 - 0.0837
1-(4-bromophenyl)-3-(3-methylpiperidin-1-yl)propan-1-one
0.0844 - 0.0906
1-(4-chlorophenyl)-3-morpholin-4-ylpropan-1-one
0.0472 - 0.0891
1-(4-fluorophenyl)-3-morpholin-4-ylpropan-1-one
0.0569 - 0.0889
1-(4-methylphenyl)-3-morpholin-4-ylpropan-1-one
0.0106
1-phenyl-2,3,4,9-tetrahydro-1H-beta-carbolin-7-ol
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.097
1-phenyl-4,9-dihydro-3H-beta-carboline
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.4
1-[4-(2-aminopyrimidin-4-yl)phenyl]-3-(4-chlorophenyl)urea
Staphylococcus aureus
-
-
0.069
1H-indol-3-yl(oxo)acetic acid
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.174
2-(1H-indol-3-yl)-2-oxo-N-phenylacetamide
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.061
2-(2-methyl-1H-indol-3-yl)-2-oxo-N-phenylacetamide
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.301
2-(3,5-dichlorophenyl)-4-(ethylsulfanyl)-5-sulfanylpyridazin-3(2H)-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.166
2-(3,5-dichlorophenyl)-5-ethoxy-4-sulfanylpyridazin-3(2H)-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.05
2-(3-bromophenyl)-4,5-dichloropyridazin-3(2H)-one
0.0045
2-(3-chlorophenyl)-4-methoxy-5-sulfanylpyridazin-3(2H)-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.00611
2-(3-oxo-1,2-benzothiazol-2(3H)-yl)-N-(tricyclo[3.3.1.13,7]dec-1-yl)acetamide
Staphylococcus aureus
-
pH 7.5, 37C, recombinant His6-tagged truncated enzyme mutant variant SrtADELTA59
0.05
2-(4-nitrophenyl)-4,5-dichloropyridazin-3-one
Staphylococcus aureus
-
IC50 above 0.05 mM, in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.0179
2-cyclohexyl-4-(ethylsulfanyl)-5-sulfanylpyridazin-3(2H)-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.05
2-ethyl-4-hydroxy-5-(methylsulfanyl)pyridazin-3(2H)-one
Staphylococcus aureus
-
IC50 above 0.05 mM, in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.226
2-hydroxy-N-[4-[([[(4-methylphenyl)sulfonyl]amino]carbonyl)amino]phenyl]benzamide
Staphylococcus aureus
-
-
0.105
2-morpholin-4-yl-5-[[(2E)-3-(2-thienyl)prop-2-enoyl]amino]benzamide
Staphylococcus aureus
-
-
0.05
2-phenyl-4,5-dichloro-pyridazin-3-one
Staphylococcus aureus
-
IC50 above 0.05 mM, in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.19
3,3,3-trifluoro-1-(phenylsulfonyl)-1-propene
Staphylococcus aureus
-
IC50: 0.19 mM, irreversible
0.0973
3,5-bis[[2-(4-nitrophenyl)-2-oxoethyl]thio]isothiazole-4-carbonitrile
Staphylococcus aureus
-
-
0.0128
3-(3-oxo-1,2-benzothiazol-2(3H)-yl)propanoic acid
Staphylococcus aureus
-
pH 7.5, 37C, recombinant His6-tagged truncated enzyme mutant variant SrtADELTA75
0.0548 - 0.0907
3-(dimethylamino)-1-(2-thienyl)propan-1-one
0.0543 - 0.0902
3-(dimethylamino)-1-(3-nitrophenyl)propan-1-one
0.066 - 0.0873
3-anilino-1-(3-nitrophenyl)propan-1-one
0.061
4,5-dichloro-2-(3,5-dichlorophenyl)pyridazin-3(2H)-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.05
4,5-dichloro-2-(3-fluorophenyl)pyridazin-3(2H)-one
0.0055
4-(ethylsulfanyl)-2-(3-fluorophenyl)-5-sulfanylpyridazin-3(2H)-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.0033
4-(ethylsulfanyl)-2-(3-methylphenyl)-5-sulfanylpyridazin-3(2H)-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.03
4-(ethylsulfanyl)-2-(4-nitrophenyl)-5-sulfanylpyridazin-3(2H)-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.0014
4-(ethylsulfanyl)-2-phenyl-5-sulfanylpyridazin-3(2H)-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.05
4-(ethylsulfanyl)-5-hydroxy-2-phenylpyridazin-3(2H)-one
0.219
4-chloro-5-ethoxy-2-(4-nitrophenyl)pyridazin-3(2H)-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.001
