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Information on EC 6.1.1.10 - methionine-tRNA ligase
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6.1.1.10 methionine-tRNA ligaseIUBMB Comments
In those organisms producing N-formylmethionyl-tRNAfMet for translation initiation, this enzyme also recognizes the initiator tRNAfMet and catalyses the formation of L-methionyl-tRNAfMet, the substrate for EC 2.1.2.9, methionyl-tRNA formyltransferase.
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Word Map
- 6.1.1.10
- synthetases
- aminoacyl-trna
- aminoacylation
-
anticodons
- homocysteine
- trnafmet
-
trypsin-modified
-
thiolactone
-
isoleucyl-trna
- arc1p
-
aarss
- tyrosyl-trna
-
isoleucylation
-
atp-ppi
-
noncognate
-
trna-binding
-
anticodon-binding
-
hcy-thiolactone
- ilers
-
blanquet
- formylmethionine
- medicine
- leucyl-trna
-
kmsks
-
multisynthetase
-
cysteinyl-trna
- valyl-trna
- lysyl-trna
-
misacylation
- valrs
- met-trna
- pharmacology
- drug development
The enzyme appears in viruses and cellular organisms
Synonyms
methionyl-trna synthetase, metrs, methionyl trna synthetase, mars-1, hcmetrs, metrs2, methionyl-trna-synthetase, let-65, metrs1, methionine-trna ligase, 
more
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SYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
let-65
mars-1
Methionine translase
Methionine--tRNA ligase
Methionyl tRNA synthetase
Methionyl-transfer ribonucleate synthetase
Methionyl-transfer ribonucleic acid synthetase
Methionyl-transfer RNA synthetase
methionyl-tRNA synthetase
methionyl-tRNA-synthetase
MetRS
MRS
Synthetase, methionyl-transfer ribonucleate
additional information
Methionine translase
-
-
Methionine--tRNA ligase
-
-
Methionyl tRNA synthetase
-
-
Methionyl-transfer ribonucleate synthetase
-
-
Methionyl-transfer ribonucleic acid synthetase
-
-
Methionyl-transfer RNA synthetase
-
-
methionyl-tRNA synthetase
-
-
MetRS
-
-
Synthetase, methionyl-transfer ribonucleate
-
-
additional information
-
the enzyme belongs to the class I aminoacyl-tRNA synthetases
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REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
ATP + L-methionine + tRNAMet = AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
-
ATP + L-methionine + tRNAMet = AMP + diphosphate + L-methionyl-tRNAMet
active site structure and reaction mechanism involving Tyr15 and Thr10, Tyr94 is involved in maintaining the native enzyme conformation
-
ATP + L-methionine + tRNAMet = AMP + diphosphate + L-methionyl-tRNAMet
amino acid residues D138, R139, and F135 are important for activity
-
ATP + L-methionine + tRNAMet = AMP + diphosphate + L-methionyl-tRNAMet
amino acid residues involved in tRNA binding are K30, N66, S78, and M81
ATP + L-methionine + tRNAMet = AMP + diphosphate + L-methionyl-tRNAMet
mechanism, catalytic domain is formed by amino acid residues A215-K823
-
ATP + L-methionine + tRNAMet = AMP + diphosphate + L-methionyl-tRNAMet
reaction mechanism, Lys261, Lys295, and Lys301 are located in the catalytic crevice of the enzyme
-
ATP + L-methionine + tRNAMet = AMP + diphosphate + L-methionyl-tRNAMet
substrate binding and mechanism
ATP + L-methionine + tRNAMet = AMP + diphosphate + L-methionyl-tRNAMet
substrate recognition and structure
-
ATP + L-methionine + tRNAMet = AMP + diphosphate + L-methionyl-tRNAMet
substrate recognition and structure
-
ATP + L-methionine + tRNAMet = AMP + diphosphate + L-methionyl-tRNAMet
substrate recognition, editing, binding and reaction mechanism
-
ATP + L-methionine + tRNAMet = AMP + diphosphate + L-methionyl-tRNAMet
the amino acid acceptor arm of tRNAMet binds to the plant enzyme
ATP + L-methionine + tRNAMet = AMP + diphosphate + L-methionyl-tRNAMet
the anticodon sequence is important for tRNA substrate specificity
-
ATP + L-methionine + tRNAMet = AMP + diphosphate + L-methionyl-tRNAMet
two-step reaction process via anenzyme-L-Met-AMP intermediate
ATP + L-methionine + tRNAMet = AMP + diphosphate + L-methionyl-tRNAMet
the aminoacylation reaction is a two-step mechanism: in the first step, the synthetase recognizes the appropriate amino acid and activates it with ATP to form the activated intermediate, an aminoacyl-adenylate, aa-AMP, the second step transfers the aminoacyl moiety onto the 3'-hydroxyl of the CCA end of the tRNA, the methionine-binding pocket is composed of residues Ala12, Leu13, Tyr15, Trp253, Ala256, Pro257, Tyr260, Ile297, His301, and Trp305
-
ATP + L-methionine + tRNAMet = AMP + diphosphate + L-methionyl-tRNAMet
the anticodon sequence is important for tRNA substrate specificity
-
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Acylation
Aminoacylation
esterification
Aminoacylation
-
-
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PATHWAY SOURCE
PATHWAYS
BRENDA
MetaCyc
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SYSTEMATIC NAME
IUBMB Comments
L-methionine:tRNAMet ligase (AMP-forming)
In those organisms producing N-formylmethionyl-tRNAfMet for translation initiation, this enzyme also recognizes the initiator tRNAfMet and catalyses the formation of L-methionyl-tRNAfMet, the substrate for EC 2.1.2.9, methionyl-tRNA formyltransferase.
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CAS REGISTRY NUMBER
COMMENTARY
9033-22-1
-
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SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
AMP + diphosphate + L-methionyl-tRNAMet
ATP + L-methionine + tRNAMet
-
-
-
r
ATP + (S)-2-aminohex-5-enoic acid + tRNAMet
AMP + diphosphate + (S)-2-aminohex-5-enoyl-tRNAMet
1850fold reduced activity compared to L-methionine
-
?
ATP + (S)-2-aminohex-5-enoic acid + tRNAMet
AMP + diphosphate + 2(S)-aminohex-5-enoyl-tRNAMet
-
-
?
ATP + (S)-2-aminohex-5-ynoic acid + tRNAMet
AMP + diphosphate + 2(S)-aminohex-5-ynoyl-tRNAMet
500fold reduced activity compared to L-methionine
-
?
ATP + azidonorleucine + tRNAMet
AMP + diphosphate + azidonorleucinyl-tRNAMet
MetRS SLL-mutant
-
?
ATP + azidonorleucine + tRNAMet
AMP + diphosphate + azidonorleucyl-tRNAMet
activity of mutant L13G, overview
-
?
ATP + L-homocysteine + tRNAMet
?
-
edition and aminoacylation by cytoplasmic and mitochondrial isozyme
-
?
ATP + L-methionine + tRNA fraction from Saccharomyces cerevisiae
?
-
-
?
ATP + L-methionine + tRNAAsp
AMP + diphosphate + L-methionyl-tRNAAsp
only the wild-type enzyme, not the C-terminally deleted enzyme mutant
-
?
