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Literature summary extracted from

  • Devi, P.; Sridevi, J.; Kakan, S.; Saxena, S.; Jeankumar, V.; Soni, V.; Anantaraju, H.; Yogeeswari, P.; Sriram, D.
    Discovery of novel lysine ?-aminotransferase inhibitors: An intriguing potential target for latent tuberculosis. (2015), Tuberculosis, 95, 786-794.
    View publication on PubMed

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
2.6.1.36 molecular docking of inhibitors 4-methoxy-2-(pyridin-4-yl)-2,3-dihydro-1,3-thiazole-5-carboxylic acid, 2-phenyl-4-(prop-2-yn-1-yloxy)-2,3-dihydro-1,3-thiazole-5-carboxylic acid, 4-ethoxy-2-phenyl-2,3-dihydro-1,3-thiazole-5-carboxamide. Ligands are found in the vicinity of the Arg422, Gln274, Lys300, Arg170, Phe167, Glu243 amino acid residues. Compounds can make favourable interactions with important amino acid residues such as Arg170, Arg440, and Lys300 Mycobacterium tuberculosis

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.6.1.36 2-phenyl-4-(prop-2-yn-1-yloxy)-2,3-dihydro-1,3-thiazole-5-carboxylic acid
-
 Mycobacterium tuberculosis
2.6.1.36 4-ethoxy-2-phenyl-2,3-dihydro-1,3-thiazole-5-carboxamide protein is stabilzed in presence of the inhibitor Mycobacterium tuberculosis
2.6.1.36 4-methoxy-2-(pyridin-4-yl)-2,3-dihydro-1,3-thiazole-5-carboxylic acid at 0.05 mM, 24.87% cytotoxicity in a HEK-293 cell line Mycobacterium tuberculosis

Organism

EC Number Organism UniProt Comment Textmining
2.6.1.36 Mycobacterium tuberculosis P9WQ77
-
-
2.6.1.36 Mycobacterium tuberculosis H37Rv P9WQ77
-
-

Temperature Stability [°C]

EC Number Temperature Stability Minimum [°C] Temperature Stability Maximum [°C] Comment Organism
2.6.1.36 50.6
-
 melting temperature Mycobacterium tuberculosis
2.6.1.36 52.1
-
 melting temperature in presence of inhibitor 4-ethoxy-2-phenyl-2,3-dihydro-1,3-thiazole-5-carboxamide Mycobacterium tuberculosis

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.6.1.36 0.0012
-
 pH 7.2, 37°C Mycobacterium tuberculosis 4-methoxy-2-(pyridin-4-yl)-2,3-dihydro-1,3-thiazole-5-carboxylic acid
2.6.1.36 0.0017
-
 pH 7.2, 37°C Mycobacterium tuberculosis 4-ethoxy-2-phenyl-2,3-dihydro-1,3-thiazole-5-carboxamide
2.6.1.36 0.0018
-
 pH 7.2, 37°C Mycobacterium tuberculosis 2-phenyl-4-(prop-2-yn-1-yloxy)-2,3-dihydro-1,3-thiazole-5-carboxylic acid