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Literature summary for 6.1.1.20 extracted from

  • Pohlmann, J.
    Phenylalanyl-tRNA synthetase as a target for potential new antibacterial agents (2004), Drugs Future, 29, 243-251.
No PubMed abstract available
Search for more literature for 6.1.1.20

Inhibitors

Inhibitors Comment Organism Structure
(2R,3R,3aS,5aR,10R,10aR)-N-(3,4-dichlorophenyl)-10-hydroxy-4-oxo-2-phenyl-2,3,3a,4,5a,10-hexahydrofuro[2,3-c]indeno[1,2-b]furan-3-carboxamide
-
 Escherichia coli
(2R,3R,3aS,5aR,10S,10aR)-N-(3,4-dichlorophenyl)-10-hydroxy-4-oxo-2-phenyl-2,3,3a,4,5a,10-hexahydrofuro[2,3-c]indeno[1,2-b]furan-3-carboxamide
-
 Escherichia coli
(2Z)-2-(cyclopropylimino)-3-(2-thienylmethyl)-1,3-thiazolidin-4-one competitive with respect to Phe, selective for bacterial Phe-RS versus human Phe-RS, IC50: 0.002 mM Enterococcus faecalis
(2Z)-2-(cyclopropylimino)-3-(2-thienylmethyl)-1,3-thiazolidin-4-one competitive with respect to Phe, selective for bacterial Phe-RS versus human Phe-RS, IC50: 0.00017 mM Escherichia coli
(2Z)-2-(cyclopropylimino)-3-(2-thienylmethyl)-1,3-thiazolidin-4-one competitive with respect to Phe, selective for bacterial Phe-RS versus human Phe-RS, IC50: 0.0016 mM Staphylococcus aureus
(2Z)-2-[(3-chlorophenyl)imino]-3-(2-thienylmethyl)-1,3-thiazolidin-4-one IC50: 600 nM Enterococcus faecalis
(2Z)-2-[(3-chlorophenyl)imino]-3-(2-thienylmethyl)-1,3-thiazolidin-4-one IC50: 10 nM Escherichia coli
(2Z)-2-[(3-chlorophenyl)imino]-3-(2-thienylmethyl)-1,3-thiazolidin-4-one IC50: 70 nM Staphylococcus aureus
(3R,3aR,6aS)-5-(3,4-dichlorophenyl)-3-phenyl-3a,6a-dihydrospiro[furo[3,4-c]pyrrole-1,2'-indene]-1',3',4,6(3H,5H)-tetrone IC50: 5 nM Enterococcus faecalis
(3R,3aR,6aS)-5-(3,4-dichlorophenyl)-3-phenyl-3a,6a-dihydrospiro[furo[3,4-c]pyrrole-1,2'-indene]-1',3',4,6(3H,5H)-tetrone IC50: 130 nM Escherichia coli
(3R,3aR,6aS)-5-(3,4-dichlorophenyl)-3-phenyl-3a,6a-dihydrospiro[furo[3,4-c]pyrrole-1,2'-indene]-1',3',4,6(3H,5H)-tetrone IC50: 4 nM Staphylococcus aureus
(3S,3aR,6aS)-5-(3,4-dichlorophenyl)-3-phenyl-3a,6a-dihydrospiro[furo[3,4-c]pyrrole-1,2'-indene]-1',3',4,6(3H,5H)-tetrone IC50: 820 nM Enterococcus faecalis
(3S,3aR,6aS)-5-(3,4-dichlorophenyl)-3-phenyl-3a,6a-dihydrospiro[furo[3,4-c]pyrrole-1,2'-indene]-1',3',4,6(3H,5H)-tetrone IC50: 3200 nM Escherichia coli
1-(3-[[4-(3,5-dichlorophenyl)piperazin-1-yl]sulfonyl]phenyl)-3-(1,3-thiazol-2-yl)urea IC50: 15 nM Escherichia coli
1-(3-[[4-(3,5-dichlorophenyl)piperazin-1-yl]sulfonyl]phenyl)-3-(1,3-thiazol-2-yl)urea IC50: 15 nM Haemophilus influenzae
1-(3-[[4-(3,5-dichlorophenyl)piperazin-1-yl]sulfonyl]phenyl)-3-(1,3-thiazol-2-yl)urea IC50: 50 nM Streptococcus pneumoniae
2-phenylacetamidine competitive with respect to phenylalanine Escherichia coli
benzylguanidine competitive with respect to phenylalanine Escherichia coli
L-phenylalanyl-adenylate
-
 Escherichia coli
N-benzyl-D-amphetamine most potent competitive inhibitor, selectivity for bacterial enzyme Escherichia coli
N-benzylbenzamidine competitive with respect to phenylalanine Escherichia coli
N-[2-(1H-indol-3-yl)ethyl]-3-[(1,3-thiazol-2-ylcarbamoyl)amino]benzenesulfonamide IC50: 8 nM Escherichia coli
N-[2-(1H-indol-3-yl)ethyl]-3-[(1,3-thiazol-2-ylcarbamoyl)amino]benzenesulfonamide IC50: 8 nM Haemophilus influenzae
N-[2-(1H-indol-3-yl)ethyl]-3-[(1,3-thiazol-2-ylcarbamoyl)amino]benzenesulfonamide IC50: 50 nM Staphylococcus aureus
ochratoxin A
-
 Escherichia coli

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.05
-
 L-Phe
-
 Staphylococcus aureus
0.05
-
 L-Phe
-
 Haemophilus influenzae
0.05
-
 L-Phe
-
 Escherichia coli
0.05
-
 L-Phe
-
 Enterococcus faecalis
0.05
-
 L-Phe
-
 Streptococcus pneumoniae

Organism

Organism UniProt Comment Textmining
Enterococcus faecalis
-
-
-
Escherichia coli
-
-
-
Haemophilus influenzae
-
-
-
Staphylococcus aureus
-
-
-
Streptococcus pneumoniae
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + L-Phe + tRNAPhe
-
 Enterococcus faecalis AMP + diphosphate + L-phenylalanyl-tRNAPhe
-
 ?
ATP + L-phenylalanine + tRNAPhe
-
 Staphylococcus aureus AMP + diphosphate + L-phenylalanyl-tRNAPhe
-
 ?
ATP + L-phenylalanine + tRNAPhe
-
 Haemophilus influenzae AMP + diphosphate + L-phenylalanyl-tRNAPhe
-
 ?
ATP + L-phenylalanine + tRNAPhe
-
 Streptococcus pneumoniae AMP + diphosphate + L-phenylalanyl-tRNAPhe
-
 ?

