6.1.1.4: leucine-tRNA ligase
This is an abbreviated version!
For detailed information about leucine-tRNA ligase, go to the full flat file.
Word Map on EC 6.1.1.4
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6.1.1.4
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aminoacyl-trna
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synthetases
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aminoacylation
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fidelity
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leucylation
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aarss
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mischarged
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post-transfer
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norvaline
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perrault
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anticodon
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aeolicus
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isoacceptors
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misactivated
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aquifex
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ilers
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noncognate
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valrs
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benzoxaborole
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isoleucyl-trna
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misaminoacylated
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hsd17b4
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kmsks
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metrs
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pour
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trnaser
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clinique
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trnaleuuur
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valyl-trna
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isoleucyl
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trna-dependent
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pre-transfer
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drug development
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medicine
- 6.1.1.4
- aminoacyl-trna
- synthetases
- aminoacylation
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fidelity
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leucylation
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aarss
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mischarged
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post-transfer
- norvaline
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perrault
-
anticodon
- aeolicus
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isoacceptors
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misactivated
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aquifex
- ilers
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noncognate
- valrs
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benzoxaborole
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isoleucyl-trna
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misaminoacylated
- hsd17b4
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kmsks
- metrs
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pour
- trnaser
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clinique
- trnaleuuur
- valyl-trna
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isoleucyl
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trna-dependent
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pre-transfer
- drug development
- medicine
Reaction
Synonyms