ATP + L-trans-alpha-crotylglycine + tRNAMet
AMP + diphosphate + L-trans-alpha-crotylglycyl-tRNAMet
4700fold reduced activity compared to L-methionine
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
the MetRS specificity for methionine and conformity with the identity rules for tRNAMet for archea/eukarya, anticodon binding site, overview
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
functional idiosyncrasies of the viral MetRS, activity with Escherichia coli native tRNAMet and initiator tRNAMet, and Saccharomyces cerevisiae native tRNAMet and initiator tRNAMet, overview, the MetRS specificity for methionine and recognition of the tRNAMet acceptor stem show conformity with the identity rules for tRNAMet for archea/eukarya, overview
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
r
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
structural basis for anticodon recognition by the enzyme, catalytic Rossmann fold domain
-
r
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
essentiality of the metS1, nonessentiality of the metS2 for vegetative growth
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
MetRS specifically binds tRNAMet and catalyzes the synthesis of methionyl-tRNAMet. The C-terminal appended domain causes a slow release of aminoacyl-tRNA and establishes a limiting step in the global aminoacylation reaction
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
also utilizes both subtypes of Escherichia coli tRNAMet
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
active site analysis and docking study, overview. Key residues are His53, Asp51 and Lys56 consistently forming H-bonding interactions with the carboxylic acid moiety of methionine. Ile12 forms a hydrogen bond with this moiety in different dockings and the residues Ile224, Val226 and Ala230 form a hydrophobic pocket
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
active site analysis and docking study, overview. Key residues are His53, Asp51 and Lys56 consistently forming H-bonding interactions with the carboxylic acid moiety of methionine. Ile12 forms a hydrogen bond with this moiety in different dockings and the residues Ile224, Val226 and Ala230 form a hydrophobic pocket
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
r
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
binding of L-methionine induces conformational changes of the active site of the enzyme, amino acid residues Y15 and W253 are important for the strength of binding, H301 is responsible for the specific recognition of the sulfur atom of methionine
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
covalent binding of methionine to the tRNAMet
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
formation of an methionine adenylate reaction intermediate
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
reduced activity with L-methionine analogues, overview, two-step reaction, the first step, the aminoacylation, is reversible, the seconde, the transfer reaction, is not
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
substrate editing mechanism, L-methionine is bound to a hydrophobic pocket formed by amino acid residues W253, Y15, A256, P257, L13, A12, I297, Y260, H301, and W305 around the side-chain
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
L-methionine and methionine analogue substrates are incorporated in proteins, overview
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
conformation of tRNA and the recognition of anticodon by MetRS, hydrogen bonding patterns, interactions at the active site, overview
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
residues L13, P257, Y260, and H301 are involved in the Met binding site
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
two-step reaction mechanism, enzyme forms the reaction intermediate L-methionyl-adenylate, which covalently methionylates the enzyme at the epsilon-amino group of a lysine residue, inducing structural modifcation, 4.3 and 2.2 mol of Met are incorporated by 1 mol of wild-type enzyme and truncated mutant enzyme, respectively
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
r
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
protein biosynthesis in archaea is initiated with methionine not with formylmethionine
-
r
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
r
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
protein biosynthesis in archaea is initiated with methionine not with formylmethionine
-
r
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
r
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
r
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
the C-terminal ancillary RNA-binding domain is important for activity and has dual function provided by 2 structural motifs: 1. the helix-turn-helix HTH motif, which confers rate-limiting dissociation of the aminoaclyted tRNA from the enzyme, and 2. the KGKKKK lysine-rich cluster LRC, which is probably involved in accelerating the association step of deacylated tRNA
-
r
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
the nucleolar located enzyme is related to rRNA synthesis, the cytoplasmic enzyme is involved in protein biosynthesis
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
human mitochondrial wild-type and mutant mtRNAs: T5048 deletion, and T5052C or T5012A point mutations, initiator tRNA from Escherichia coli, tRNAMet from Bos taurus
-
r
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
binding structures of substrates and products, overview
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
also utilizes tRNAMet from Escherichia coli
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
analysis of methionine and adenosine binding to MetRS, catalytic domain structure, overview. The KMSKS domain, residues 293-350, or stem contact fold domain, with a beta-alpha-alpha-beta-alpha topology domain, connects the catalytic domain with the anticodon domain, KMSKS domain conformation and structure, modelling, overview
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
the EMAPII-like C-terminal appendix domain provides the enzyme with non-specific tRNA binding properties, the deleted enzyme form missing this domain is therefore more specific and shows a 10fold lower Km for the tRNA substrate, enzyme is also active with tRNAMet from Saccharomyces cerevisiae
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
r
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
dimerization of the enzyme is required for affinity to tRNAMet
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
tRNA anticodon binding site structure
-
r
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
initiator and elongation tRNAMet, cytoplasmic and mitochondrial isozyme
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
covalent binding of methionine to the tRNAMet
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
Thermus thermophilus HB8 / ATCC 27634 / DSM 579
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
Thermus thermophilus HB8 / ATCC 27634 / DSM 579
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
Thermus thermophilus HB8 / ATCC 27634 / DSM 579
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
substrates: prokaryotic, chloroplastic, cytoplasmic (initiator not non-initiator)
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-norleucine + tRNAMet
AMP + diphosphate + L-norleucyl-tRNAMet
1050fold reduced activity compared to L-methionine
-
?
ATP + L-norleucine + tRNAMet
AMP + diphosphate + L-norleucyl-tRNAMet
-
-
-
?
ATP + L-valine + tRNAMetG34C36
AMP + diphosphate + L-valyl-tRNAMetG34C36
-
anticodon mutant initiator tRNAMet, reduced reverse, i.e. deacetylation, reaction
-
r
ATP + L-valine + tRNAMetG34C36
AMP + diphosphate + L-valyl-tRNAMetG34C36
-
CAU to GAC anticodon mutant initiator tRNAMet, reduced reverse, i.e. deacetylation, reaction
-
r
ATP + L-valine + tRNAMetG34C36
AMP + diphosphate + L-valyl-tRNAMetG34C36
-
anticodon mutant initiator tRNAMet, reduced reverse, i.e. deacetylation, reaction
-
r
ATP + L-valine + tRNAMetG34C36
AMP + diphosphate + L-valyl-tRNAMetG34C36
-
CAU to GAC anticodon mutant initiator tRNAMet, reduced reverse, i.e. deacetylation, reaction
-
r
ATP + methionine + hydroxylamine
methionine hydroxamate + AMP + diphosphate
-
-
-
?
ATP + methionine + hydroxylamine
methionine hydroxamate + AMP + diphosphate
-
-
-
?
ATP + selenomethionine + tRNAMet
AMP + diphosphate + selenomethionyl-tRNAMet
-
-
-
?
ATP + selenomethionine + tRNAMet
AMP + diphosphate + selenomethionyl-tRNAMet
-
-
-
?
ATP + selenomethionine + tRNAMet
AMP + diphosphate + selenomethionyl-tRNAMet
-
-
-
?
additional information
?
-
-
mimivirus aminoacyl-tRNA synthetases function as regular translation enzymes in infected amoebas
-
?
additional information
?
-
Met-tRNA anticodon interactions with the MetRS homology model, overview
-
?
additional information
?
-
-
Met-tRNA anticodon interactions with the MetRS homology model, overview
-
?
additional information
?
-
Met-tRNA anticodon interactions with the MetRS homology model, overview
-
?
additional information
?
-
-
homocysteine thiolactone is formed as a product of an error-editing reaction, which prevents incorporation of homocysteine into tRNA and protein (not enzyme from temperature-sensitive mutant of CHO-cells, at non-permissive temperature)
-
?
additional information
?
-
-
homocysteine thiolactone is formed as a product of an error-editing reaction, which prevents incorporation of homocysteine into tRNA and protein (not enzyme from temperature-sensitive mutant of CHO-cells, at non-permissive temperature)
-
?
additional information
?
-
-
methionine-dependent ATP-diphosphate exchange
-
?
additional information
?
-
-
methionine-dependent ATP-diphosphate exchange
-
?
additional information
?
-
-
methionine-dependent ATP-diphosphate exchange
-
?
additional information
?
-
-
enzyme also performs the ATP-diphosphate exchange reaction
-
?
additional information
?
-
-
the enzyme also performs the ATP-diphosphate exchange reaction
-
?
additional information
?
-
the enzyme also performs the ATP-diphosphate exchange reaction
-
?
additional information
?
-
-
L-homocysteine is a natural competitor to L-methionine, its activation by the enzyme is prevented by a proof-reading mechanism, structural requirements are determined form the crystal structure
-
?
additional information
?
-
-
modeling of the structure of a complex consisting of MetRS, tRNA, and activated methionine, molecular dynamics simulations, evaluation of the equilibrated structure of the complex and the cross-correlations between the residues in MetRS, analysis of communication between the activation site and the anticodon recognition site, overview
-
?
additional information
?
-
-
enzyme also performs the ATP-diphosphate exchange reaction
-
?
additional information
?
-
-
no activity with the CAU to CUA initiator tRNAMet mutant in vivo
-
?
additional information
?
-
-
no activity with the CAU to CUA initiator tRNAMet mutant in vivo
-
?
additional information
?
-
-
homocysteine thiolactone is formed as a product of an error-editing reaction, which prevents incorporation of homocysteine into tRNA and protein (not enzyme from temperature-sensitive mutant of CHO-cells, at non-permissive temperature)
-
?
additional information
?
-
the enzyme performs ATP/diphosphate exchange in absence of substrates
-
?
additional information
?
-
-
the enzyme performs ATP/diphosphate exchange in absence of substrates
-
?
additional information
?
-
-
homocysteine thiolactone is formed as a product of an error-editing reaction, which prevents incorporation of homocysteine into tRNA and protein (not enzyme from temperature-sensitive mutant of CHO-cells, at non-permissive temperature)
-
?
additional information
?
-
-
no other amino acid than methionine is activated in ATP-diphosphate exchange
-
?
additional information
?
-
-
enzyme forms A and B show differences in their capacity to recognize the cognate tRNAs
-
?
additional information
?
-
-
methionine-dependent ATP-diphosphate exchange
-
?
additional information
?
-
binding of the enzyme to the split 3'-half tRNA species is stronger than to that of the 5'-half species
-
?
additional information
?
-
-
binding of the enzyme to the split 3'-half tRNA species is stronger than to that of the 5'-half species
-
?
additional information
?
-
-
methionine-dependent ATP-diphosphate exchange
-
?
additional information
?
-
-
also catalyzes L-homocysteine, L-selenocysteine and norleucine-dependent ATP-diphosphate exchange
-
?
additional information
?
-
-
methionine-dependent ATP-diphosphate exchange
-
?
additional information
?
-
-
also catalyzes L-homocysteine, L-selenocysteine and norleucine-dependent ATP-diphosphate exchange
-
?
additional information
?
-
-
methionine-dependent ATP-diphosphate exchange
-
?
additional information
?
-
-
homocysteine thiolactone is formed as a product of an error-editing reaction, which prevents incorporation of homocysteine into tRNA and protein (not enzyme from temperature-sensitive mutant of CHO-cells, at non-permissive temperature)
-
?
additional information
?
-
-
the isozymes also perform the ATP-diphosphate exchange reaction
-
?
additional information
?
-
MetRS interacts with the accessory protein Arc1p, interaction mode and structure, overview
-
?
additional information
?
-
-
MetRS interacts with the accessory protein Arc1p, interaction mode and structure, overview
-
?
additional information
?
-
-
methionine-dependent ATP-diphosphate exchange
-
?
additional information
?
-
-
also catalyzes selenomethionine- and selenoethionine-dependent ATP-diphosphate exchange
-
?
additional information
?
-
-
no other amino acid than methionine is activated in ATP-diphosphate exchange
-
?
additional information
?
