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Literature summary for 2.3.1.81 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
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Crystallization (Commentary)

Crystallization (Comment) Organism
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

Protein Variants Comment Organism
C204A active site mutant Mycobacterium tuberculosis

Inhibitors

Inhibitors Comment Organism Structure
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
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

Organism UniProt Comment Textmining
Mycobacterium tuberculosis P9WFK7
-
-
Mycobacterium tuberculosis H37Rv P9WFK7
-
-

Synonyms

Synonyms Comment Organism
Eis
-
 Mycobacterium tuberculosis

IC50 Value

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

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