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Literature summary extracted from

  • Garzan, A.; Willby, M.; Green, K.; Gajadeera, C.; Hou, C.; Tsodikov, O.; Posey, J.; Garneau-Tsodikova, S.
    Sulfonamide-based inhibitors of aminoglycoside acetyltransferase Eis abolish resistance to kanamycin in Mycobacterium tuberculosis (2016), J. Med. Chem., 59, 10619-10628 .
    View publication on PubMedView publication on EuropePMC

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
2.3.1.81 in complex with inhibitor N-(3-methoxyphenyl)-N-methyl-2,3-dioxo-1,2,3,4-tetrahydro-6-quinoxalinesulfonamide. Inhibitor binds Eis in the AG-binding pocket held by a conformationally malleable region of Eis (residues 28-37) bearing key hydrophobic residues Mycobacterium tuberculosis

Protein Variants

EC Number Protein Variants Comment Organism
2.3.1.81 C204A active site mutant Mycobacterium tuberculosis

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.81 N-(2-naphthyl)-N-methyl-2,3-dioxo-1,2,3,4-tetrahydro-6-quinoxalinesulfonamide lacks anti-Mycobacterium tuberculosis activity in the absence of kanamycin in either tested strain Mycobacterium tuberculosis
2.3.1.81 N-(3-methoxyphenyl)-N-methyl-2,3-dioxo-1,2,3,4-tetrahydro-6-quinoxalinesulfonamide inhibitor completely overcomes kanamycin resistance in Mycobacterium tuberculosis K204, lacks anti-Mycobacterium tuberculosis activity in the absence of kanamycin in either tested strain Mycobacterium tuberculosis

Organism

EC Number Organism UniProt Comment Textmining
2.3.1.81 Mycobacterium tuberculosis P9WFK7
-
-
2.3.1.81 Mycobacterium tuberculosis H37Rv P9WFK7
-
-

Synonyms

EC Number Synonyms Comment Organism
2.3.1.81 Eis
-
 Mycobacterium tuberculosis

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.1.81 0.00000024
-
 pH 8.0, 25°C Mycobacterium tuberculosis N-(2-naphthyl)-N-methyl-2,3-dioxo-1,2,3,4-tetrahydro-6-quinoxalinesulfonamide
2.3.1.81 0.058
-
 pH 8.0, 25°C Mycobacterium tuberculosis N-(3-methoxyphenyl)-N-methyl-2,3-dioxo-1,2,3,4-tetrahydro-6-quinoxalinesulfonamide

General Information

EC Number General Information Comment Organism
2.3.1.81 physiological function acetyltransferase Eis upregulation causes resistance to kanamycin A in Mycobacterium tuberculosis Mycobacterium tuberculosis