-
-
methionine-dependent ATP-diphosphate exchange
-
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
ATP + azidonorleucine + tRNAMet
AMP + diphosphate + azidonorleucyl-tRNAMet
activity of mutant L13G, overview
-
-
?
ATP + L-homocysteine + tRNAMet
?
-
edition and aminoacylation by cytoplasmic and mitochondrial isozyme
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
the MetRS specificity for methionine and conformity with the identity rules for tRNAMet for archea/eukarya, anticodon binding site, overview
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
-
r
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
essentiality of the metS1, nonessentiality of the metS2 for vegetative growth
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
Brucella melitensis 2308
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
MetRS specifically binds tRNAMet and catalyzes the synthesis of methionyl-tRNAMet. The C-terminal appended domain causes a slow release of aminoacyl-tRNA and establishes a limiting step in the global aminoacylation reaction
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
-
r
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
L-methionine and methionine analogue substrates are incorporated in proteins, overview
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
protein biosynthesis in archaea is initiated with methionine not with formylmethionine
-
r
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
protein biosynthesis in archaea is initiated with methionine not with formylmethionine
-
r
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
r
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
r
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
the nucleolar located enzyme is related to rRNA synthesis, the cytoplasmic enzyme is involved in protein biosynthesis
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
r
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
initiator and elongation tRNAMet, cytoplasmic and mitochondrial isozyme
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
Thermus thermophilus HB8 / ATCC 27634 / DSM 579
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-methionine + tRNAMet
AMP + diphosphate + L-methionyl-tRNAMet
-
-
-
?
ATP + L-valine + tRNAMetG34C36
AMP + diphosphate + L-valyl-tRNAMetG34C36
-
CAU to GAC anticodon mutant initiator tRNAMet, reduced reverse, i.e. deacetylation, reaction
-
r
ATP + L-valine + tRNAMetG34C36
AMP + diphosphate + L-valyl-tRNAMetG34C36
-
CAU to GAC anticodon mutant initiator tRNAMet, reduced reverse, i.e. deacetylation, reaction
-
r
additional information
?
-
-
mimivirus aminoacyl-tRNA synthetases function as regular translation enzymes in infected amoebas
-
-
?
additional information
?
-
-
L-homocysteine is a natural competitor to L-methionine, its activation by the enzyme is prevented by a proof-reading mechanism, structural requirements are determined form the crystal structure
-
?
additional information
?
-
-
no activity with the CAU to CUA initiator tRNAMet mutant in vivo
-
?
additional information
?
-
-
no activity with the CAU to CUA initiator tRNAMet mutant in vivo
-
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
COFACTOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Ca2+
-
supports methionine-dependent ATP-diphosphate exchange with 14% of the efficiency of Mg2+
Co2+
-
supports methionine-dependent ATP-diphosphate exchange with 20% of the efficiency of Mg2+
K+
-
in presence of 15 mM Mg2+, K+ stimulates up to concentration of about 50 mM, inhibits at higher concentrations. Unable to stimulate aminoacylation in absence of Mg2+
KCl
Mg2+
Mn2+
NH4+
-
in presence of 15 mM Mg2+, NH4+ stimulates up to a concentration of about 50 mM, inhibits at higher concentrations. In presence of 0.5 mM Mg2+, NH4+ alone stimulates aminoacylation
Zn2+
additional information
-
enzyme lacks Zn2+ binding motif and contains no Zn2+
Mg2+
-
required. The Mg2+ ion has six atoms arranged in a square bipyramidal coordination shell and bridges the diphosphate and MetAMP products. It is interacting with two oxygen atoms from two different phosphoryl groups of the diphosphate, one oxygen from the MetAMP phosphoryl group, and three water molecules, though one of these is a bit distant for a typical Mg2+ ligand at approximately 2.5 A
Mn2+
-
enzyme binds 2 Mn2+ per dimer, no binding with the trypsin-modified monomer
Mn2+
-
supports methionine-dependent ATP-diphosphate exchange with 15% of the efficiency of Mg2+
Mn2+
-
optimal Mn2+/ATP ratio: 1 (ATP-diphosphate exchange), 1.5 (aminoacylation)
Zn2+
zinc is an absolute requirement for enzyme activity, binding site residues, overview
Zn2+
-
2 tightly bound Zn2+ per polypeptide chain, in the vicinity of the active site
Zn2+
-
2 binding sites, 0.14 mM tightly bound zinc is present in 1 mol of cytoplasmic isozyme, but not in the mitochondrial one, required for stability and activity of the cytoplasmic isozyme
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
(1R,3S)-3-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl) cyclohexanamine
-
(E)-N-[3-(1H-benzimidazol-1-yl)propyl]-1-(3,5-dimethoxyphenyl)methanimine
-
-
(E)-N-[3-(1H-benzimidazol-1-yl)propyl]-1-(4-bromophenyl)methanimine
-
-
(E)-N-[3-(1H-benzimidazol-1-yl)propyl]-1-(4-chlorophenyl)methanimine
-
-
(E)-N-[3-(1H-benzimidazol-1-yl)propyl]-1-(4-methoxyphenyl)methanimine
-
-
(R)-1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl) piperidin-3-amine
-
(R)-1-(5-chloro-3H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl) pyrrolidin-3-amine
-
(S)-1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl) piperidin-3-amine
-
(S)-1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorophenyl) piperidine-3-carboxamide
-
(S)-1-(5-chloro-3H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl) pyrrolidin-3-amine
-
(S)-3,5-dichloro-N-(1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)piperidin-3-yl)benzamide
-
(S)-5-chloro-2-(3-((3,5-dichlorobenzyl)oxy)piperidin-1-yl)-1H-imidazo[4,5-b]pyridine
-
1,4-anhydro-2-bromo-2,3,5-trideoxy-1-(1-fluoroethenyl)-3-methyl-5-([3-[(4-oxo-1,4-dihydroquinolin-2-yl)amino]propyl]amino)-1-thiopentitol
-
-
1-(3-(1H-benzo[d]imidazol-2-yl)piperidin-1-yl)-2-(3,5-dichlorophenyl) ethanone
-
1-(3-(4-chloro-1H-benzo[d]imidazol-2-yl)piperidin-1-yl)-2-(3,5-dichlorophenyl) ethanone
-
1-(3-(5,6-dichloro-1H-benzo[d]imidazol-2-yl)piperidin-1-yl)-2-(3,5-dichlorophenyl)ethanone
-
1-(3-(5-chloro-1H-benzo[d]imidazol-2-yl) piperidin-1-yl)-2-(3,5-dichlorophenyl) ethanone
-
1-(3-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)piperidin-1-yl)-2-(3,5-dichlorophenyl)ethanone
-
1-(3-(5-chloro-6-fluoro-1H-benzo[d]imidazol-2-yl)piperidin-1-yl)-2-(3,5-dichlorophenyl)ethanone
-
1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl)azepan-3-amine
-
1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl)azetidin-3-amine
-
1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl)piperidin-3-amine
-
1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl)piperidin-4-amine
-
1-[1-[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidene]-butyl]-azetidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
1-[1-[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidene]-butyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
1-[1-[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidene]-ethyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
1-[1-[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidene]-propyl]-azetidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
1-[1-[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidene]-propyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
1-[1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidene]-butyl]-azetidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
1-[1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidene]-butyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
