6.1.1.6: lysine-tRNA ligase
This is an abbreviated version!
For detailed information about lysine-tRNA ligase, go to the full flat file.
Word Map on EC 6.1.1.6
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6.1.1.6
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synthetases
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aminoacylation
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lysylation
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anticodon
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aarss
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isoacceptors
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diadenosine
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aspartyl-trna
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gagpol
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tetraphosphate
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trnalys3
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prors
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valrs
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leurs
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arginyl-trna
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isoleucyl-trna
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glnrs
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atp-ppi
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anticodon-binding
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prolyl-trna
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multi-trna
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asprs
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diagnostics
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pharmacology
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medicine
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drug development
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synthesis
- 6.1.1.6
- synthetases
- aminoacylation
- lysylation
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anticodon
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aarss
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isoacceptors
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diadenosine
- aspartyl-trna
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gagpol
- tetraphosphate
- trnalys3
- prors
- valrs
- leurs
- arginyl-trna
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isoleucyl-trna
- glnrs
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atp-ppi
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anticodon-binding
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prolyl-trna
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multi-trna
- asprs
- diagnostics
- pharmacology
- medicine
- drug development
- synthesis
Reaction
Synonyms
Ap4A synthase, BBA_03037, class 1 lysyl tRNA synthetase, class I LysRS, class I lysyl-tRNA synthetase, class II lysyl-tRNA synthetase, cyto-LysRS, cytoKARS, cytoplasmic lysyl-tRNA synthetase, FOSTERSO_4045, GsLysRS, hKRS, KARS, KRS, KRS-1, L-Lysine-transfer RNA ligase, lysine aminoacyl-tRNA synthetase, Lysine translase, Lysine--tRNA ligase, Lysine-tRNA synthetase, LysRS, LysRS-I, LysRS-II, LysRS1, LysRS2, lysS, lysS2, LysU, LysX, lysyl tRNA synthetase, Lysyl-transfer ribonucleate synthetase, Lysyl-transfer RNA synthetase, Lysyl-tRNA synthetase, lysylphosphatidylglycerol biosynthesis bifunctional protein, mito-LysRS, mitochondrial lysyl-tRNA synthetase, mitoKARS, More, Msk1p, MSMEG_3796, MSMEG_6094, MSMEI_3707, MXAN_4731, PF3D7_1350100, PfKRS, preMsk1p, Synthetase, lysyl-transfer ribonucleate, tRK1
ECTree
6.1.1.6 lysine-tRNA ligaseAdvanced search results
results (
results (Inhibitors
Inhibitors on EC 6.1.1.6 - lysine-tRNA ligase
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INHIBITOR 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
IMAGE
(3R,5S)-1-[(6-amino-9H-purin-9-yl)acetyl]-5-carbamoylpyrrolidin-3-yl L-lysylsulfamate
strong inhibitory effect
(4R)-1-[(3-chloro-4-hydroxyphenyl)acetyl]-4-[(L-lysylsulfamoyl)oxy]-L-prolinamide
strong inhibitory effect
(4S)-1-(3-bromo-4-hydroxybenzyl)-4-[hydroxy(L-lysyl)amino]-L-prolinamide
strong inhibitory effect
2-(5,6-difluoro-2-([3-(trifluoromethyl)benzoyl]imino)benzo[d]thiazol-3(2H)-yl)butanoic acid
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i.e. BC-K-YH16899, shows three to sixfold better inhibition of KRS as BC-K01 in most of the assays and better volume of distribution in vivo
ADP
the addition of ADP inhibits the diadenosine tetraphosphate synthesis by Ap4A synthase activity of LysS. Ap4A production decreases by 22% and 52% at 1 mM and 5 mM ADP, respectively. In the presence of ADP, Ap3A is not synthesized by LysS during 30 min of incubation. ADP may act as a competitive inhibitor of LysS in the first step reaction, i.e. lysyl-AMP formation from lysine and ATP
ATP
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substrate inhibition in the aminoacylation reaction above 0.4 mM, no inhibition in the ATP-diphosphate exchange reaction
BC-K-01
the inhibitor interferes with the binding between enzyme KRS and laminin receptor 37LRP domain
BC-K-YH16899
the inhibitor interferes with the binding between enzyme KRS and laminin receptor 37LRP domain
CNBr
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treatment of tRNALys substrate with CNBr reduces the enzyme activity
human tRNALys anticodon domain
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from wild-type tRNALys, N-terminally truncated mutant enzyme
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human tRNALys-3'oxidized
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3'-oxidized by periodate, N-terminally truncated mutant enzyme
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human tRNALysU35G mutant
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defective substrate in both binding and catalysis, N-terminally truncated mutant enzyme
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Mg2+
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synthesis of lysyl-tRNA from lysyl-AMP-enzyme inhibited, formation of Lys-tRNALys from lysine, tRNA and ATP-enzyme complex or ATP is dependent on Mg2+
NH4+
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formation of Lys-tRNALys from lysine, tRNA and ATP-enzyme complex or ATP
YH16899
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KRS is the main target of YH16899. YH16899 inhibits enzyme KRS and KRS-mediated metastasis, it also reduces pulmonary nodule formation by approximately 70% without any effects on bodyweight. While YH16899 does not affect cancer cell viability, it inhibits the H226 cell migration with an IC50 of 0.0085 mM
3'-Deoxyadenosine 5'-triphosphate
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inhibitor in aminoacylation, good substrate in ATP-diphosphate exchange
cladosporin
has the ability to mimic the natural substrate adenosine and thereby colonize the PfKRS active site, binding structure analysis, overview. Plasmodium falciparum lysyl-tRNA synthetase (PfKRS) as the cellular target for cladosporin activity. Structural basis of inhibition by cladosporin, overview. The isocoumarin moiety of cladosporin stacks between Ph342 and Arg559 in PfKRS. In addition, His338 provides edge-toface interaction with hydroxybenzene ring of isocoumarin moiety. The THP ring points towards L-Lys binding pocket and its methyl group faces Ser344
additional information
the complex formation among KRS, p67LR, and integrins alpha6 and beta1 upon cell adhesion can be disrupted by YH16899 treatment. SW620 cells with inhibitors U1026 or YH16899 blocks dissemination. Blockade of dissemination of KRS-suppressed cells is relieved by ERK1/2 and/or paxillin expression
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additional information
the formation of diadenosine tetraphosphate (Ap4A) by LysS is inhibited by tRNA(Lys) in the presence of 1 mM ATP
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additional information
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the formation of diadenosine tetraphosphate (Ap4A) by LysS is inhibited by tRNA(Lys) in the presence of 1 mM ATP
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additional information
the solid-phase combinatorial synthesis of a new library with potential inhibitory activity against the cytoplasmic lysyl-tRNA synthetase (LysRS) isoform of Trypanosoma brucei is described. Among the 65 compounds tested, there are 15 that have a mild inhibitory effect at 100 microM, and 3 have a strong effect
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additional information
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the solid-phase combinatorial synthesis of a new library with potential inhibitory activity against the cytoplasmic lysyl-tRNA synthetase (LysRS) isoform of Trypanosoma brucei is described. Among the 65 compounds tested, there are 15 that have a mild inhibitory effect at 100 microM, and 3 have a strong effect
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