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Literature summary for 6.1.1.5 extracted from

  • Cestari, I.; Stuart, K.
    Inhibition of isoleucyl-tRNA synthetase as a potential treatment for human African Trypanosomiasis (2013), J. Biol. Chem., 288, 14256-14263.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
medicine inhibition of the enzyme constitutes a potential treatment for African sleeping sickness Trypanosoma brucei

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli Trypanosoma brucei

Protein Variants

Protein Variants Comment Organism
D539A/W541A catalytically inactive Trypanosoma brucei

Inhibitors

Inhibitors Comment Organism Structure
2-fluoro-9-(5-O-phosphono-alpha-L-arabinofuranosyl)-9H-purin-6-amine
-
Trypanosoma brucei
2-fluoroadenosine
-
Trypanosoma brucei
3'-amino-3'-deoxy-N,N-dimethyladenosine
-
Trypanosoma brucei
4,6-dideoxy-4-[[N-(14-methylpentadecanoyl)glycyl]amino]-N-9H-purin-6-ylhexopyranosylamine
-
Trypanosoma brucei
9-(3-deoxy-alpha-L-threo-pentofuranosyl)-9H-purin-6-amine
-
Trypanosoma brucei
9-(5-O-acetyl-alpha-L-arabinofuranosyl)-9H-purin-6-amine
-
Trypanosoma brucei
9-(alpha-D-arabinofuranosyl)-9H-purin-6-amine competitive inhibition Trypanosoma brucei
9-(alpha-L-arabinofuranosyl)-9H-purin-6-amine
-
Trypanosoma brucei
9-(alpha-L-arabinofuranosyl)-N-(3-methylbut-2-en-1-yl)-9H-purin-6-amine
-
Trypanosoma brucei
9-(beta-D-arabinofuranosyl)-9H-purin-6-amine
-
Trypanosoma brucei
9-[5-deoxy-5-[(methylsulfonyl)amino]-alpha-L-arabinofuranosyl]-9H-purin-6-amine
-
Trypanosoma brucei
9-[5-O-(dimethoxyphosphoryl)-alpha-L-arabinofuranosyl]-9H-purin-6-amine
-
Trypanosoma brucei
9-[5-O-[tert-butyl(dimethyl)silyl]-alpha-L-arabinofuranosyl]-9H-purin-6-amine
-
Trypanosoma brucei
N8,N8-dimethyl-9-pentofuranosyl-9H-purine-6,8-diamine
-
Trypanosoma brucei
NSC70422
-
Trypanosoma brucei

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.00000004
-
L-isoleucine pH and temperature not specified in the publication Trypanosoma brucei

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
110000
-
x * 110000, SDS-PAGE Trypanosoma brucei

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + L-isoleucine + tRNAIle Trypanosoma brucei
-
AMP + diphosphate + L-isoleucyl-tRNAIle
-
?

Organism

Organism UniProt Comment Textmining
Trypanosoma brucei
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + L-isoleucine + tRNAIle
-
Trypanosoma brucei AMP + diphosphate + L-isoleucyl-tRNAIle
-
?

Subunits

Subunits Comment Organism
? x * 110000, SDS-PAGE Trypanosoma brucei

Synonyms

Synonyms Comment Organism
IleRS
-
Trypanosoma brucei
Isoleucyl-tRNA synthetase
-
Trypanosoma brucei

Cofactor

Cofactor Comment Organism Structure
ATP
-
Trypanosoma brucei

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000027
-
9-(alpha-D-arabinofuranosyl)-9H-purin-6-amine pH and temperature not specified in the publication Trypanosoma brucei
0.0000027
-
NSC70422 pH and temperature not specified in the publication Trypanosoma brucei

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000141
-
pH and temperature not specified in the publication Trypanosoma brucei 9-(alpha-D-arabinofuranosyl)-9H-purin-6-amine
0.0000141
-
pH and temperature not specified in the publication Trypanosoma brucei NSC70422