1-[1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidene]-ethyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
1-[1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidene]-propyl]-azetidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
1-[1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidene]-propyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
1-[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-azetidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
1-[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-piperidine-3-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
1-[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-piperidine-4-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
1-[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-azetidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-piperidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-piperidine-3-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-piperidine-4-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
1-[2-(4-dichloro-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-piperidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
1-[[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidene]-phenyl-methyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
1-[[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidene]-phenyl-methyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
2-((5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)thio)-N-(3,5-dichlorobenzyl) ethanamine
-
2-(2-butyl-4-chloro-1-(4-nitrobenzyl)-1H-imidazol-5-yl)-2,4-dihydro-1Hbenzo[d][1,3]oxazine
-
-
2-(2-butyl-4-chloro-1-(4-phenoxybenzyl)-1H-imidazol-5-yl)-5-(4-methoxyphenyl)-1-oxa-3-azaspiro[5.5]undecane
-
-
2-(2-butyl-4-chloro-1H-imidazol-5-yl)-5-(4-methoxyphenyl)-1-oxa-3-azaspiro[5.5]undecane
-
-
2-(3,5-dichlorophenyl)-1-(3-(5-fluoro-1H-benzo[d]imidazol-2-yl)piperidin-1-yl)ethanone
-
2-(3-[[(4,6-dichloro-1H-indol-2-yl)methyl]amino]propoxy)quinazolin-4(1H)-one
-
-
2-([2-[([2-[(2-fluorophenyl)methoxy]naphthalen-1-yl]methyl)amino]ethyl]amino)ethan-1-ol
-
-
2-([2-[([2-[(4-fluorophenyl)methoxy]naphthalen-1-yl]methyl)amino]ethyl]amino)ethan-1-ol
-
-
2-([3-[(2,3-dichlorobenzyl)amino]propyl]amino)quinolin-4(1H)-one
-
77.9% inhibition at 50 nM
2-([3-[(2,4-dichlorobenzyl)amino]propyl]amino)quinolin-4(1H)-one
-
87.1% inhibition at 50 nM
2-([3-[(2,5-dichlorobenzyl)amino]propyl]amino)quinolin-4(1H)-one
-
93.1% inhibition at 50 nM
2-([3-[(2,6-dichlorobenzyl)amino]propyl]amino)quinolin-4(1H)-one
-
51.3% inhibition at 50 nM
2-([3-[(2-bromo-4-chloro-6-ethoxybenzyl)amino]propyl]amino)thieno[3,2-d]pyrimidin-4(1H)-one
2-([3-[(2-bromo-6-ethoxy-4-methoxybenzyl)amino]propyl]amino)thieno[3,2-d]pyrimidin-4(1H)-one
2-([3-[(2-chlorobenzyl)amino]propyl]amino)quinolin-4(1H)-one
-
31.8% inhibition at 50 nM
2-([3-[(3,4-dichlorobenzyl)amino]propyl]amino)quinolin-4(1H)-one
-
91.7% inhibition at 50 nM
2-([3-[(3,5-dibromobenzyl)amino]propyl]amino)-1,5,6,7-tetrahydro-4H-cyclopenta[d]pyrimidin-4-one
2-([3-[(3,5-dichlorobenzyl)amino]propyl]amino)-4a,8a-dihydroquinolin-4(1H)-one
-
2-([3-[(3,5-dichlorobenzyl)amino]propyl]amino)quinolin-4(1H)-one
-
99.2% inhibition at 50 nM
2-([3-[(3,5-difluorobenzyl)amino]propyl]amino)quinolin-4(1H)-one
-
45.8% inhibition at 50 nM
2-([3-[(3,5-dimethoxybenzyl)amino]propyl]amino)quinolin-4(1H)-one
-
35.3% inhibition at 50 nM
2-([3-[(3,5-dimethylbenzyl)amino]propyl]amino)quinolin-4(1H)-one
-
91.1% inhibition at 50 nM
2-([3-[(3-bromobenzyl)amino]propyl]amino)quinolin-4(1H)-one
-
82.7% inhibition at 50 nM
2-([3-[(3-chlorobenzyl)amino]propyl]amino)quinolin-4(1H)-one
-
97.3% inhibition at 50 nM
2-([3-[(3-ethoxybenzyl)amino]propyl]amino)quinolin-4(1H)-one
-
19.1% inhibition at 50 nM
2-([3-[(4-chlorobenzyl)amino]propyl]amino)quinolin-4(1H)-one
-
52.0% inhibition at 50 nM
2-([3-[(5,7-dibromo-1,2,3,4-tetrahydroquinolin-4-yl)amino]propyl]amino)thieno[3,2-d]pyrimidin-4(1H)-one
2-([3-[(7-bromo-5-chloro-1,2,3,4-tetrahydroquinolin-4-yl)amino]propyl]amino)quinazolin-4(1H)-one
2-([3-[(7-bromo-5-chloro-1,2,3,4-tetrahydroquinolin-4-yl)amino]propyl]amino)thieno[3,2-d]pyrimidin-4(1H)-one
2-([3-[(7-ethyl-5-iodo-1,2,3,4-tetrahydroquinolin-4-yl)amino]propyl]amino)quinazolin-4(1H)-one
2-([3-[(7-ethyl-5-iodo-1,2,3,4-tetrahydroquinolin-4-yl)amino]propyl]amino)thieno[3,2-d]pyrimidin-4(1H)-one
2-[(3-[[(3,5-dichlorophenyl)methyl]amino]propyl)amino]quinazolin-4(1H)-one
-
-
2-[(3-[[(3,5-dichlorophenyl)methyl]amino]propyl)amino]quinolin-4(1H)-one
-
2-[(3-[[(4,6-dichloro-1H-indol-2-yl)methyl](methyl)amino]propyl)amino]quinazolin-4(1H)-one
-
-
2-[(3-[[(4,6-dichloro-1H-indol-2-yl)methyl]amino]propyl)amino]quinazolin-4(1H)-one
-
DDDD806905, highly potent inhibitor, competitive inhibition with respect to L-methionine
2-[(3-[[3,5-bis(trifluoromethyl)benzyl]amino]propyl)amino]quinolin-4(1H)-one
-
36.9% inhibition at 50 nM
2-[(3-[[3-(trifluoromethoxy)benzyl]amino]propyl)amino]quinolin-4(1H)-one
-
56.5% inhibition at 50 nM
2-[([2-[(4-fluorophenyl)methoxy]naphthalen-1-yl]methyl)amino]ethan-1-ol
-
-
2-[([3-[(1H-benzimidazol-2-yl)amino]propyl]amino)methyl]-6-(trifluoromethyl)-1H-indole-4-peroxol
-
-
2-[2-allyloxy-3-(3,4-dichlorobenzylamino)-propylamino]-1H-quinolin-4-one
-
-
2-[2-amino-3-(3,4-dichlorobenzylamino)-propylamino]-1H-quinolin-4-one tri(trifluoroacetic acid)
-
-
2-[2-benzyloxy-3-(3,4-dichlorobenzylamino)-propylamino]-1H-quinolin-4-one
-
-
2-[2-[([3-[(1H-benzimidazol-2-yl)amino]propyl]amino)methyl]-4,6-dichloro-1H-indol-1-yl]ethan-1-ol
-
-
2-[3-(3,4-dichlorobenzylamino)-1-hydroxymethylpropylamino]-1H-quinolin-4-one
-
-
2-[3-(3,4-dichlorobenzylamino)-2-dimethylaminopropylamino]-1H-quinolin-4-one
-
-
2-[3-(3,4-dichlorobenzylamino)-2-ethoxypropylamino]-1H-quinolin-4-one
-
-
2-[3-(3,4-dichlorobenzylamino)-2-hydroxymethylpropylamino]-1H-quinolin-4-one
-
-
2-[3-(3,4-dichlorobenzylamino)-2-hydroxypropylamino]-1H-quinolin-4-one
-
-
2-[3-(3,4-dichlorobenzylamino)-2-isopropoxy-propylamino]-1H-quinolin-4-one
-
-
2-[3-(3,4-dichlorobenzylamino)-2-methoxymethylpropylamino]-1H-quinolin-4-one
-
-
2-[3-(3,4-dichlorobenzylamino)-2-methoxypropylamino]-1H-quinolin-4-one
-
-
2-[3-(3,4-dichlorobenzylamino)-4-hydroxybutylamino]-1H-quinolin-4-one
-
-
2-[3-[bis-(3,4-dichlorobenzyl)-amino]-2-dimethylamino-propylamino]-1H-quinolin-4-one
-
-
2-[[2-([[2-(benzyloxy)naphthalen-1-yl]methyl]amino)ethyl]amino]ethan-1-ol
-
-
2-[[3-(benzylamino)propyl]amino]quinolin-4(1H)-one
-
9.0% inhibition at 50 nM
3,5-dichloro-N-((1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)piperidin-3-yl)methyl)aniline
-
3,5-dichloro-N-[3-[(4-oxo-1,4-dihydroquinazolin-2-yl)amino]propyl]benzene-1-sulfonamide
-
-
3-(1H-benzimidazol-1-yl)-N-[(3,5-dimethoxyphenyl)methyl]propan-1-amine
-
-
3-(1H-benzimidazol-1-yl)-N-[(4-bromophenyl)methyl]propan-1-amine
-
-
3-(1H-benzimidazol-1-yl)-N-[(4-chlorophenyl)methyl]propan-1-amine
-
-
3-(1H-benzimidazol-1-yl)-N-[(4-methoxyphenyl)methyl]propan-1-amine
-
-
3-(5-chloro-1H-benzo[d]imidazol-2-yl)-N-(3,5-dichlorobenzyl)cyclohexanamine
-
3-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N-(3,5-dichlorobenzyl) cyclohexanamine
-
3-(5-chloro-3H-imidazo [4,5-b] pyridin-2-yl)-N-(3,5-dichlorobenzyl)propan-1-amine
-
3-(6-chloro-1H-benzo[d]imidazol-2-yl)-N-(3,5-dichlorobenzyl) propan-1-amine
-
3-[([3-[(4-oxo-1,4-dihydroquinolin-2-yl)amino]propyl]amino)methyl]benzonitrile
-
20.2% inhibition at 50 nM
4'-((2-butyl-4-chloro-5-(5-(4-methoxyphenyl)-1-oxa-3-azaspiro[5.5]undecan-2-yl)-1H-imidazol-1-yl)methyl)-[1,1'-biphenyl]-2-carbonitrile
-
-
4'-[(3-[5-[4-(hydroxymethyl)phenyl]-1-oxa-3-azaspiro[5.5]undecan-2-yl]-2,3-dihydro-1H-indol-1-yl)methyl][1,1'-biphenyl]-2-carbonitrile
-
-
4'-[[3-(1,4-dihydro-2H-3,1-benzoxazin-2-yl)-1H-indol-1-yl]methyl][1,1'-biphenyl]-2-carbonitrile
-
-
4-(1H-benzimidazol-2-yl)-N-[(2-chloro-6-fluorophenyl)methyl]aniline
-
-
4-(5-(4-methoxyphenyl)-1-oxa-3-azaspiro[5.5]undecan-2-yl)-N,Ndimethylaniline
-
-
4-[(E)-[([[N-(thiophen-2-ylcarbonyl)glycyl]amino]methyl)imino]methyl]benzoic acid
-
