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Literature summary for 2.7.11.10 extracted from

  • Tegeder, I.; Niederberger, E.; Schmidt, R.; Kunz, S.; Guehring, H.; Ritzeler, O.; Michaelis, M.; Geisslinger, G.
    Specific inhibition of IkB kinase reduces hyperalgesia in inflammatory and neuropathic pain models in rats (2004), J. Neurosci., 24, 1637-1645.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
S1627 specific for the IKK complex, inhibits purified IKK in vitro with IC50 of 0.02 mM, inhibits IKK and NFkappaB nuclear translocation in vivo in umbilical vein endothelial cells and in rats, overview Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol
-
Homo sapiens 5829
-
nucleus
-
Homo sapiens 5634
-

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + [IkappaB protein] Homo sapiens
-
ADP + [IkappaB phosphoprotein]
-
?
additional information Homo sapiens enzyme is responsible for NFkappaB activation, specific inhibition of IkB kinase reduces hyperalgesia in inflammatory and neuropathic pain models in male Sprague-Dawley rats ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
native IkappaBalpha kinase from HeLa S3 cells by ammonium sulfate fractionation, ultrafiltration, and gel filtration Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
endothelial cell from umbilical vein Homo sapiens
-
HeLa-S3 cell
-
Homo sapiens
-
umbilical vein
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + [IkappaB protein]
-
Homo sapiens ADP + [IkappaB phosphoprotein]
-
?
ATP + [IkappaB protein] the enzyme is also active with a peptide derived from IkappaB protein spanning Ser32 and Ser36 which are phosphorylated Homo sapiens ADP + [IkappaB phosphoprotein]
-
?
additional information enzyme is responsible for NFkappaB activation, specific inhibition of IkB kinase reduces hyperalgesia in inflammatory and neuropathic pain models in male Sprague-Dawley rats Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
IKK
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.02
-
specific for the IKK complex, inhibits purified IKK in vitro with IC50 of 0.02 mM, inhibits IKK and NFkappaB nuclear translocation in vivo in umbilical vein endothelial cells and in rats, overview Homo sapiens S1627