4-chloro-5-ethoxy-2-phenylpyridazin-3-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.0002
4-ethoxy-2-phenyl-5-sulfanylpyridazin-3(2H)-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.013
4-ethoxy-5-mercapto-2-phenylpyridazin-3-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.05
4-hydroxy-5-(methylsulfanyl)-2-phenylpyridazin-3(2H)-one
Staphylococcus aureus
-
IC50 above 0.05 mM, in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.1125
4-hydroxymercuribenzoate
Streptococcus mutans
-
pH and temperature not specified in the publication
0.05
5-chloro-2-(3,5-dichlorophenyl)-4-ethoxypyridazin-3(2H)-one
0.0057
5-ethoxy-2-(3-fluorophenyl)-4-sulfanylpyridazin-3(2H)-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.0031
5-ethoxy-2-(3-methylphenyl)-4-sulfanylpyridazin-3(2H)-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.0044
5-ethoxy-2-phenyl-4-sulfanylpyridazin-3(2H)-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.05
5-hydroxy-4-methoxy-2-phenylpyridazin-3(2H)-one
Staphylococcus aureus
-
IC50 above 0.05 mM,
0.0093
5-methoxy-2-phenyl-4-sulfanylpyridazin-3(2H)-one
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.181
5-[[(2E)-3-(2-furyl)prop-2-enoyl]amino]-2-morpholin-4-ylbenzoic acid
Staphylococcus aureus
-
-
0.067
6-hydroxydihydro-beta-carboline
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.0115
7-methoxy-1-phenyl-2,3,4,9-tetrahydro-1H-beta-carboline
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.025
7-methoxy-1-phenyl-4,9-dihydro-3H-beta-carboline
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.0015
bis(4-ethoxy-2-phenyl-5-pyridazyl)disulfide
Staphylococcus aureus
-
in 20 mM HEPES, 5 mM CaCl2, 0.05% (v/v) Tween-20, pH 7.5, at 25C
0.00113
cis-1,2-bis(phenylsulfonyl)ethylene
Staphylococcus aureus
-
IC50: 0.00113 mM, irreversible
0.0915
curcumin
Streptococcus mutans
-
pH and temperature not specified in the publication
0.00106
divinyl sulfone
Staphylococcus aureus
-
IC50: 0.00106 mM, irreversible
0.0802 - 0.0907
ethyl 4-[3-(4-bromophenyl)-3-oxopropyl]piperazine-1-carboxylate
0.00471
ethyl vinyl sulfone
Staphylococcus aureus
-
IC50: 0.00471 mM, irreversible
0.123
galangin
Staphylococcus aureus
-
IC50 for recombinant SrtA(DELTA24): 0.123 mM, no antibacterial activity against Staphylococcus aureus
0.1179
galangin-3-methyl ether
Staphylococcus aureus
-
IC50 for recombinant SrtA(DELTA24): 0.1179 mM, no antibacterial activity against Staphylococcus aureus
0.05886
isorhamnetin
Staphylococcus aureus
-
IC50 for recombinant SrtA(DELTA24): 0.05886 mM, no antibacterial activity against Staphylococcus aureus
0.0621
isorhamnetin 3-O-beta-D-rutinoside
Streptococcus mutans
-
pH and temperature not specified in the publication
-
0.07794
kaempferol
Staphylococcus aureus
-
IC50 for recombinant SrtA(DELTA24): 0.07794 mM, no antibacterial activity against Staphylococcus aureus
0.0607
kaempferol-3-rutinoside
Streptococcus mutans
-
pH and temperature not specified in the publication
-
0.0943
maltol 3-O-(4'-O-p-coumaroyl-6'-O-(3-hydroxy-3-methylglutaroyl))-beta-glucopyranoside
Streptococcus mutans
-
pH and temperature not specified in the publication
0.0586
maltol-3-O-(4'-O-cis-p-coumaroyl-6'-O-(3-hydroxy-3-methylglutaroyl))-beta-glucopyranoside
Streptococcus mutans
-
pH and temperature not specified in the publication
0.231
methyl (2E)-2,3-bis(4-methoxyphenyl)acrylate
Staphylococcus aureus
-
IC50: 0.231 mM
2.2
methyl (2S,3S,7aS)-2-ethenesulfonyl-5-oxo-3-phenyltetrahydropyrrolizine-7a-carboxylate
Staphylococcus aureus
-
pH 7.5, 37C
2.47
methyl (2S,3S,7aS)-2-ethenesulfonyl-5-oxo-3-pyridin-3-yl-tetrahydropyrrolizine-7a-carboxylate