structure molecular modeling, binding mode, detailed overview
4-[4-[(1H-benzimidazol-2-ylmethyl)amino]-6-(2-chloro-4-methoxyphenoxy)pyrimidin-2-yl]piperazin-2-one
-
5-(4-methoxyphenyl)-2-(2-methyl-1H-indol-3-yl)-1-oxa-3-azaspiro[5.5]undecane
-
-
5-(4-methoxyphenyl)-2-(2-phenyl-1H-indol-3-yl)-1-oxa-3-azaspiro[5.5]undecane
-
-
5-([3-[(6,8-dibromo-3,4-dihydro-2H-1-benzopyran-4-yl)amino]propyl]amino)thieno[3,2-b]pyridin-7(4H)-one
-
-
5-chloro-2-(1-(3,5-dichlorophenethyl)piperidin-3-yl)-1H-imidazo[4,5-b]pyridine
-
9-(3-[(E)-[(3,5-dimethoxyphenyl)methylidene]amino]propyl)-9H-purin-6-amine
-
-
9-(3-[(E)-[(4-bromophenyl)methylidene]amino]propyl)-9H-purin-6-amine
-
-
9-(3-[(E)-[(4-chlorophenyl)methylidene]amino]propyl)-9H-purin-6-amine
-
-
9-(3-[(E)-[(4-methoxyphenyl)methylidene]amino]propyl)-9H-purin-6-amine
-
-
9-(3-[[(3,5-dimethoxyphenyl)methyl]amino]propyl)-9H-purin-6-amine
-
-
actinomycin D
-
inhibits the nucleolar located enzyme due to dependence on polymerase I
adenosine
-
maximal inhibition at MgCl2 concentration from 4.0 mM to 10 mM, effective inhibition at high concentration of diphosphate
alpha-Amanitin
-
inhibits the nucleolar located enzyme due to dependence on polymerase I
benzoic acid 1-[(3,4-dichlorobenzylamino)-methyl]-2-(4-oxo-1,4-dihydroquinolin-2-ylamino)-ethyl ester
-
-
cisplatin
-
inhibits the nucleolar located enzyme due to dependence on polymerase I
ester analogues of L-methionyl adenylate
-
overview, modeling of interaction with the active site
hydroxamate analogues of L-methionyl adenylate
-
overview, modeling of the interaction with the active site
isovanilloid analogues of L-methionyl adenylate
-
overview, containing ribose biooisosteres
L-methionine hydroxamate
-
substrate analogue, inhibition mechanism, no inhibition of mutant T10M
N-(1H-benzimidazol-2-yl)-N'-(3,5-dichlorobenzyl)propane-1,3-diamine
-
N-(3-[[(2,5-dichlorothiophen-3-yl)methyl]amino]propyl)-N'-thiophen-3-ylurea
-
N-(3-[[(2-methyl-1-benzothiophen-3-yl)methyl]amino]propyl)-N'-thiophen-3-ylurea
-
N-(3-[[(3,5-dichlorophenyl)methyl]amino]propyl)-N'-(2-hydroxyphenyl)urea
-
N-(3-[[(3,5-dichlorophenyl)methyl]amino]propyl)-N'-(3-hydroxyphenyl)urea
-
N-(3-[[(3-chloro-5-methoxyphenyl)methyl]amino]propyl)-N'-thiophen-3-ylurea
-
N-(3-[[(5-chloro-2-ethoxy-3-iodophenyl)methyl]amino]propyl)-N'-thiophen-3-ylurea
-
N-(3-[[(5-chloro-2-hydroxyphenyl)methyl]amino]propyl)-N'-thiophen-3-ylurea
-
N-(6,8-dibromo-1,2,3,4-tetrahydroquinolin-4-yl)-N'-1H-imidazo[4,5-b]pyridin-2-ylpropane-1,3-diamine
N-(7-ethyl-5-iodo-1,2,3,4-tetrahydroquinolin-4-yl)-N'-1H-imidazo[4,5-b]pyridin-2-ylpropane-1,3-diamine
N-1H-benzimidazol-2-yl-N'-(5,7-dibromo-1,2,3,4-tetrahydroquinolin-4-yl)propane-1,3-diamine
N-1H-benzimidazol-2-yl-N'-(7-ethyl-5-iodo-1,2,3,4-tetrahydroquinolin-4-yl)propane-1,3-diamine
N-[(3,5-dichlorophenyl)methyl]-3-[(4-oxo-1,4-dihydroquinazolin-2-yl)amino]propanamide
-
-
N-[(4R)-6,8-dibromo-1,2,3,4-tetrahydroquinolin-4-yl]-N'-1H-imidazo[4,5-b]pyridin-2-ylpropane-1,3-diamine
N-[(4S)-6,8-dibromo-1,2,3,4-tetrahydroquinolin-4-yl]-N'-1H-imidazo[4,5-b]pyridin-2-ylpropane-1,3-diamine
N-[3-([[2-(benzyloxy)-5-chloro-3-(prop-2-en-1-yl)phenyl]methyl]amino)propyl]-N'-thiophen-3-ylurea
-
N-[3-([[5-chloro-2-hydroxy-3-(prop-2-en-1-yl)phenyl]methyl]amino)propyl]-N'-thiophen-3-ylurea
-
N-[3-[(1H-benzimidazol-2-yl)amino]propyl]-3-(trifluoromethoxy)benzamide
-
-
N-[3-[([5-chloro-3-(prop-2-en-1-yl)-2-[(prop-2-en-1-yl)oxy]phenyl]methyl)amino]propyl]-N'-thiophen-3-ylurea
-
N-[[(1R)-2-[[(4,6-dichloro-1H-indol-2-yl)methyl]amino]cyclopentyl]methyl]-1H-benzimidazol-2-amine
-
-
N1-(1H-benzimidazol-2-yl)-N3-(6,8-dichloro-3,4-dihydro-2H-1-benzopyran-4-yl)propane-1,3-diamine
-
-
N1-(1H-benzimidazol-2-yl)-N3-[(3,5-dichloro-2-ethoxyphenyl)methyl]propane-1,3-diamine
-
-
N1-(1H-benzimidazol-2-yl)-N3-[(3,5-dichlorophenyl)methyl]propane-1,3-diamine
-
N1-(1H-benzimidazol-2-yl)-N3-[(3,6-dichloro-1H-indol-2-yl)methyl]propane-1,3-diamine
-
-
N1-(1H-benzimidazol-2-yl)-N3-[(3-bromo-2-ethoxy-5-methylphenyl)methyl]propane-1,3-diamine
-
-
N1-(1H-benzimidazol-2-yl)-N3-[(3-bromo-5-chloro-2-ethoxyphenyl)methyl]propane-1,3-diamine
-
-
N1-(1H-benzimidazol-2-yl)-N3-[(4,6-dichloro-3-methyl-1H-indol-2-yl)methyl]propane-1,3-diamine
-
-
N1-(1H-benzimidazol-2-yl)-N3-[(4,7-dichloro-1H-indol-2-yl)methyl]propane-1,3-diamine
-
-
N1-(1H-benzimidazol-2-yl)-N3-[[4,6-bis(trifluoromethyl)-1H-indol-2-yl]methyl]propane-1,3-diamine
-
-
N1-(1H-benzimidazol-2-yl)-N3-[[6-methoxy-4-(trifluoromethyl)-1H-indol-2-yl]methyl]propane-1,3-diamine
-
-
N1-(5-chloro-1H-imidazo[4,5-b]pyridin-2-yl)-N2-[(3,5-dichlorophenyl)methyl]-N1-methylethane-1,2-diamine
-
N1-(5-chloro-3H-imidazo[4,5-b]pyridin-2-yl)-N2-(3,5-dichlorobenzyl) ethane-1,2-diamine
-
N1-(6,8-dibromo-1,2,3,4-tetrahydroquinolin-4-yl)-N3-(1H-imidazo[4,5-b]pyridin-2-yl)propane-1,3-diamine
-
-
N1-(6-chloro-1H-benzo[d]imidazol-2-yl)-N2-(3,5-dichlorobenzyl)ethane-1,2-diamine
-
N1-[(3,5-dibromophenyl)methyl]-N3-(7-methoxy-1H-benzimidazol-2-yl)propane-1,3-diamine
-
-
N1-[(3,5-dichloro-4-propylphenyl)methyl]-N3-(3H-imidazo[4,5-c]pyridin-2-yl)propane-1,3-diamine
-
-
N1-[(4,5-dibromo-3-methylthiophen-2-yl)methyl]-N3-(3H-imidazo[4,5-c]pyridin-2-yl)propane-1,3-diamine
-
-
N1-[(4,6-dimethyl-1H-indol-2-yl)methyl]-N3-(1H-imidazo[4,5-b]pyridin-2-yl)propane-1,3-diamine
-
-
N1-[(5-bromo-2-ethoxy-3-methoxyphenyl)methyl]-N3-(1H-imidazo[4,5-b]pyridin-2-yl)propane-1,3-diamine
-
-
N1-[[4-bromo-5-(1-fluoroethenyl)-3-methylthiophen-2-yl]methyl]-N3-(1H-imidazo[4,5-c]pyridin-2-yl)propane-1,3-diamine
-
-
N1-[[4-bromo-5-(difluoromethyl)-3-methylthiophen-2-yl]methyl]-N3-(1H-imidazo[4,5-c]pyridin-2-yl)propane-1,3-diamine
-
-
N1-[[4-chloro-3-(trifluoromethyl)phenyl]methyl]-N3-(1H-imidazo[4,5-c]pyridin-2-yl)-2-propylpropane-1,3-diamine
-
-
N1-[[4-chloro-3-(trifluoromethyl)phenyl]methyl]-N3-(3H-imidazo[4,5-c]pyridin-2-yl)propane-1,3-diamine
-
-
vanilloid analogues of L-methionyl adenylate
-
overview, containing ribose biooisosteres
[1-[(3,4-dichlorobenzylamino)-methyl]-2-(4-oxo-1,4-dihydroquinolin-2-ylamino)ethyl]-carbamic acid tert-butyl ester
-
-
[2-[([3-[(1H-benzimidazol-2-yl)amino]propyl]amino)methyl]-4,6-dichlorophenyl]methanol
-
-
[3-(1H-benzimidazol-2-yl)piperidin-1-yl](2-methyl-1-benzofuran-5-yl)methanone
78% and 20% inhibition at 0.1 and 0.01 mM, respectively
1,10-phenanthroline
-
little or no inhibition by 1,7-phenanthroline and 4,7-phenanthroline
1,10-phenanthroline
-
complete inhibition of the cytoplasmic isozyme at 1 mM
1-[1-[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidene]-butyl]-azetidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is 0.0035 mM
1-[1-[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidene]-butyl]-azetidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is 40 nM
1-[1-[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidene]-butyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is 0.099 mM
1-[1-[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidene]-butyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is 170 nM
1-[1-[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidene]-ethyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is 0.0066 mM
1-[1-[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidene]-ethyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is 340 nM
1-[1-[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidene]-propyl]-azetidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is 0.0035 mM
1-[1-[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidene]-propyl]-azetidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is 18 nM
1-[1-[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidene]-propyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is 0.0013 mM
1-[1-[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidene]-propyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is 180 nM
1-[1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidene]-butyl]-azetidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is above 0.001 mM