AaLeuRS, alphabeta-LeuRS, b0642, cytoplasmic LeuRS, EcLeuRS, GlLeuRS, HcleuRS, hs mt LeuRS, JW0637, LARS, LARS1, LARS2, Leucine translase, Leucine--tRNA ligase, Leucyl-transfer ribonucleate synthetase, Leucyl-transfer ribonucleic acid synthetase, Leucyl-transfer RNA synthetase, leucyl-tRNA ligase, leucyl-tRNA syntethase, Leucyl-tRNA synthetase, leucyl-tRNA synthetase 1, leucyl—tRNA synthetase, LeuRS, LeuRS1, LeuRS2, LeuRSTT, leuS, LRS, MmLeuRS, More, mt leucyl-tRNA synthetase, mt-LeuRS, mtLeuRS, PhLeuRS, Synthetase, leucyl-transfer ribonucleate, ycLeuRS
ECTree
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Inhibitors
Inhibitors on EC 6.1.1.4 - leucine-tRNA ligase
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(2E)-3-(1-hydroxy-1,3-dihydro-2,1-benzoxaborol-6-yl)-1-phenylprop-2-en-1-one
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(2E)-3-(1-hydroxy-1,3-dihydro-2,1-benzoxaborol-7-yl)-1-phenylprop-2-en-1-one
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(E)-[3-(1,3-dihydro-1-hydroxy-2,1-benzoxaborol-7-yl)]acrylic acid ethyl ester
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1-[(1-hydroxy-1,3-dihydro-2,1-benzoxaborol-6-yl)oxy]-4-methylpentan-2-one
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2-(2,5-dimethylanilino)-5,6,7,8-tetrahydroquinazolin-4(3H)-one
residual activity compared to wild-type enzyme is 71%
2-(2-hydroxy-5-methylanilino)-3,5,6,7-tetrahydro-4H-cyclopenta[d]pyrimidin-4-one
residual activity compared to wild-type enzyme is 40%
2-(2-hydroxy-5-methylanilino)-6-propylpyrimidin-4(3H)-one
residual activity compared to wild-type enzyme is 93%
2-(2-hydroxy-5-methylanilino)quinazolin-4(3H)-one
residual activity compared to wild-type enzyme is 26%
2-(2-hydroxyanilino)-6-methylpyrimidin-4(3H)-one
residual activity compared to wild-type enzyme is 42%
2-(2-hydroxyanilino)pyrimidin-4(3H)-one
residual activity compared to wild-type enzyme is 37%
2-(2-hydroxyanilino)quinazolin-4(3H)-one
residual activity compared to wild-type enzyme is 36%
2-(3-hydroxy-4-methylanilino)-6-propylpyrimidin-4(3H)-one
residual activity compared to wild-type enzyme is 36%
2-(3-hydroxyanilino)-6-methylpyrimidin-4(3H)-one
residual activity compared to wild-type enzyme is 39%
2-(3-hydroxyanilino)quinazolin-4(3H)-one
residual activity compared to wild-type enzyme is 26%
2-(4-hydroxy-2-methylanilino)-5,6,7,8-tetrahydroquinazolin-4(3H)-one
residual activity compared to wild-type enzyme is 70%
2-(4-hydroxy-2-methylanilino)-6-(propan-2-yl)pyrimidin-4(3H)-one
residual activity compared to wild-type enzyme is 29%
2-(4-hydroxy-2-methylanilino)-6-methylpyrimidin-4(3H)-one
residual activity compared to wild-type enzyme is 61%
2-(4-hydroxy-2-methylanilino)-6-phenylpyrimidin-4(3H)-one
residual activity compared to wild-type enzyme is 94%
2-(4-hydroxyanilino)-6-methylpyrimidin-4(3H)-one
residual activity compared to wild-type enzyme is 28%
2-(5-chloro-2-hydroxyanilino)-6-propylpyrimidin-4(3H)-one
residual activity compared to wild-type enzyme is 86%
2-[3-[(1-hydroxy-1,3-dihydro-2,1-benzoxaborol-6-yl)oxy]propyl]-1H-isoindole-1,3(2H)-dione
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3-(2-hydroxy-5-methylanilino)-1,2,4-triazin-5(4H)-one
residual activity compared to wild-type enzyme is 70%
3-(2-hydroxy-5-methylanilino)-6-methyl-1,2,4-triazin-5(4H)-one
residual activity compared to wild-type enzyme is 44%
3-(2-hydroxy-5-methylanilino)-6-phenyl-1,2,4-triazin-5(4H)-one
residual activity compared to wild-type enzyme is 36%
3-(2-hydroxyanilino)-6-methyl-1,2,4-triazin-5(4H)-one
residual activity compared to wild-type enzyme is 38%
3-(3-hydroxy-4-methylanilino)-6-methyl-1,2,4-triazin-5(4H)-one
residual activity compared to wild-type enzyme is 83%
3-(3-hydroxyanilino)-6-methyl-1,2,4-triazin-5(4H)-one
residual activity compared to wild-type enzyme is 40%
3-(3-hydroxyanilino)-6-phenyl-1,2,4-triazin-5(4H)-one
residual activity compared to wild-type enzyme is 57%
3-(4-hydroxy-2-methylanilino)-1,2,4-triazin-5(4H)-one
residual activity compared to wild-type enzyme is 51%
3-(4-hydroxy-2-methylanilino)-6-methyl-1,2,4-triazin-5(4H)-one
residual activity compared to wild-type enzyme is 70%
3-(4-hydroxyanilino)-6-methyl-1,2,4-triazin-5(4H)-one
residual activity compared to wild-type enzyme is 55%
