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Literature summary 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

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

Cloned(Commentary)

EC Number Cloned (Comment) Organism
6.1.1.5 expressed in Escherichia coli Trypanosoma brucei

Protein Variants

EC Number Protein Variants Comment Organism
6.1.1.5 D539A/W541A catalytically inactive Trypanosoma brucei

Inhibitors

EC Number Inhibitors Comment Organism Structure
6.1.1.5 2-fluoro-9-(5-O-phosphono-alpha-L-arabinofuranosyl)-9H-purin-6-amine
-
 Trypanosoma brucei
6.1.1.5 2-fluoroadenosine
-
 Trypanosoma brucei
6.1.1.5 3'-amino-3'-deoxy-N,N-dimethyladenosine
-
 Trypanosoma brucei
6.1.1.5 4,6-dideoxy-4-[[N-(14-methylpentadecanoyl)glycyl]amino]-N-9H-purin-6-ylhexopyranosylamine
-
 Trypanosoma brucei
6.1.1.5 9-(3-deoxy-alpha-L-threo-pentofuranosyl)-9H-purin-6-amine
-
 Trypanosoma brucei
6.1.1.5 9-(5-O-acetyl-alpha-L-arabinofuranosyl)-9H-purin-6-amine
-
 Trypanosoma brucei
6.1.1.5 9-(alpha-D-arabinofuranosyl)-9H-purin-6-amine competitive inhibition Trypanosoma brucei
6.1.1.5 9-(alpha-L-arabinofuranosyl)-9H-purin-6-amine
-
 Trypanosoma brucei
6.1.1.5 9-(alpha-L-arabinofuranosyl)-N-(3-methylbut-2-en-1-yl)-9H-purin-6-amine
-
 Trypanosoma brucei
6.1.1.5 9-(beta-D-arabinofuranosyl)-9H-purin-6-amine
-
 Trypanosoma brucei
6.1.1.5 9-[5-deoxy-5-[(methylsulfonyl)amino]-alpha-L-arabinofuranosyl]-9H-purin-6-amine
-
 Trypanosoma brucei
6.1.1.5 9-[5-O-(dimethoxyphosphoryl)-alpha-L-arabinofuranosyl]-9H-purin-6-amine
-
 Trypanosoma brucei
6.1.1.5 9-[5-O-[tert-butyl(dimethyl)silyl]-alpha-L-arabinofuranosyl]-9H-purin-6-amine
-
 Trypanosoma brucei
6.1.1.5 N8,N8-dimethyl-9-pentofuranosyl-9H-purine-6,8-diamine
-
 Trypanosoma brucei
6.1.1.5 NSC70422
-
 Trypanosoma brucei

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
6.1.1.5 0.00000004
-
 L-isoleucine pH and temperature not specified in the publication Trypanosoma brucei

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
6.1.1.5 110000
-
 x * 110000, SDS-PAGE Trypanosoma brucei

Natural Substrates/ Products (Substrates)

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

Organism

EC Number Organism UniProt Comment Textmining
6.1.1.5 Trypanosoma brucei
-
-
-

Substrates and Products (Substrate)

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

Subunits

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

Synonyms

EC Number Synonyms Comment Organism
6.1.1.5 IleRS
-
 Trypanosoma brucei
6.1.1.5 Isoleucyl-tRNA synthetase
-
 Trypanosoma brucei

Cofactor

EC Number Cofactor Comment Organism Structure
6.1.1.5 ATP
-
 Trypanosoma brucei

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
6.1.1.5 0.0000027
-
 9-(alpha-D-arabinofuranosyl)-9H-purin-6-amine pH and temperature not specified in the publication Trypanosoma brucei
6.1.1.5 0.0000027
-
 NSC70422 pH and temperature not specified in the publication Trypanosoma brucei

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
6.1.1.5 0.0000141
-
 pH and temperature not specified in the publication Trypanosoma brucei 9-(alpha-D-arabinofuranosyl)-9H-purin-6-amine
6.1.1.5 0.0000141
-
 pH and temperature not specified in the publication Trypanosoma brucei NSC70422