2.7.1.190: aminoglycoside 2''-phosphotransferase
This is an abbreviated version!
For detailed information about aminoglycoside 2''-phosphotransferase, go to the full flat file.
Word Map on EC 2.7.1.190
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2.7.1.190
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aph3\'-iiia
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kanamycin
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enterococci
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aac6\'-ie-aph2\'\'-ia
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faecium
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aminoglycoside-modifying
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phosphotransferases
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aph2\'\'-ic
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amikacin
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gentamicin-resistant
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aac6\'-aph2
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tobramycin
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4,6-disubstituted
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casseliflavus
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aac6'-ie
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ant6\'-ia
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gallinarum
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aminoglycoside-resistance
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lividomycin
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butirosin
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o-phosphorylation
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sisomicin
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durans
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molecular biology
- 2.7.1.190
-
aph3\'-iiia
- kanamycin
-
enterococci
-
aac6\'-ie-aph2\'\'-ia
- faecium
-
aminoglycoside-modifying
-
phosphotransferases
-
aph2\'\'-ic
- amikacin
-
gentamicin-resistant
-
aac6\'-aph2
- tobramycin
-
4,6-disubstituted
- casseliflavus
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aac6'-ie
-
ant6\'-ia
- gallinarum
-
aminoglycoside-resistance
- lividomycin
- butirosin
-
o-phosphorylation
- sisomicin
- durans
- molecular biology
Reaction
Synonyms
AAC(6')-APH(2''), AAC(6')-Ie/APH(2'')-Ia, aac6-aph2, aacA-aphD, AME, aminoglycoside (2'') kinase, aminoglycoside 2''-phosphotransferase IVa, aminoglycoside 2''-phosphotransferase type IIIa, aminoglycoside kinase, aminoglycoside phosphotransferase, aminoglycoside-2''-phosphotransferase, aminoglycoside-2''-phosphotransferase type IVa, aminoglycoside-modification enzyme, APH, APH(2''), APH(2'')-Ia, APH(2'')-Ia aminoglycoside resistance enzyme, APH(2'')-Id, Aph(2'')-If, APH(2'')-IIIa, APH(2'')-IVa, aphD, AphSR2, bifunctional 6'-aminoglycoside acetyltransferase/2"-aminoglycoside phosphotransferase, bifunctional AAC/APH, bifunctional aminoglycoside acetyltransferase(6')-Ie/aminoglycoside phosphotransferase(2'')-Ia, bifunctional aminoglycoside acetyltransferase/phosphotransferase, gentamicin kinase, gentamicin phosphotransferase, gentamicin resistance protein
ECTree
2.7.1.190 aminoglycoside 2''-phosphotransferaseAdvanced search results
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results (Inhibitors
Inhibitors on EC 2.7.1.190 - aminoglycoside 2''-phosphotransferase
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INHIBITOR 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
IMAGE
ZINC13236811
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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
additional information
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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
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additional information
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the ternary complex between APH(2'')-IIIa, GDP and kanamycin can be regarded as an inactive abortive complex, since the gamma-phosphate group which would normally be transferred to the 2''-hydroxyl of the substrate is absent. The cofactor binding in the ternary complex is similar in detail to that in the previously described binary complex
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additional information
inhibitor screening of a chemical library using ultra-high performance liquid chromatography-quadrupole-time-of-flight mass spectrometry, assay method optimization and validation, overview. Poor inhibition by Mer-C-3, Mer-C-8e, and paromomycin
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