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Literature summary extracted from

  • Milicaj, J.; Hassan, B.; Cote, J.; Ramirez-Mondragon, C.; Jaunbocus, N.; Rafalowski, A.; Patel, K.; Castro, C.; Muthyala, R.; Sham, Y.; Taylor, E.
    Discovery of first-in-class nanomolar inhibitors of heptosyltransferase I reveals a new aminoglycoside target and potential alternative mechanism of action (2022), Sci. Rep., 12, 7302 .
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.4.99.23 the enzyme is cloned from the Escherichia coli K12 strain MB1760 (Escherichia coli ATCC 19215) and is expressed in Escherichia coli One Shot BL-21-AI Escherichia coli

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.99.23 amikacin
-
 Escherichia coli
2.4.99.23 kanamycin B competitive inhibition Escherichia coli
2.4.99.23 neomycin competitive inhibition Escherichia coli
2.4.99.23 streptomycin non-competitive inhibition Escherichia coli
2.4.99.23 tobramycin mixed competitive inhibition Escherichia coli

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.4.99.23 0.0025
-
 ADP-L-glycero-beta-D-manno-heptose pH 7.5, 37°C, mutant enzyme R61A Escherichia coli
2.4.99.23 0.0029
-
 ADP-L-glycero-beta-D-manno-heptose pH 7.5, 37°C, wild-type enzyme Escherichia coli
2.4.99.23 0.006
-
 ADP-L-glycero-beta-D-manno-heptose pH 7.5, 37°C, mutant enzyme R60A Escherichia coli
2.4.99.23 0.008
-
 ADP-L-glycero-beta-D-manno-heptose pH 7.5, 37°C, mutant enzyme R64A Escherichia coli
2.4.99.23 0.01
-
 ADP-L-glycero-beta-D-manno-heptose pH 7.5, 37°C, mutant enzyme R63A Escherichia coli
2.4.99.23 0.015
-
 ADP-L-glycero-beta-D-manno-heptose pH 7.5, 37°C, mutant enzyme R120A Escherichia coli

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
2.4.99.23 37000
-
 SDS-PAGE Escherichia coli

Organism

EC Number Organism UniProt Comment Textmining
2.4.99.23 Escherichia coli P24173
-
-
2.4.99.23 Escherichia coli K12 P24173
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.4.99.23
-
 Escherichia coli

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.99.23 ADP-L-glycero-beta-D-manno-heptose + alpha-Kdo-(2->4)-alpha-Kdo-(2->6)-[O-deacylated Escherichia coli Kdo2-lipid A]
-
 Escherichia coli ADP + alpha-Hep-(1->5)-[alpha-Kdo-(2->4)]-alpha-Kdo-(2->6)-[O-deacylated Escherichia coli Kdo2-lipid A]
-
 ?
2.4.99.23 ADP-L-glycero-beta-D-manno-heptose + alpha-Kdo-(2->4)-alpha-Kdo-(2->6)-[O-deacylated Escherichia coli Kdo2-lipid A]
-
 Escherichia coli K12 ADP + alpha-Hep-(1->5)-[alpha-Kdo-(2->4)]-alpha-Kdo-(2->6)-[O-deacylated Escherichia coli Kdo2-lipid A]
-
 ?

Subunits

EC Number Subunits Comment Organism
2.4.99.23 ? x * 37000, SDS-PAGE Escherichia coli

Synonyms

EC Number Synonyms Comment Organism
2.4.99.23 HepI
-
 Escherichia coli
2.4.99.23 heptosyltransferase I
-
 Escherichia coli

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2.4.99.23 0.198
-
 ADP-L-glycero-beta-D-manno-heptose pH 7.5, 37°C, mutant enzyme R60A Escherichia coli
2.4.99.23 0.32
-
 ADP-L-glycero-beta-D-manno-heptose pH 7.5, 37°C, mutant enzyme R120A Escherichia coli
2.4.99.23 0.33
-
 ADP-L-glycero-beta-D-manno-heptose pH 7.5, 37°C, mutant enzyme R64A Escherichia coli
2.4.99.23 0.36
-
 ADP-L-glycero-beta-D-manno-heptose pH 7.5, 37°C, wild-type enzyme Escherichia coli
2.4.99.23 0.36
-
 ADP-L-glycero-beta-D-manno-heptose pH 7.5, 37°C, mutant enzyme R61A Escherichia coli
2.4.99.23 0.41
-
 ADP-L-glycero-beta-D-manno-heptose pH 7.5, 37°C, mutant enzyme R63A Escherichia coli

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.4.99.23 0.000422
-
 tobramycin pH 7.5, 37°C, mutant enzyme R120A Escherichia coli
2.4.99.23 0.000595
-
 streptomycin pH 7.5, 37°C, wild-type enzyme Escherichia coli
2.4.99.23 0.00099
-
 kanamycin B pH 7.5, 37°C, wild-type enzyme Escherichia coli
2.4.99.23 0.001125
-
 tobramycin pH 7.5, 37°C, wild-type enzyme Escherichia coli
2.4.99.23 0.001643
-
 neomycin pH 7.5, 37°C, wild-type enzyme Escherichia coli
2.4.99.23 0.0034
-
 tobramycin pH 7.5, 37°C, mutant enzyme R60A Escherichia coli
2.4.99.23 0.004258
-
 amikacin pH 7.5, 37°C, wild-type enzyme Escherichia coli
2.4.99.23 0.0058
-
 streptomycin pH 7.5, 37°C, mutant enzyme R64A Escherichia coli
2.4.99.23 0.006254
-
 streptomycin pH 7.5, 37°C, mutant enzyme R60A Escherichia coli
2.4.99.23 0.0067
-
 streptomycin pH 7.5, 37°C, mutant enzyme R63A Escherichia coli
2.4.99.23 0.00789
-
 streptomycin pH 7.5, 37°C, mutant enzyme R61A Escherichia coli

General Information

EC Number General Information Comment Organism
2.4.99.23 drug target fighting bacterial infections by inhibition of the enzyme (HepI) by aminoglycosides Escherichia coli
2.4.99.23 physiological function critical role in the biosynthesis of lipopolysaccharides on bacterial cell surfaces Escherichia coli