3-(4-hydroxyanilino)-6-phenyl-1,2,4-triazin-5(4H)-one
residual activity compared to wild-type enzyme is 36%
3-(5-chloro-2-hydroxyanilino)-1,2,4-triazin-5(4H)-one
residual activity compared to wild-type enzyme is 45%
3-(5-chloro-2-hydroxyanilino)-6-methyl-1,2,4-triazin-5(4H)-one
residual activity compared to wild-type enzyme is 42%
3-[(1-hydroxy-1,3-dihydro-2,1-benzoxaborol-6-yl)oxy]-3-methylbutan-2-one
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3-[(1-hydroxy-1,3-dihydro-2,1-benzoxaborol-6-yl)oxy]-4-methylpentan-2-one
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3-[(3-oxo-2,3-dihydro-1,2,4-triazin-5-yl)amino]benzoic acid
residual activity compared to wild-type enzyme is 69%
3-[(4-oxo-3,4-dihydroquinazolin-2-yl)amino]benzoic acid
residual activity compared to wild-type enzyme is 36%
3-[(6-methyl-3-oxo-2,3-dihydro-1,2,4-triazin-5-yl)amino]benzoic acid
residual activity compared to wild-type enzyme is 57%
3-[4-(2-oxopropyl)anilino]-6-phenyl-1,2,4-triazin-5(4H)-one
residual activity compared to wild-type enzyme is 52%
4-methyl-3-[(3-oxo-2,3-dihydro-1,2,4-triazin-5-yl)amino]benzoic acid
residual activity compared to wild-type enzyme is 65%
4-methyl-3-[(4-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)amino]benzoic acid
residual activity compared to wild-type enzyme is 56%
4-[(4-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)amino]benzoic acid
residual activity compared to wild-type enzyme is 70%
4-[(5-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)amino]benzoic acid
residual activity compared to wild-type enzyme is 71%
4-[(5-oxo-4,5-dihydro-1,2,4-triazin-3-yl)amino]benzoic acid
residual activity compared to wild-type enzyme is 70%
4-[(6-methyl-3-oxo-2,3-dihydro-1,2,4-triazin-5-yl)amino]benzoic acid
residual activity compared to wild-type enzyme is 64%
5-(2-hydroxy-4-methylanilino)-1,2,4-triazin-3(2H)-one
residual activity compared to wild-type enzyme is 73%
5-(2-hydroxy-5-methylanilino)-1,2,4-triazin-3(2H)-one
residual activity compared to wild-type enzyme is 70%
5-(2-hydroxyanilino)-1,2,4-triazin-3(2H)-one
residual activity compared to wild-type enzyme is 72%
5-(2-hydroxyanilino)-6-methyl-1,2,4-triazin-3(2H)-one
residual activity compared to wild-type enzyme is 67%
5-(4-hydroxy-2-methylanilino)-6-methyl-1,2,4-triazin-3(2H)-one
residual activity compared to wild-type enzyme is 72%
5-(4-hydroxyanilino)-1,2,4-triazin-3(2H)-one
residual activity compared to wild-type enzyme is 70%
5-(4-hydroxyanilino)-6-methyl-1,2,4-triazin-3(2H)-one
residual activity compared to wild-type enzyme is 55%
5-[(6-methyl-3-oxo-2,3-dihydro-1,2,4-triazin-5-yl)amino]benzene-1,3-dicarboxylic acid
residual activity compared to wild-type enzyme is 72%
6,8-dibenzyl-2-(4-methylphenyl)-4,7-dioxo-N-(prop-2-en-1-yl)hexahydro-2H-pyrazino[2,1-c][1,2,4]triazine-1(6H)-carboxamide
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8-benzyl-6-[(4-chlorophenyl)methyl]-2-(4-methylphenyl)-4,7-dioxo-N-(prop-2-en-1-yl)hexahydro-2H-pyrazino[2,1-c][1,2,4]triazine-1(6H)-carboxamide
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8-benzyl-N-([1,1'-biphenyl]-2-yl)-2-methyl-4,7-dioxo-6-(propan-2-yl)hexahydro-2H-pyrazino[2,1-c][1,2,4]triazine-1(6H)-carboxamide
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Al3+
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in vitro the enzyme is inhibited by 40% at 0.04 mM, Al3+ inhibits the enzyme in vivo and in vitro, quantitative analysis, in vivo acceptor activity of tRNALeu is decreased by 23% thereby the leucyl-tRNA synthetase activity is increased by 20%, overview
BC-LI-0186
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the interaction between RagD and LRS is disrupted by compound BC-LI-0186 inhibitong the translocation of the enzyme to the lysosome
ethyl (2E)-3-(1-hydroxy-1,3-dihydro-2,1-benzoxaborol-6-yl)prop-2-enoate
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ethyl 2-[(1-hydroxy-1,3-dihydro-2,1-benzoxaborol-6-yl)oxy]-2-methylpropanoate