1-[1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidene]-butyl]-azetidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is 87 nM
1-[1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidene]-butyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is 0.0031 mM
1-[1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidene]-butyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is 760 nM
1-[1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidene]-ethyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is above 0.1 mM
1-[1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidene]-ethyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is 1670 nM
1-[1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidene]-propyl]-azetidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is 0.099 mM
1-[1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidene]-propyl]-azetidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is 170 nM
1-[1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidene]-propyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is 0.0059 mM
1-[1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidene]-propyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is 850 nM
1-[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-azetidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is above 0.1 mM
1-[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-azetidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is 70 nM
1-[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-piperidine-3-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
-
1-[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-piperidine-3-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
-
1-[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-piperidine-4-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
-
1-[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-piperidine-4-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
-
1-[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is above 0.1 mM
1-[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is 680 nM
1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-azetidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is above 0.1 mM
1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-azetidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is 510 nM
1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-piperidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
-
1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-piperidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
-
1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-piperidine-3-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
-
1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-piperidine-3-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
-
1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-piperidine-4-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
-
1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-piperidine-4-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
-
1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
-
1-[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is 1100 nM
1-[2-(4-dichloro-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-piperidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
-
1-[2-(4-dichloro-phenyl)-5-oxo-oxazol-4-ylidenemethyl]-piperidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
-
1-[[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidene]-phenyl-methyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is 0.027 mM
1-[[2-(2,4-dichloro-phenyl)-5-oxo-oxazol-4-ylidene]-phenyl-methyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is 430 nM
1-[[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidene]-phenyl-methyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is 0.0061 mM
1-[[2-(4-bromo-phenyl)-5-oxo-oxazol-4-ylidene]-phenyl-methyl]-pyrrolidine-2-carboxylic acid [1-carbamoyl-2-(4-hydroxy-phenyl)-ethyl]-amide
-
IC50 is 810 nM
2-([3-[(2,3,5-trichlorobenzyl)amino]propyl]amino)-4H-chromen-4-one
-
IC50 is 0.001 mM
2-([3-[(2,3,5-trichlorobenzyl)amino]propyl]amino)quinolin-4(1H)-one
-
-
2-([3-[(2,3,5-trichlorobenzyl)amino]propyl]amino)quinolin-4(1H)-one
-
IC50 is below 0.3 nM
2-([3-[(2,4-dibromo-6-ethoxybenzyl)amino]propyl]amino)quinazolin-4(1H)-one
-
-
2-([3-[(2,4-dibromo-6-ethoxybenzyl)amino]propyl]amino)quinazolin-4(1H)-one
-
IC50 is 9.7 nM
2-([3-[(2,4-dibromo-6-ethoxybenzyl)amino]propyl]amino)thieno[3,2-d]pyrimidin-4(1H)-one
-
-
2-([3-[(2,4-dibromo-6-ethoxybenzyl)amino]propyl]amino)thieno[3,2-d]pyrimidin-4(1H)-one
-
IC50 is 4.9 nM
2-([3-[(2,4-dichloro-6-ethoxybenzyl)amino]propyl]amino)quinazolin-4(1H)-one
-
-
2-([3-[(2,4-dichloro-6-ethoxybenzyl)amino]propyl]amino)quinazolin-4(1H)-one
-
IC50 is below 3 nM
2-([3-[(2,4-dichloro-6-ethoxybenzyl)amino]propyl]amino)thieno[3,2-d]pyrimidin-4(1H)-one
-
-
2-([3-[(2,4-dichloro-6-ethoxybenzyl)amino]propyl]amino)thieno[3,2-d]pyrimidin-4(1H)-one
-
IC50 is below 3 nM
2-([3-[(2-bromo-4-chloro-6-ethoxybenzyl)amino]propyl]amino)quinazolin-4(1H)-one
-
-
2-([3-[(2-bromo-4-chloro-6-ethoxybenzyl)amino]propyl]amino)quinazolin-4(1H)-one
-
IC50 is below 3 nM
2-([3-[(2-bromo-4-chloro-6-ethoxybenzyl)amino]propyl]amino)thieno[3,2-d]pyrimidin-4(1H)-one
-
-
2-([3-[(2-bromo-4-chloro-6-ethoxybenzyl)amino]propyl]amino)thieno[3,2-d]pyrimidin-4(1H)-one
-
IC50 is below 3 nM
2-([3-[(2-bromo-6-ethoxy-4-methoxybenzyl)amino]propyl]amino)quinazolin-4(1H)-one
-
-
2-([3-[(2-bromo-6-ethoxy-4-methoxybenzyl)amino]propyl]amino)quinazolin-4(1H)-one
-
IC50 is 7.0 nM
2-([3-[(2-bromo-6-ethoxy-4-methoxybenzyl)amino]propyl]amino)thieno[3,2-d]pyrimidin-4(1H)-one
-
-
2-([3-[(2-bromo-6-ethoxy-4-methoxybenzyl)amino]propyl]amino)thieno[3,2-d]pyrimidin-4(1H)-one
-
IC50 is 3.3 nM
2-([3-[(3,4-dichlorobenzyl)amino]propyl]thio)quinolin-4(1H)-one
-
IC50 is 680 nM
2-([3-[(3,5-dibromo-2-ethoxybenzyl)amino]propyl]amino)quinolin-4(1H)-one
-
98.2% inhibition at 50 nM
2-([3-[(3,5-dibromo-2-ethoxybenzyl)amino]propyl]amino)quinolin-4(1H)-one
-
2-([3-[(3,5-dibromo-2-methoxybenzyl)amino]propyl]amino)quinolin-4(1H)-one
-
95.0% inhibition at 50 nM
2-([3-[(3,5-dibromo-2-methoxybenzyl)amino]propyl]amino)quinolin-4(1H)-one
-
2-([3-[(3,5-dibromobenzyl)amino]propyl]amino)-1,5,6,7-tetrahydro-4H-cyclopenta[d]pyrimidin-4-one
-
-
2-([3-[(3,5-dibromobenzyl)amino]propyl]amino)-1,5,6,7-tetrahydro-4H-cyclopenta[d]pyrimidin-4-one
-
IC50 is 580 nM
2-([3-[(3,5-dibromobenzyl)amino]propyl]amino)-1H-indole-3-carbonitrile
-
-
2-([3-[(3,5-dibromobenzyl)amino]propyl]amino)-1H-indole-3-carbonitrile
-
IC50 is 54 nM
2-([3-[(3,5-dibromobenzyl)amino]propyl]amino)-6-phenylpyrimidin-4(1H)-one
-
-
2-([3-[(3,5-dibromobenzyl)amino]propyl]amino)-6-phenylpyrimidin-4(1H)-one
-
IC50 is 0.001 mM
2-([3-[(3,5-dibromobenzyl)amino]propyl]amino)quinazolin-4(1H)-one
-
IC50 is 8.1 nM
2-([3-[(3,5-dibromobenzyl)amino]propyl]amino)quinolin-4(1H)-one
-
IC50 is below 3 nM
2-([3-[(3,5-dibromobenzyl)amino]propyl]amino)quinolin-4(1H)-one
-
98.8% inhibition at 50 nM
2-([3-[(3,5-dibromobenzyl)amino]propyl]amino)thieno[2,3-d]pyrimidin-4(1H)-one
-
-
2-([3-[(3,5-dibromobenzyl)amino]propyl]amino)thieno[2,3-d]pyrimidin-4(1H)-one
-
IC50 is 150 nM
2-([3-[(3,5-dibromobenzyl)amino]propyl]amino)thieno[3,2-d]pyrimidin-4(1H)-one
-
-
2-([3-[(3,5-dibromobenzyl)amino]propyl]amino)thieno[3,2-d]pyrimidin-4(1H)-one
-
IC50 is 3.9 nM
2-([3-[(5,7-dibromo-1,2,3,4-tetrahydroquinolin-4-yl)amino]propyl]amino)thieno[3,2-d]pyrimidin-4(1H)-one
-
-
2-([3-[(5,7-dibromo-1,2,3,4-tetrahydroquinolin-4-yl)amino]propyl]amino)thieno[3,2-d]pyrimidin-4(1H)-one
-
IC50 is 14 nM
2-([3-[(7-bromo-5-chloro-1,2,3,4-tetrahydroquinolin-4-yl)amino]propyl]amino)quinazolin-4(1H)-one
-
-
2-([3-[(7-bromo-5-chloro-1,2,3,4-tetrahydroquinolin-4-yl)amino]propyl]amino)quinazolin-4(1H)-one
-
IC50 is 8.2 nM
2-([3-[(7-bromo-5-chloro-1,2,3,4-tetrahydroquinolin-4-yl)amino]propyl]amino)thieno[3,2-d]pyrimidin-4(1H)-one