Staphylococcus aureus
-
pH 7.5, 37C
2.68
methyl (2S,3S,7aS)-3-(3,4-dimethoxyphenyl)-2-ethenesulfonyl-5-oxotetrahydropyrrolizine-7a-carboxylate
Staphylococcus aureus
-
pH 7.5, 37C
1.86
methyl (2S,4S,5S)-4-ethenesulfonyl-2-(2-methoxycarbonylethyl)-5-pyridin-3-yl-pyrrolidine-2-carboxylate
Staphylococcus aureus
-
pH 7.5, 37C
0.909
methyl (2Z)-2,3-bis(4-methoxyphenyl)acrylate
Staphylococcus aureus
-
IC50: 0.909 mM
1.32
methyl (4S,5S)-4-(ethenylsulfonyl)-5-(2-fluorophenyl)-L-prolinate
Staphylococcus aureus
-
pH 7.5, 37C
1.04
methyl (4S,5S)-4-(ethenylsulfonyl)-5-(3-fluorophenyl)-L-prolinate
Staphylococcus aureus
-
pH 7.5, 37C
0.85
methyl (4S,5S)-4-(ethenylsulfonyl)-5-phenyl-L-prolinate
Staphylococcus aureus
-
pH 7.5, 37C
0.071
methyl 2-morpholin-4-yl-5-[[(2E)-3-(2-thienyl)prop-2-enoyl]amino]benzoate
Staphylococcus aureus
-
-
0.00508
methyl 3-(3-(3-oxobenzo[d]isothiazol-2(3H)-yl)propanamido)adamantane-1-carboxylate
Staphylococcus aureus
-
pH 7.5, 37C, recombinant His6-tagged truncated enzyme mutant variant SrtADELTA66
0.00506
methyl 3-(3-(4-fluoro-3-oxobenzo[d]isothiazol-2(3H)-yl)propanamido)adamantane-1-carboxylate
Staphylococcus aureus
-
pH 7.5, 37C, recombinant His6-tagged truncated enzyme mutant variant SrtADELTA71
0.0698 - 0.0913
methyl 4-[3-(dimethylamino)propanoyl]benzenesulfinate
0.058
methyl 5-[[(2E)-3-(2-furyl)prop-2-enoyl]amino]-2-morpholin-4-ylbenzoate
Staphylococcus aureus
-
-
0.00624
methyl vinyl sulfone
Staphylococcus aureus
-
IC50: 0.00624 mM, irreversible
0.03739
morin
Staphylococcus aureus
-
IC50 for recombinant SrtA(DELTA24): 0.03739 mM, no antibacterial activity against Staphylococcus aureus
0.04403
myricetin
Staphylococcus aureus
-
IC50 for recombinant SrtA(DELTA24): 0.04403 mM, no antibacterial activity against Staphylococcus aureus
0.0038
N'-(2-(3-oxobenzo[d]isothiazol-2(3H)-yl)acetyl)adamantane-1-carbohydrazide
Staphylococcus aureus
-
pH 7.5, 37C, recombinant His6-tagged truncated enzyme mutant variant SrtADELTA72
0.00422
N'-(3-(3-oxobenzo[d]isothiazol-2(3H)-yl)propanoyl)adamantane-1-carbohydrazide
Staphylococcus aureus
-
pH 7.5, 37C, recombinant His6-tagged truncated enzyme mutant variant SrtADELTA73
0.00339
N'-(3-(4-fluoro-3-oxobenzo[d]isothiazol-2(3H)-yl)propanoyl)adamantane-1-carbohydrazide
Staphylococcus aureus
-
pH 7.5, 37C, recombinant His6-tagged truncated enzyme mutant variant SrtADELTA74
0.00499
N-(3,5-dimethyladamantan-1-yl)-3-(3-oxobenzo[d]isothiazol-2(3H)-yl)acetamide
Staphylococcus aureus
-
pH 7.5, 37C, recombinant His6-tagged truncated enzyme mutant variant SrtADELTA60
0.00462
N-(3,5-dimethyladamantan-1-yl)-3-(3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
Staphylococcus aureus
-
pH 7.5, 37C, recombinant His6-tagged truncated enzyme mutant variant SrtADELTA63
0.0041
N-(3,5-dimethyladamantan-1-yl)-3-(4-fluoro-3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
Staphylococcus aureus
-
pH 7.5, 37C, recombinant His6-tagged truncated enzyme mutant variant SrtADELTA68
0.00387
N-(3-hydroxy-5,7-dimethyladamantan-1-yl)-2-(3-oxobenzo[d]isothiazol-2(3H)-yl)acetamide
Staphylococcus aureus
-
pH 7.5, 37C, recombinant His6-tagged truncated enzyme mutant variant SrtADELTA61
0.00706
N-(3-hydroxy-5,7-dimethyladamantan-1-yl)-3-(3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
Staphylococcus aureus
-
pH 7.5, 37C, recombinant His6-tagged truncated enzyme mutant variant SrtADELTA64
0.00396
N-(3-hydroxy-5,7-dimethyladamantan-1-yl)-3-(4-fluoro-3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
Staphylococcus aureus
-
pH 7.5, 37C, recombinant His6-tagged truncated enzyme mutant variant SrtADELTA69
0.00644
