Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.7.1.190 extracted from

  • Leban, N.; Kaplan, E.; Chaloin, L.; Godreuil, S.; Lionne, C.
    Kinetic characterization and molecular docking of novel allosteric inhibitors of aminoglycoside phosphotransferases (2017), Biochim. Biophys. Acta, 1861, 3464-3473 .
    View publication on PubMed
Search for more literature for 2.7.1.190

Cloned(Commentary)

Cloned (Comment) Organism
recombinant expression of wild-type and mutant enzymes in Escherichia coli strain BL21(DE3) Enterococcus casseliflavus

Inhibitors

Inhibitors Comment Organism Structure
kanamycin A
-
 Enterococcus casseliflavus
additional information identification os specific inhibitors of APHs that can restore bacterial susceptibility to aminoglycosides, screening of the Zinc database for search for allosteric inhibitors that bind to small cavities of the protein and block the enzyme function by perturbing its dynamics, docking study usig the crystal structure of the enzyme (PDB ID 3SG8) with removed aminoglycoside substrate, overview. The two interactions with side chain of Arg211 and backbones of Leu209 and Gly210 are shown to play an essential role in the inhibition of APH. No inhibition by ZINC6751595 and ZINC8981627 Enterococcus casseliflavus
ZINC05277506
-
 Enterococcus casseliflavus
ZINC08981682 10% inhibition at 0.5 mM Enterococcus casseliflavus
ZINC1143187 45% inhibition at 0.5 mM Enterococcus casseliflavus
ZINC12636347 24% inhibition at 0.5 mM Enterococcus casseliflavus
ZINC13001089
-
 Enterococcus casseliflavus
ZINC13001091 9% inhibition at 0.5 mM Enterococcus casseliflavus
ZINC13236811 63% inhibition at 0.5 mM of APH(2'')-IVa, ZINC13236811 is a non-competitive inhibitor of APH(2'')-IVa towards both ATP and ZINC8790387 Enterococcus casseliflavus
ZINC13572054 68% inhibition at 0.5 mM Enterococcus casseliflavus
ZINC14746000 12% inhibition at 0.5 mM Enterococcus casseliflavus
ZINC1792615 27% inhibition at 0.5 mM Enterococcus casseliflavus
ZINC20737652 14% inhibition at 0.5 mM Enterococcus casseliflavus
ZINC20785546 26% inhibition at 0.5 mM Enterococcus casseliflavus
ZINC22357542 14% inhibition at 0.5 mM Enterococcus casseliflavus
ZINC22406103 19% inhibition at 0.5 mM Enterococcus casseliflavus
ZINC36046879
-
 Enterococcus casseliflavus
ZINC36589946 12% inhibition at 0.5 mM Enterococcus casseliflavus
ZINC40455179 17% inhibition at 0.5 mM Enterococcus casseliflavus
ZINC52627502
-
 Enterococcus casseliflavus
ZINC8790387
-
 Enterococcus casseliflavus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
 additional information steady-state kinetics Enterococcus casseliflavus

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Enterococcus casseliflavus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + kanamycin Enterococcus casseliflavus
-
 ADP + kanamycin 2''-phosphate
-
 ?
ATP + tobramycin Enterococcus casseliflavus
-
 ADP + tobramycin 2''-phosphate
-
 ?

Organism

Organism UniProt Comment Textmining
Enterococcus casseliflavus
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + kanamycin
-
 Enterococcus casseliflavus ADP + kanamycin 2''-phosphate
-
 ?
ATP + tobramycin
-
 Enterococcus casseliflavus ADP + tobramycin 2''-phosphate
-
 ?
additional information enzyme assay with coupling the release of ADP to a pyruvate kinase/lactate dehydrogenase reaction Enterococcus casseliflavus ?
-
-

Synonyms

Synonyms Comment Organism
aminoglycoside phosphotransferase
-
 Enterococcus casseliflavus
APH
-
 Enterococcus casseliflavus
APH(2'')-IVa
-
 Enterococcus casseliflavus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
 assay at Enterococcus casseliflavus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
 assay at Enterococcus casseliflavus

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Enterococcus casseliflavus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.074
-
 ZINC13236811 pH 7.5, 25°C, recombinant enzyme, versus kanamycin Enterococcus casseliflavus
0.085
-
 ZINC13236811 pH 7.5, 25°C, recombinant enzyme, versus ATP Enterococcus casseliflavus