-
-
2-([3-[(7-bromo-5-chloro-1,2,3,4-tetrahydroquinolin-4-yl)amino]propyl]amino)thieno[3,2-d]pyrimidin-4(1H)-one
-
IC50 is below 3 nM
2-([3-[(7-ethyl-5-iodo-1,2,3,4-tetrahydroquinolin-4-yl)amino]propyl]amino)quinazolin-4(1H)-one
-
-
2-([3-[(7-ethyl-5-iodo-1,2,3,4-tetrahydroquinolin-4-yl)amino]propyl]amino)quinazolin-4(1H)-one
-
IC50 is 17 nM
2-([3-[(7-ethyl-5-iodo-1,2,3,4-tetrahydroquinolin-4-yl)amino]propyl]amino)thieno[3,2-d]pyrimidin-4(1H)-one
-
-
2-([3-[(7-ethyl-5-iodo-1,2,3,4-tetrahydroquinolin-4-yl)amino]propyl]amino)thieno[3,2-d]pyrimidin-4(1H)-one
-
IC50 is below 3 nM
2-[3-[(3,4-dichlorobenzyl)amino]propoxy]quinolin-4(1H)-one
-
IC50 is 38 nM
3-([3-[(2,3,5-trichlorobenzyl)amino]propyl]amino)-1,4-dihydronaphthalen-1-ol
-
-
3-([3-[(2,3,5-trichlorobenzyl)amino]propyl]amino)-1,4-dihydronaphthalen-1-ol
-
IC50 is 0.0018 mM
5-([3-[(3,5-dibromobenzyl)amino]propyl]amino)thieno[3,2-b]pyridin-7(4H)-one
-
-
5-([3-[(3,5-dibromobenzyl)amino]propyl]amino)thieno[3,2-b]pyridin-7(4H)-one
-
IC50 is 4 nM
6-([3-[(3,5-dibromobenzyl)amino]propyl]amino)thieno[2,3-b]pyridin-4(7H)-one
-
-
6-([3-[(3,5-dibromobenzyl)amino]propyl]amino)thieno[2,3-b]pyridin-4(7H)-one
-
IC50 is 6.2 nM
N-(1,4-dihydroquinolin-2-yl)-N'-(2,3,5-trichlorobenzyl)propane-1,3-diamine
-
-
N-(1,4-dihydroquinolin-2-yl)-N'-(2,3,5-trichlorobenzyl)propane-1,3-diamine
-
IC50 is 0.0001 mM
N-(3,5-dibromobenzyl)-N'-1H-imidazo[4,5-b]pyridin-2-ylpropane-1,3-diamine
-
-
N-(3,5-dibromobenzyl)-N'-1H-imidazo[4,5-b]pyridin-2-ylpropane-1,3-diamine
-
IC50 is 5.0 nM
N-(3-[[(3,5-dichlorophenyl)methyl]amino]propyl)-N'-thiophen-3-ylurea
-
N-(3-[[(3,5-dichlorophenyl)methyl]amino]propyl)-N'-thiophen-3-ylurea
-
N-(3-[[(3-chloro-5-methoxyphenyl)methyl]amino]propyl)-N'-phenylurea
-
N-(3-[[(3-chloro-5-methoxyphenyl)methyl]amino]propyl)-N'-phenylurea
-
N-(6,8-dibromo-1,2,3,4-tetrahydroquinolin-4-yl)-N'-1H-imidazo[4,5-b]pyridin-2-ylpropane-1,3-diamine
-
-
N-(6,8-dibromo-1,2,3,4-tetrahydroquinolin-4-yl)-N'-1H-imidazo[4,5-b]pyridin-2-ylpropane-1,3-diamine
-
-
N-(6,8-dibromo-1,2,3,4-tetrahydroquinolin-4-yl)-N'-1H-imidazo[4,5-b]pyridin-2-ylpropane-1,3-diamine
-
IC50 is 11 nM
N-(6,8-dibromo-1,2,3,4-tetrahydroquinolin-4-yl)-N'-1H-imidazo[4,5-b]pyridin-2-ylpropane-1,3-diamine
-
-
N-(7-ethyl-5-iodo-1,2,3,4-tetrahydroquinolin-4-yl)-N'-1H-imidazo[4,5-b]pyridin-2-ylpropane-1,3-diamine
-
-
N-(7-ethyl-5-iodo-1,2,3,4-tetrahydroquinolin-4-yl)-N'-1H-imidazo[4,5-b]pyridin-2-ylpropane-1,3-diamine
-
IC50 is 18 nM
N-1H-benzimidazol-2-yl-N'-(2,4-dibromo-6-ethoxybenzyl)propane-1,3-diamine
-
-
N-1H-benzimidazol-2-yl-N'-(2,4-dibromo-6-ethoxybenzyl)propane-1,3-diamine
-
IC50 is 17 nM
N-1H-benzimidazol-2-yl-N'-(2,4-dichloro-6-ethoxybenzyl)propane-1,3-diamine
-
-
N-1H-benzimidazol-2-yl-N'-(2,4-dichloro-6-ethoxybenzyl)propane-1,3-diamine
-
IC50 is below 3 nM
N-1H-benzimidazol-2-yl-N'-(2-bromo-4-chloro-6-ethoxybenzyl)propane-1,3-diamine
-
-
N-1H-benzimidazol-2-yl-N'-(2-bromo-4-chloro-6-ethoxybenzyl)propane-1,3-diamine
-
IC50 is 3.8 nM
N-1H-benzimidazol-2-yl-N'-(2-bromo-6-ethoxy-4-methoxybenzyl)propane-1,3-diamine
-
-
N-1H-benzimidazol-2-yl-N'-(2-bromo-6-ethoxy-4-methoxybenzyl)propane-1,3-diamine
-
IC50 is 17 nM
N-1H-benzimidazol-2-yl-N'-(3,5-dibromobenzyl)propane-1,3-diamine
-
IC50 is 29 nM
N-1H-benzimidazol-2-yl-N'-(5,7-dibromo-1,2,3,4-tetrahydroquinolin-4-yl)propane-1,3-diamine
-
-
N-1H-benzimidazol-2-yl-N'-(5,7-dibromo-1,2,3,4-tetrahydroquinolin-4-yl)propane-1,3-diamine
-
IC50 is 14 nM
N-1H-benzimidazol-2-yl-N'-(7-ethyl-5-iodo-1,2,3,4-tetrahydroquinolin-4-yl)propane-1,3-diamine
-
-
N-1H-benzimidazol-2-yl-N'-(7-ethyl-5-iodo-1,2,3,4-tetrahydroquinolin-4-yl)propane-1,3-diamine
-
IC50 is 16 nM
N-[(4R)-6,8-dibromo-1,2,3,4-tetrahydroquinolin-4-yl]-N'-1H-imidazo[4,5-b]pyridin-2-ylpropane-1,3-diamine
-
-
N-[(4R)-6,8-dibromo-1,2,3,4-tetrahydroquinolin-4-yl]-N'-1H-imidazo[4,5-b]pyridin-2-ylpropane-1,3-diamine
-
IC50 is 6.3 nM
N-[(4S)-6,8-dibromo-1,2,3,4-tetrahydroquinolin-4-yl]-N'-1H-imidazo[4,5-b]pyridin-2-ylpropane-1,3-diamine
-
-
N-[(4S)-6,8-dibromo-1,2,3,4-tetrahydroquinolin-4-yl]-N'-1H-imidazo[4,5-b]pyridin-2-ylpropane-1,3-diamine
-
IC50 is 48 nM
REP3123
-
active against a collection of 108 clinical isolates of Clostridium difficile and against epidemic, moxifloxacin-resistant BI/NAP1/027 strains
REP3123
a selective and potent competitive, versus methionine not ATP, MetRS inhibitor, that strongly binds at the active site, docking study
[3-[4-(4-Methoxy-benzyloxy)-quinolin-2-ylsulfanyl]-propyl]-carbamic acid tert-butyl ester
-
-
[3-[4-(4-Methoxy-benzyloxy)-quinolin-2-ylsulfanyl]-propyl]-carbamic acid tert-butyl ester
-
-
additional information
MetRS drug design and homology modelling, overview
-
additional information
-
MetRS drug design and homology modelling, overview
-
additional information
-
structure-activity relationships of inhibitor derived from an oxazolone-dipeptide scaffold
-
additional information
-
antibacterial potency of the inhibitors, structure-activity relationships, inhibition mechanism, the quinolone moiety of the right hand side pharmacophore is crucial for enzyme inhibition, overview
-
additional information
-
inhibition mechanism, the quinolone moiety of the right hand side pharmacophore is crucial for enzyme inhibition, overview
-
additional information
-
large scale MetRS inhibitor screening, diverse compounds, overview
-
additional information
-
structure-activity relationships of inhibitor derived from an oxazolone-dipeptide scaffold
-
additional information
-
antibacterial potency of the inhibitors, structure-activity relationships, inhibition mechanism, the quinolone moiety of the right hand side pharmacophore is crucial for enzyme inhibition, overview
-
additional information
-
in vitro minimum inhibitory concentrations of quinoline compounds with different strains of Staphylococcus aureus, structure-activity relationships
-
additional information
-
inhibitor screening, hstructures, omology modeling, molecular docking studies, and computational development of pharmacophore models, overview; inhibitor screening, structures, homology modeling, molecular docking studies, and computational development of pharmacophore models, overview
-
additional information
-
inhibition mechanism, the quinolone moiety of the right hand side pharmacophore is crucial for enzyme inhibition, overview
-
additional information
-
a homology model of the Trypanosoma brucei MetRS based on other MetRS structures is used to model binding of lead diaryl diamine compounds in the design and development of selective parasite MetRS inhibitors for treatment of African trypanosomiasis, overview
-
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ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
12 kDa protein 2
the recombinant 12 kDa protein 2 plays an important role in dimerization of the enzyme
-
elongation factor EF-1alpha
-
activates, assists in dissociation of Met-tRNAMet from the enzyme, the aminoacylated tRNA is transfered from to the enzyme to the elongation factor
-
spermine
slight stimulation, additionally spermine increases the enzyme activity by stabilizing conformation of negatively charged DNA
5SrRNA
-
positive effector of MetRS, markedly enhances the MetRS activity in the MetRS complex
-
Arc1p-N
residues 1-122 of Arc1p, recombinantly expressed, crystal structure analysis, three interacting domains, MetRS-N–Arc1p-N hetero-dimer resembles a classical GST homo-dimer, overview
-
Arc1p-N
residues 1-122 of Arc1p, recombinantly expressed, crystal structure analysis, three interacting domains, MetRS-N-Arc1p-N hetero-dimer resembles a classical GST homo-dimer, overview
-
additional information
bovine serum albumin has no effect on the enzyme
-
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DISEASE
TITLE OF PUBLICATION
LINK TO PUBMED
Anemia
Mutations in methionyl-tRNA synthetase gene in a Chinese family with interstitial lung and liver disease, postnatal growth failure and anemia.