N-(3-hydroxyadamantan-1-yl)-3-(3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
Staphylococcus aureus
-
pH 7.5, 37C, recombinant His6-tagged truncated enzyme mutant variant SrtADELTA65
0.00626
N-(3-ydroxyadamantan-1-yl)-3-(4-fluoro-3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
Staphylococcus aureus
-
pH 7.5, 37C, recombinant His6-tagged truncated enzyme mutant variant SrtADELTA70
0.00401
N-(adamantan-1-yl)-3-(4-fluoro-3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
Staphylococcus aureus
-
pH 7.5, 37C, recombinant His6-tagged truncated enzyme mutant variant SrtADELTA67
0.00381
N-adamantan-1-yl-3-(3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
Staphylococcus aureus
-
pH 7.5, 37C, recombinant His6-tagged truncated enzyme mutant variant SrtADELTA62
0.042
p-hydroxymercuribenzoic acid
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.0169 - 0.736
phenyl vinyl sulfone
0.0527
quercetin
Staphylococcus aureus
-
IC50 for recombinant SrtA(DELTA24): 0.0527 mM, no antibacterial activity against Staphylococcus aureus
0.05361
quercetin-3,3'-dimethyl ether
Staphylococcus aureus
-
IC50 for recombinant SrtA(DELTA24): 0.05361 mM, no antibacterial activity against Staphylococcus aureus
additional information
additional information
Staphylococcus aureus
-
IC50 for aaptamine is 0.0235 mg/ml, IC50 for isoaaptamine is 0.0037 mg/ml, IC50 for demethylaaptamine is 0.0172 mg/ml, IC50 for demethyloxyaaptamine is 0.0201 mg/ml, IC50 for berberine chloride is 0.0087 mg/ml
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
8.5 - 9
-
wild-type enzyme
pH RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
5.5 - 9.5
-
mutant Sec-sortase enzyme, activity range, profile overview
6.5 - 11
-
wild-type enzyme, activity range, profile overview
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
additional information
-
kidney of Mus musculus infected with Staphylococcus aureus. mRNA levels of sortase A decrease over time, from day 3 of infection to day 14. The transcript number of srtA decreases faster in septic mice than in mice with a non-septic disease
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
PDB
SCOP
CATH
ORGANISM
UNIPROT
Clostridium perfringens (strain 13 / Type A)
Streptococcus pneumoniae (strain ATCC BAA-255 / R6)
Streptococcus pneumoniae (strain ATCC BAA-255 / R6)
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
17800
-
SDS-PAGE
23000
-
SDS-PAGE, immune-reactive species
additional information
-
signal peptide, membrane anchor and a shorter linker domain of sortase enzymes display no amino acid conservation. The core residue, SrtA residues 60-206, is present in all sortase homologs examined, suggesting that this domain may comprise the catalytically active domain
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
monomer
-
the dimeric form of SrtA is more active than the monomeric enzyme
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
crystals are grown by the hanging-drop technique with a protein concentration of 50 mg/ml in 25 mM MES buffer, pH 6.35. The crystallization conditions include 3.2 M ammonium sulfate, 0.1 M NaCl, and trace amounts of ethylene glycol. Crystal structure of native SrtA, of an active-site mutant of SrtA, and of the mutant SrtA complexed with its substrate LPETG peptide
-
wild-type enzyme SrtA apo and mutant enzyme C184A bound to LPETG peptide sequence, crystal structure analysis
hanging drop method of vapor diffusion at 20C, SrtA residues Val82-Thr249 (catalytic domain)
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
by Ni-NTA affinity chromatography
-
His-Trap column chromatography