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ethyl [(1-hydroxy-1,3-dihydro-2,1-benzoxaborol-6-yl)oxy](phenyl)acetate
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N,8-dibenzyl-6-[(4-hydroxyphenyl)methyl]-2-methyl-4,7-dioxohexahydro-2H-pyrazino[2,1-c][1,2,4]triazine-1(6H)-carboxamide
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N-(4-fluorophenyl)-8-[(furan-2-yl)methyl]-2-methyl-4,7-dioxo-6-[3-[N'-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-yl)carbamimidamido]propyl]hexahydro-2H-pyrazino[2,1-c][1,2,4]triazine-1(6H)-carboxamide
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N-benzyl-8-butyl-2-(4-methylphenyl)-4,7-dioxo-6-(propan-2-yl)hexahydro-2H-pyrazino[2,1-c][1,2,4]triazine-1(6H)-carboxamide
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N-benzyl-8-butyl-6-[(4-chlorophenyl)methyl]-2-(4-methylphenyl)-4,7-dioxohexahydro-2H-pyrazino[2,1-c][1,2,4]triazine-1(6H)-carboxamide
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N-benzyl-8-[(furan-2-yl)methyl]-2-(4-methylphenyl)-4,7-dioxo-6-(propan-2-yl)hexahydro-2H-pyrazino[2,1-c][1,2,4]triazine-1(6H)-carboxamide
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N-tert-butyl-2-[(1-hydroxy-1,3-dihydro-2,1-benzoxaborol-6-yl)oxy]acetamide
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O-[N-(L-norvalyl)sulfamoyl]adenosine
analogue to the reaction intermediate, non-hydrolyzable
tert-butyl [2-[(1-hydroxy-1,3-dihydro-2,1-benzoxaborol-6-yl)oxy]ethyl]carbamate
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[4-[(4-oxo-3,4-dihydroquinazolin-2-yl)amino]phenyl]acetic acid
residual activity compared to wild-type enzyme is 37%
[4-[(5-oxo-4,5-dihydro-1,2,4-triazin-3-yl)amino]phenyl]acetic acid
residual activity compared to wild-type enzyme is 72%
[4-[(6-methyl-5-oxo-4,5-dihydro-1,2,4-triazin-3-yl)amino]phenyl]acetic acid
residual activity compared to wild-type enzyme is 71%
binding mode, overview
5-(5-chloro-2-hydroxy-phenylamino)-2H-[1,2,4]triazin-3-one
residual activity compared to wild-type enzyme is 18%, binding mode, overview
binding mode, overview
5-(5-chloro-2-hydroxy-phenylamino)-6-methyl-2H-[1,2,4]triazin-3-one
residual activity compared to wild-type enzyme is 2.3%, binding mode, overview
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i.e. AN2690, 0.1 mM, 5fold decrease in aminoacylation activity
5-fluoro-1,3-dihydro-1-hydroxy-2,1-benzoxaborole
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i.e. AN2690, the editing active site is the proven target for the broad-spectrum drug. But the post-transfer editing by LeuRS is resistant to the broad-spectrum drug AN2690, AN2690 resistance and its possible mechanism, overview
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AN-2690, antibiotic which specifically targets the editing active site of LeuRS
5-fluoro-2,1-benzoxaborol-1(3H)-ol
AN-2690, antibiotic which specifically targets the editing active site of LeuRS
ATP
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at high concentration, the mutants are more sensisitve than the wild-type enzyme
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aminoacylation and editing reaction are resistant to inactivation by compound AN2690
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additional information
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development of a GlLeuRS-specific inhibitor for the treatment of giardiasis
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additional information
inhibition by high levels of mono- and divalent cations
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additional information
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inhibition by high levels of mono- and divalent cations
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additional information
design and synthesis of tetra-substituted hexahydro-4H-pyrazino[2,1-c][1,2,4]triazine-4,7(6H)-diones as beta-turn mimetics via tandem N-acyliminium cyclization using a parallel synthetic strategy involving both solid and solution-phase reactions. Construction of a 162-member library of tetra-substituted pyrazinotriazinediones with an average purity of 90% using a solid-phase parallel synthesis platform, and screening for the LRS-RagD interaction inhibition by the compounds, overview