Anthrax
Horizontal transfer of drug-resistant aminoacyl-transfer-RNA synthetases of anthrax and Gram-positive pathogens.
Ataxia
Mutations in the mitochondrial methionyl-tRNA synthetase cause a neurodegenerative phenotype in flies and a recessive ataxia (ARSAL) in humans.
Bile Duct Neoplasms
New staining method using methionyl-tRNA synthetase 1 antibody for brushing cytology of bile duct cancer.
Breast Neoplasms
High methionyl-tRNA synthetase expression predicts poor prognosis in patients with breast cancer.
Brucellosis
Brucella melitensis Methionyl-tRNA-Synthetase (MetRS), a Potential Drug Target for Brucellosis.
Brucellosis
Correction: Brucella melitensis Methionyl-tRNA-Synthetase (MetRS), a Potential Drug Target for Brucellosis.
Brucellosis
High Throughput Virtual Screening to Identify Novel natural product Inhibitors for MethionyltRNA-Synthetase of Brucella melitensis.
Carcinoma
Cloning of a human cDNA encoding a protein with high homology to yeast methionyl-tRNA synthetase.
Carcinoma, Non-Small-Cell Lung
Methionyl-tRNA Synthetase is a Useful Diagnostic Marker for Lymph Node Metastasis in Non-Small Cell Lung Cancer.
Carcinoma, Non-Small-Cell Lung
Methionyl-tRNA synthetase overexpression is associated with poor clinical outcomes in non-small cell lung cancer.
Clostridium Infections
Inhibitory effect of REP3123 on toxin and spore formation in Clostridium difficile, and in vivo efficacy in a hamster gastrointestinal infection model.
Clostridium Infections
Spectrum of activity and mode of action of REP3123, a new antibiotic to treat Clostridium difficile infections.
Decompression Sickness
Topographic modeling of free and methionyl-tRNA synthetase bound tRNAfMet by singlet-singlet energy transfer: bending of the 3'-terminal arm in tRNAfMet.
Gram-Positive Bacterial Infections
Development of methionyl-tRNA synthetase inhibitors as antibiotics for Gram-positive bacterial infections.
Heart Defects, Congenital
Inhibiting MARSs reduces hyperhomocysteinemia-associated neural tube and congenital heart defects.
Infections
Induced resistance to methionyl-tRNA synthetase inhibitors in Trypanosoma brucei is due to overexpression of the target.
Infections
Inhibitory effect of REP3123 on toxin and spore formation in Clostridium difficile, and in vivo efficacy in a hamster gastrointestinal infection model.
Infections
Methionyl-tRNA synthetase inhibitor has potent in vivo activity in a novel Giardia lamblia luciferase murine infection model.
Infections
Selective inhibitors of methionyl-tRNA synthetase have potent activity on Trypanosoma brucei infection in mice.
Infections
Spectrum of activity and mode of action of REP3123, a new antibiotic to treat Clostridium difficile infections.
Liver Diseases
Mutations in methionyl-tRNA synthetase gene in a Chinese family with interstitial lung and liver disease, postnatal growth failure and anemia.
Liver Diseases
Novel methionyl-tRNA synthetase gene variants/phenotypes in interstitial lung and liver disease: A case report and review of literature.
Lung Neoplasms
Methionyl-tRNA Synthetase is a Useful Diagnostic Marker for Lymph Node Metastasis in Non-Small Cell Lung Cancer.
Lung Neoplasms
Methionyl-tRNA synthetase overexpression is associated with poor clinical outcomes in non-small cell lung cancer.
Metabolic Syndrome
A 3-SNP gene risk score and a metabolic risk score both predict hypertriglyceridemia and cardiovascular disease risk.
Myocardial Infarction
Urinary excretion of homocysteine thiolactone and the risk of acute myocardial infarction in coronary artery disease patients: the WENBIT trial.
Neoplasm Metastasis
Methionyl-tRNA Synthetase is a Useful Diagnostic Marker for Lymph Node Metastasis in Non-Small Cell Lung Cancer.
Neoplasms
Determination of three-dimensional structure and residues of the novel tumor suppressor AIMP3/p18 required for the interaction with ATM.
Neoplasms
Dual role of methionyl-tRNA synthetase in the regulation of translation and tumor suppressor activity of aminoacyl-tRNA synthetase-interacting multifunctional protein-3.
Neoplasms
Methionyl-tRNA synthetase overexpression is associated with poor clinical outcomes in non-small cell lung cancer.
Neoplasms
New staining method using methionyl-tRNA synthetase 1 antibody for brushing cytology of bile duct cancer.
Neoplasms
Screening of quinoline, 1,3-benzoxazine, and 1,3-oxazine-based small molecules against isolated methionyl-tRNA synthetase and A549 and HCT116 cancer cells including an in silico binding mode analysis.
Neoplasms
Stabilization of Cyclin-Dependent Kinase 4 by Methionyl-tRNA Synthetase in p16INK4a-Negative Cancer.
Neural Tube Defects
Inhibiting MARSs reduces hyperhomocysteinemia-associated neural tube and congenital heart defects.
Osteosarcoma
Nuclear localization of aminoacyl-tRNA synthetases using single-cell capillary electrophoresis laser-induced fluorescence analysis.
Parasitic Diseases
Screening of quinoline, 1,3-benzoxazine, and 1,3-oxazine-based small molecules against isolated methionyl-tRNA synthetase and A549 and HCT116 cancer cells including an in silico binding mode analysis.
Pulmonary Alveolar Proteinosis
Biallelic Mutations of Methionyl-tRNA Synthetase Cause a Specific Type of Pulmonary Alveolar Proteinosis Prevalent on Réunion Island.
Pulmonary Alveolar Proteinosis
Methionyl-tRNA synthetase novel mutation causes pulmonary alveolar proteinosis.
Pulmonary Alveolar Proteinosis
Mutations in MARS identified in a specific type of pulmonary alveolar proteinosis alter methionyl-tRNA synthetase activity.
Trypanosomiasis, African
Distinct States of Methionyl-tRNA Synthetase Indicate Inhibitor Binding by Conformational Selection.
Trypanosomiasis, African
Urea-Based Inhibitors of Trypanosoma brucei Methionyl-tRNA Synthetase: Selectivity and in Vivo Characterization.
Tuberculosis
Biochemical and phylogenetic analyses of methionyl-tRNA synthetase isolated from a pathogenic microorganism, Mycobacterium tuberculosis.
Tuberculosis
Convergent evolution of two different random RNAs for specific interaction with methionyl-tRNA synthetase.
Tuberculosis
Dual-target inhibitors of mycobacterial aminoacyl-tRNA synthetases among N-benzylidene-N'-thiazol-2-yl-hydrazines.
Tuberculosis
Structural characterization of free-state and product-state Mycobacterium tuberculosis methionyl-tRNA synthetase reveals an induced-fit ligand-recognition mechanism.
Tuberculosis
The crystal structure of the drug target Mycobacterium tuberculosis methionyl-tRNA synthetase in complex with a catalytic intermediate.
Vascular Diseases
Mutations in methylenetetrahydrofolate reductase or cystathionine beta-synthase gene, or a high-methionine diet, increase homocysteine thiolactone levels in humans and mice.
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KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
15.68
(S)-2-aminohex-5-enoic acid
ATP-diphosphate exchange reaction, pH 7.6
2.42
(S)-2-aminohex-5-ynoic acid
ATP-diphosphate exchange reaction, pH 7.6
4.56
L-trans-alpha-crotylglycine
ATP-diphosphate exchange reaction, pH 7.6