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Literature summary extracted from

  • Dai, R.; Wilson, D.J.; Geders, T.W.; Aldrich, C.C.; Finzel, B.C.
    Inhibition of Mycobacterium tuberculosis transaminase BioA by aryl hydrazines and hydrazides (2014), ChemBioChem, 15, 575-586.
    View publication on PubMedView publication on EuropePMC

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
2.6.1.62 in complex with substrate 7-oxo-8-aminopelargonic acid and in complex with inhibitors 1-(1,3-benzothiazol-2-yl)methanamine and 2-hydrazinyl-1,3-benzothiazole. The side chains of Tyr25, Trp65, Arg400, and Tyr407 are shown to be quite flexible. Small molecule binding induces unexpected conformational remodeling in the substrate binding site Mycobacterium tuberculosis

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.6.1.62 1-(1,3-benzothiazol-2-yl)methanamine
-
 Mycobacterium tuberculosis
2.6.1.62 2-hydrazinyl-1,3-benzothiazole reversible covalent inhibitor Mycobacterium tuberculosis

Organism

EC Number Organism UniProt Comment Textmining
2.6.1.62 Mycobacterium tuberculosis P9WQ81
-
-
2.6.1.62 Mycobacterium tuberculosis H37Rv P9WQ81
-
-

Synonyms

EC Number Synonyms Comment Organism
2.6.1.62 bioA
-
 Mycobacterium tuberculosis

Temperature Stability [°C]

EC Number Temperature Stability Minimum [°C] Temperature Stability Maximum [°C] Comment Organism
2.6.1.62 67
-
 melting temperature, in complex with inhibitor 2-hydrazinyl-1,3-benzothiazole Mycobacterium tuberculosis
2.6.1.62 78
-
 melting temperature, in complex with inhibitor 1-(1,3-benzothiazol-2-yl)methanamine Mycobacterium tuberculosis

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.6.1.62 0.01
-
 2-hydrazinyl-1,3-benzothiazole pH 8.6, 25°C Mycobacterium tuberculosis