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Literature summary for 2.4.99.23 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
Search for more literature for 2.4.99.23

Cloned(Commentary)

Cloned (Comment) Organism
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

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

KM Value [mM]

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

Molecular Weight [Da]

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

Organism

Organism UniProt Comment Textmining
Escherichia coli P24173
-
-
Escherichia coli K12 P24173
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Escherichia coli

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
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]
-
 ?
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

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

Synonyms

Synonyms Comment Organism
HepI
-
 Escherichia coli
heptosyltransferase I
-
 Escherichia coli

Turnover Number [1/s]

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

Ki Value [mM]

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

General Information

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