Synonyms

Synonyms Comment Organism
Phe-RS
-
 Staphylococcus aureus
Phe-RS
-
 Haemophilus influenzae
Phe-RS
-
 Escherichia coli
Phe-RS
-
 Enterococcus faecalis
Phe-RS
-
 Streptococcus pneumoniae

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00014
-
 N-benzyl-D-amphetamine
-
 Escherichia coli
0.058
-
 N-benzylbenzamidine
-
 Escherichia coli
0.077
-
 benzylguanidine
-
 Escherichia coli
0.23
-
 2-phenylacetamidine
-
 Escherichia coli

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000004
-
 IC50: 4 nM Staphylococcus aureus (3R,3aR,6aS)-5-(3,4-dichlorophenyl)-3-phenyl-3a,6a-dihydrospiro[furo[3,4-c]pyrrole-1,2'-indene]-1',3',4,6(3H,5H)-tetrone
0.000005
-
 IC50: 5 nM Enterococcus faecalis (3R,3aR,6aS)-5-(3,4-dichlorophenyl)-3-phenyl-3a,6a-dihydrospiro[furo[3,4-c]pyrrole-1,2'-indene]-1',3',4,6(3H,5H)-tetrone
0.000008
-
 IC50: 8 nM Haemophilus influenzae N-[2-(1H-indol-3-yl)ethyl]-3-[(1,3-thiazol-2-ylcarbamoyl)amino]benzenesulfonamide
0.000008
-
 IC50: 8 nM Escherichia coli N-[2-(1H-indol-3-yl)ethyl]-3-[(1,3-thiazol-2-ylcarbamoyl)amino]benzenesulfonamide
0.00001
-
 IC50: 10 nM Escherichia coli (2Z)-2-[(3-chlorophenyl)imino]-3-(2-thienylmethyl)-1,3-thiazolidin-4-one
0.000015
-
 IC50: 15 nM Haemophilus influenzae 1-(3-[[4-(3,5-dichlorophenyl)piperazin-1-yl]sulfonyl]phenyl)-3-(1,3-thiazol-2-yl)urea
0.000015
-
 IC50: 15 nM Escherichia coli 1-(3-[[4-(3,5-dichlorophenyl)piperazin-1-yl]sulfonyl]phenyl)-3-(1,3-thiazol-2-yl)urea
0.00005
-
 IC50: 50 nM Staphylococcus aureus N-[2-(1H-indol-3-yl)ethyl]-3-[(1,3-thiazol-2-ylcarbamoyl)amino]benzenesulfonamide
0.00005
-
 IC50: 50 nM Streptococcus pneumoniae 1-(3-[[4-(3,5-dichlorophenyl)piperazin-1-yl]sulfonyl]phenyl)-3-(1,3-thiazol-2-yl)urea
0.00007
-
 IC50: 70 nM Staphylococcus aureus (2Z)-2-[(3-chlorophenyl)imino]-3-(2-thienylmethyl)-1,3-thiazolidin-4-one
0.00013
-
 IC50: 130 nM Escherichia coli (3R,3aR,6aS)-5-(3,4-dichlorophenyl)-3-phenyl-3a,6a-dihydrospiro[furo[3,4-c]pyrrole-1,2'-indene]-1',3',4,6(3H,5H)-tetrone
0.00017
-
 competitive with respect to Phe, selective for bacterial Phe-RS versus human Phe-RS, IC50: 0.00017 mM Escherichia coli (2Z)-2-(cyclopropylimino)-3-(2-thienylmethyl)-1,3-thiazolidin-4-one
0.0006
-
 IC50: 600 nM Enterococcus faecalis (2Z)-2-[(3-chlorophenyl)imino]-3-(2-thienylmethyl)-1,3-thiazolidin-4-one
0.00082
-
 IC50: 820 nM Enterococcus faecalis (3S,3aR,6aS)-5-(3,4-dichlorophenyl)-3-phenyl-3a,6a-dihydrospiro[furo[3,4-c]pyrrole-1,2'-indene]-1',3',4,6(3H,5H)-tetrone
0.0016
-
 competitive with respect to Phe, selective for bacterial Phe-RS versus human Phe-RS, IC50: 0.0016 mM Staphylococcus aureus (2Z)-2-(cyclopropylimino)-3-(2-thienylmethyl)-1,3-thiazolidin-4-one
0.002
-
 competitive with respect to Phe, selective for bacterial Phe-RS versus human Phe-RS, IC50: 0.002 mM Enterococcus faecalis (2Z)-2-(cyclopropylimino)-3-(2-thienylmethyl)-1,3-thiazolidin-4-one
0.0032
-
 IC50: 3200 nM Escherichia coli (3S,3aR,6aS)-5-(3,4-dichlorophenyl)-3-phenyl-3a,6a-dihydrospiro[furo[3,4-c]pyrrole-1,2'-indene]-1',3',4,6(3H,5H)-tetrone