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additional information
derivatives of 5-phenylamino-2H-[1,2,4]triazin-3-one as leucyl-tRNA synthetase (LeuRS) inhibitors, docking study, overview. The inhibitory activity of some compounds against pathogenic LeuRS is 10fold higher compared to the human enzyme. Hydrogen bond-foming amino acids in active site of LeuRS are Phe97, Tyr99, Glu103, His109, Tyr113, Asp137, Ser631, Gly678, Glu680, His681, Gln714, Ile717, Lys759, and Ile760
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additional information
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derivatives of 5-phenylamino-2H-[1,2,4]triazin-3-one as leucyl-tRNA synthetase (LeuRS) inhibitors, docking study, overview. The inhibitory activity of some compounds against pathogenic LeuRS is 10fold higher compared to the human enzyme. Hydrogen bond-foming amino acids in active site of LeuRS are Phe97, Tyr99, Glu103, His109, Tyr113, Asp137, Ser631, Gly678, Glu680, His681, Gln714, Ile717, Lys759, and Ile760
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additional information
derivatives of 5-phenylamino-2H-[1,2,4]triazin-3-one as leucyl-tRNA synthetase (LeuRS) inhibitors, docking study, overview. The inhibitory activity of some compounds against pathogenic LeuRS is 10fold higher compared to the human enzyme. Hydrogen bond-foming amino acids in active site of LeuRS are Phe97, Tyr99, Glu103, His109, Tyr113, Asp137, Ser631, Gly678, Glu680, His681, Gln714, Ile717, Lys759, and Ile760. No inhibition by 5-[(6-methyl-5-oxo-4,5-dihydro-1,2,4-triazin-3-yl)amino]cyclohexa-2,4-diene-1-carboxylic acid, 4-[(4-oxo-3,4,5,6,7,8-hexahydroquinazolin-2-yl)amino]benzoic acid, 2-(2-hydroxyanilino)-5,6,7,8-tetrahydroquinazolin-4(3H)-one, 4-[(6-oxo-4-propyl-1,6-dihydropyrimidin-2-yl)amino]benzoic acid, 2-(4-hydroxyanilino)-6-propylpyrimidin-4(3H)-one, 2-(2-hydroxyanilino)-6-propylpyrimidin-4(3H)-one, 2-(4-hydroxy-2-methylanilino)-6-propylpyrimidin-4(3H)-one, 2-(3-hydroxy-4-methylanilino)-6-propylpyrimidin-4(3H)-one, 3-(2-hydroxyanilino)-1,2,4-triazin-5(4H)-one, 3-(4-hydroxyanilino)-1,2,4-triazin-5(4H)-one, and 2-(2-hydroxyanilino)-3,5,6,7-tetrahydro-4H-cyclopenta[d]pyrimidin-4-one
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additional information
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derivatives of 5-phenylamino-2H-[1,2,4]triazin-3-one as leucyl-tRNA synthetase (LeuRS) inhibitors, docking study, overview. The inhibitory activity of some compounds against pathogenic LeuRS is 10fold higher compared to the human enzyme. Hydrogen bond-foming amino acids in active site of LeuRS are Phe97, Tyr99, Glu103, His109, Tyr113, Asp137, Ser631, Gly678, Glu680, His681, Gln714, Ile717, Lys759, and Ile760. No inhibition by 5-[(6-methyl-5-oxo-4,5-dihydro-1,2,4-triazin-3-yl)amino]cyclohexa-2,4-diene-1-carboxylic acid, 4-[(4-oxo-3,4,5,6,7,8-hexahydroquinazolin-2-yl)amino]benzoic acid, 2-(2-hydroxyanilino)-5,6,7,8-tetrahydroquinazolin-4(3H)-one, 4-[(6-oxo-4-propyl-1,6-dihydropyrimidin-2-yl)amino]benzoic acid, 2-(4-hydroxyanilino)-6-propylpyrimidin-4(3H)-one, 2-(2-hydroxyanilino)-6-propylpyrimidin-4(3H)-one, 2-(4-hydroxy-2-methylanilino)-6-propylpyrimidin-4(3H)-one, 2-(3-hydroxy-4-methylanilino)-6-propylpyrimidin-4(3H)-one, 3-(2-hydroxyanilino)-1,2,4-triazin-5(4H)-one, 3-(4-hydroxyanilino)-1,2,4-triazin-5(4H)-one, and 2-(2-hydroxyanilino)-3,5,6,7-tetrahydro-4H-cyclopenta[d]pyrimidin-4-one
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additional information
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enzyme drug inhibitor design and development based on the benzoxaborole structure, inhibitory potencies and effectiveness a anti-trypanosomal drugs, ligand, i.e. benzoxaborole-AMP, docking in the LeuRS homology model, overview
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