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Literature summary for 6.1.1.21 extracted from

  • Koh, C.Y.; Siddaramaiah, L.K.; Ranade, R.M.; Nguyen, J.; Jian, T.; Zhang, Z.; Gillespie, J.R.; Buckner, F.S.; Verlinde, C.L.; Fan, E.; Hol, W.G.
    A binding hotspot in Trypanosoma cruzi histidyl-tRNA synthetase revealed by fragment-based crystallographic cocktail screens (2015), Acta Crystallogr. Sect. D, 71, 1684-1698 .
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli BL21(DE3) cells Trypanosoma cruzi

Crystallization (Commentary)

Crystallization (Comment) Organism
hanging drop vapor diffusion method, using 0.2 M lithium sulfate or ammonium sulfate, 26% (w/v) PEG 3350, 0.1 M bis-Tris pH 5.5, 1 mM TCEP Trypanosoma cruzi

Inhibitors

Inhibitors Comment Organism Structure
(6-bromopyridin-2-yl)methanol
-
Trypanosoma cruzi
2-aminoquinolin-8-ol
-
Trypanosoma cruzi
2-bromo-N-(quinolin-3-yl)acetamide
-
Trypanosoma cruzi
N-(5-hydroxynaphthalen-2-yl)prop-2-enamide
-
Trypanosoma cruzi
N-(quinolin-3-yl)acetamide
-
Trypanosoma cruzi
N-(quinolin-3-yl)prop-2-enamide
-
Trypanosoma cruzi
quinolin-3-amine
-
Trypanosoma cruzi

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol
-
Trypanosoma cruzi 5829
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + L-histidine + tRNAHis Trypanosoma cruzi
-
AMP + diphosphate + L-histidyl-tRNAHis
-
?

Organism

Organism UniProt Comment Textmining
Trypanosoma cruzi Q4DA54
-
-

Purification (Commentary)

Purification (Comment) Organism
Ni-NTA column chromatography, Mono S cation-exchange column chromatography, and Superdex 200 gel filtration Trypanosoma cruzi

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + L-histidine + tRNAHis
-
Trypanosoma cruzi AMP + diphosphate + L-histidyl-tRNAHis
-
?

Synonyms

Synonyms Comment Organism
HisRS
-
Trypanosoma cruzi
Histidyl-tRNA synthetase
-
Trypanosoma cruzi

Cofactor

Cofactor Comment Organism Structure
ATP
-
Trypanosoma cruzi

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.8
-
at pH 7.5 and 25°C Trypanosoma cruzi 2-bromo-N-(quinolin-3-yl)acetamide
0.85
-
at pH 7.5 and 25°C Trypanosoma cruzi N-(quinolin-3-yl)prop-2-enamide
1.65
-
at pH 7.5 and 25°C Trypanosoma cruzi N-(5-hydroxynaphthalen-2-yl)prop-2-enamide
2
-
IC50 above 2.0 mM, at pH 7.5 and 25°C Trypanosoma cruzi 2-aminoquinolin-8-ol
2
-
IC50 above 2.0 mM, at pH 7.5 and 25°C Trypanosoma cruzi (6-bromopyridin-2-yl)methanol
2
-
IC50 above 2.0 mM, at pH 7.5 and 25°C Trypanosoma cruzi N-(quinolin-3-yl)acetamide
2
-
IC50 above 2.0 mM, at pH 7.5 and 25°C Trypanosoma cruzi quinolin-3-amine