HisTrapHP column chromatography, gel filtration
-
HiTrap Chelating HP column chromatography and Superdex 75 gel filtration
-
N-terminally His6-tagged SrtADELTAN24 expressed in Escherichia coli BL21
-
Ni-NTA column chromatography
-
Ni2+-HisTrap column chromatography
-
of SrtADELTAN59 and mutant proteins
-
purification of SrtADELTAN59 and SrtA wild-type proteins
-
recombinant enzyme, SrtA residues Val82-Thr249 (catalytic domain)
recombinant His-tagged wild-type and mutant enzymes from Escherichia coli strain BL21(DE3) by nickel affinity chromaatography and dialysis
-
recombinant His6-tagged enzyme catalytic domain from Escherichia coli strain BL21(DE3) by immobilized metal affinity chromatograph
-
recombinant mutant and modified enzymes from Escherichia coli by cation and anion exchange chromatography
-
recombinant nontagged truncated enzyme mutant variant SrtADELTA59 from Escherichia coli strain BL21(DE3) by cation and anion exchange chromatography, dialysis, and gel filtration, recombinant His6-tagged truncated enzyme mutant variant SrtADELTA59 from Escherichia coli strain BL21(DE3) by nickel affinity chromatography and gel filtration
-
recombinant sortase A-GST fusion protein
-
recombinant SrtA lacking the amino-terminal 24 amino acids
-
recombinant SrtADELTAN24 in a His6-tagged form
-
Talon His-affinity resin column chromatography and Sephacryl-100 gel filtration
-
Talon resin column chromatography
-
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
cloned into the plasmid vector pQE30
-
DNA sequence encoding SrtA residues Val82-Thr249, expression in Escherichia coli BL21
expressed in Escherichia coli BL21 cells
-
expressed in Escherichia coli BL21(DE3) cells
expression in Escherichia coli
-
expression of SrtADELTAN24 in a His6-tagged form
-
gene srtA, DNA and amino acid sequence determination and analysis, sequence comparisons and phylogenetic tree
gene srtA, recombinant expression of His6-tagged enzyme catalytic domain, comprising residues 60-206, in Escherichia coli strain BL21(DE3)
-
mutant enzymes expressed in Escherichia coli
-
N-terminally His6-tagged SrtA lacking the amino-terminal 24 amino acids is expressed in BL21(DE3) cells containing the plasmid pET15bSrtADN24
-
N-terminally His6-tagged SrtADELTAN24 is expressed in Escherichia coli BL21
-
overexpression in Escherichia coli
-
recombinant expression of His-tagged wild-type and mutant enzymes in Escherichia coli strain BL21(DE3)
-
recombinant expression of His6-tagged and of nontagged truncated enzyme mutant variant SrtADELTA59 in Escherichia coli strain BL21(DE3)
-
recombinant expression of linear truncated enzyme mutant LsrtADELTA59 in Escherichia coli strain BL21(DE3), development of an expression system in Escherichia coli that allows production of circularly closed sortase A truncated mutant CsrtADELTA59, overview. Efficient enzyme cyclization is achieved by Synechocystis sp. PCC6803 intein-mediated post-translational splicing, NMR spectroscopy of 15N-labeled LsrtADELTAN59 and CsrtADELTAN59
-
recombinant mature sortase A (without the N-terminal signal peptide) is produced as GST fusion in Escherichia coli
-
SrtADELTA24 is expressed in Escherichia coli
-
wild-type and variant SrtA proteins
-
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
H126A
-
inactive
C184Hcy
-
site-directed mutagenesis, generation of a sortase mutant with Cys184 replaced by homocysteine (Hcy). Mutant Hcy-sortase is a poor catalyst with less than 1% of wild-type activity. The sensitivity of the active site nucleophiles towards an alkylation reagent correlates with the pKa values of the mutated residues
C184S
-
