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Literature summary for 3.6.4.10 extracted from

  • Chang, L.; Bertelsen, E.B.; Wisen, S.; Larsen, E.M.; Zuiderweg, E.R.; Gestwicki, J.E.
    High-throughput screen for small molecules that modulate the ATPase activity of the molecular chaperone DnaK (2008), Anal. Biochem., 372, 167-176.
    View publication on PubMed
Search for more literature for 3.6.4.10

Activating Compound

Activating Compound Comment Organism Structure
geranylgeraniol presence of peptide NRLLLTG eliminates stimulatory effect Escherichia coli
NRLLLTG peptide binding to the substrate-binding site. Stimulates ATPase activity, eliminates stimulatory effect of geranylgeraniol Escherichia coli

Application

Application Comment Organism
analysis high-throughput screening method in 96-well plates for ATPase activity of DnaK. Screening of potential inhibitors Escherichia coli

Inhibitors

Inhibitors Comment Organism Structure
5-[1-[(6-[5-[(benzyloxy)carbonyl]-4-biphenyl-4-yl-6-methyl-2-oxo-3,4-dihydropyrimidin-1(2H)-yl]hexanoyl)(hexyl)amino]-2-[(1E)-butylideneamino]-2-oxoethyl]-2-(carboxymethoxy)benzoic acid
-
 Escherichia coli
6-[5-[(benzyloxy)carbonyl]-4-(4-cyclohexylphenyl)-6-methyl-2-oxo-3,4-dihydropyrimidin-1(2H)-yl]hexanoic acid IC50 value about 0.12-0.2 mM Escherichia coli
6-[5-[(benzyloxy)carbonyl]-4-biphenyl-4-yl-6-methyl-2-oxo-3,4-dihydropyrimidin-1(2H)-yl]hexanoic acid IC50 value about 0.12-0.2 mM Escherichia coli
methyl 4-(naphthalen-2-yl)-2-oxo-6-(phenoxymethyl)-1,2,3,4-tetrahydropyrimidine-5-carboxylate IC50 value about 0.12 -0.2 mM Escherichia coli

Organism

Organism UniProt Comment Textmining
Escherichia coli
-
 isoform DnaK
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
 high-throughput screening method in 96-well plates for ATPase activity of DnaK. Screening of potential inhibitors Escherichia coli

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O
-
 Escherichia coli ADP + phosphate
-
 ?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.002
-
 ATP pH 7.4, 37°C Escherichia coli
0.0075
-
 ATP pH 7.4, 37°C, presence of 0.0009 mM GrpE protein Escherichia coli
0.0083
-
 ATP pH 7.4, 37°C, presence of 0.00097 mM DnaJ protein Escherichia coli
0.0125
-
 ATP pH 7.4, 37°C, presence of 0.00048 mM DnaJ and 0.0009 mM GrpE proteins Escherichia coli
0.0157
-
 ATP pH 7.4, 37°C, presence of 0.00097 mM DnaJ and 0.00091 mM GrpE proteins Escherichia coli
0.167
-
 ATP pH 7.4, 37°C, presence of 0.00097 mM DnaJ and 0.0018 mM GrpE proteins Escherichia coli

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.065
-
 pH 7.4, 37°C, presence of peptide NRLLLTG Escherichia coli 5-[1-[(6-[5-[(benzyloxy)carbonyl]-4-biphenyl-4-yl-6-methyl-2-oxo-3,4-dihydropyrimidin-1(2H)-yl]hexanoyl)(hexyl)amino]-2-[(1E)-butylideneamino]-2-oxoethyl]-2-(carboxymethoxy)benzoic acid
0.13
-
 pH 7.4, 37°C Escherichia coli 5-[1-[(6-[5-[(benzyloxy)carbonyl]-4-biphenyl-4-yl-6-methyl-2-oxo-3,4-dihydropyrimidin-1(2H)-yl]hexanoyl)(hexyl)amino]-2-[(1E)-butylideneamino]-2-oxoethyl]-2-(carboxymethoxy)benzoic acid