2700fold decrease in kcat/Km compared to wild-type value
C184Sec
-
site-directed mutagenesis, generation of a sortase mutant with Cys184 replaced by selenocysteine (Sec). Mutant Sec-sortase shows a moderate 2-3fold reduction in catalytic activity. The sensitivity of the active site nucleophiles towards an alkylation reagent correlates with the pKa values of the mutated residues. The pH-profile of mutant Sec-sortase is shifted to more acidic conditions when compared to the wild-type enzyme
D185A 1.3
-
fold decrease in kcat/Km compared to wild-type value
D186A
-
1.8fold decrease in kcat/Km compared to wild-type value
DELTA N59
E108A
-
turnover-number for o-aminobenzoyl-LPETG-2,4-dinitrophenyl is 43.8fold lower than wild-type value
G167A
-
Tm is 0.5C lower than the Tm-value of wild-type enzyme. No change in kcat/KM compared to wild-type enzyme
H120A
-
96000fold decrease in kcat/Km compared to wild-type value
H120Q
-
36000fold decrease in kcat/Km compared to wild-type value
I123G
-
mutant is generated by using wild type truncated protein SrtADELTAN59 as a template. Mutation reduces dimerization
I182A
-
mutation produces modest decreases in SrtA activity and leds to substrate inhibition. 28fold decrease in kcat/Km compared to wild-type value
I182S
-
74fold decrease in kcat/Km compared to wild-type value
K137A
-
mutant is generated by using wild type truncated protein SrtADELTAN59 as a template. Mutation completely disrupts dimerization
K152A
-
mutant is generated by using wild type truncated protein SrtADELTAN59 as a template. Mutation increases dimerization
K62A
-
mutant is generated by using wild type truncated protein SrtADELTAN59 as a template
L169A
-
Tm is 1.8C lower than the Tm-value of wild-type enzyme. kcat/Km is 93fold lower than wild-type value
L181A
-
mutation produces modest decreases in SrtA activity and leds to substrate inhibition. 7.6fold decrease in kcat/Km compared to wild-type value
N132A
-
mutant is generated by using wild type truncated protein SrtADELTAN59 as a template. Mutation completely disrupts dimerization
N98A
-
kcat/Km is 1.2fold lower than wild-type value
N98Q
-
kcat/Km is 1.1fold higher than wild-type value
P126G
-
mutant is generated by using wild type truncated protein SrtADELTAN59 as a template. Mutation reduces dimerization
Q172A
-
Tm is 1.2C lower than the Tm-value of wild-type enzyme. kcat/Km is 1.4fold lower than wild-type value
R197Cit
-
generation of a semi-synthetic SrtA in which Arg197 is replaced with citrulline, a nonionizable analog. This change results in less than a 3fold decrease in kcat/KM, indicating that Arg197 utilizes a hydrogen bond, rather than an electrostatic interaction. Tm is 0.3C higher than the Tm-value of wild-type enzyme; kcat/Km is 5.9fold lower than wild-type value
R197H
-
kcat/Km is 610fold lower than wild-type value
T180A
-
mutation produces modest decreases in SrtA activity and leds to substrate inhibition. 14fold decrease in kcat/Km compared to wild-type value
T183A
-
1200fold decrease in kcat/Km compared to wild-type value
V168A
-
Tm is 1.7C lower than the Tm-value of wild-type enzyme. kcat/Km is 5.5fold lower than wild-type value
Y143A
-
mutant is generated by using wild type truncated protein SrtADELTAN59 as a template. Mutation completely disrupts dimerization
additional information
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
analysis
biotechnology
-
the bacterial transpeptidase sortase A is a well-established tool in protein chemistry and catalyzes the chemoselective ligation of peptides and proteins
drug development
medicine
molecular biology
synthesis
additional information