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Literature summary for 2.7.11.10 extracted from

  • Asamitsu, K.; Yamaguchi, T.; Nakata, K.; Hibi, Y.; Victoriano, A.F.; Imai, K.; Onozaki, K.; Kitade, Y.; Okamoto, T.
    Inhibition of human immunodeficiency virus type 1 replication by blocking IkappaB kinase with noraristeromycin (2008), J. Biochem., 144, 581-589.
    View publication on PubMed

Application

Application Comment Organism
medicine IKK is thought to be a focal target of drug development Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
Flag-IKKalpha and Flag-IKKbeta vectors for transfection of HEK293 cells are used Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
noraristeromycin NAM Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
cytoplasm
-
Homo sapiens 5737
-

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]
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HEK-293 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + NF-kappaB p65 subunit IKKalpha and IKKbeta phosphorylate NF-kappaB p65 subunit at Ser536 Homo sapiens ADP + phosphorylated NF-kappaB p65 subunit
-
?
ATP + [IkappaB protein]
-
Homo sapiens ADP + [IkappaB phosphoprotein]
-
?

Subunits

Subunits Comment Organism
oligomer IKK is a large molecular weight complex consisting of at least two catalytic subunits, IKKalpha, IKKbeta, and the associated regulatory subunit IKKgamma, NEMO Homo sapiens

Synonyms

Synonyms Comment Organism
IkappaB kinase
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00037
-
IKKalpha Homo sapiens noraristeromycin
0.00064
-
inhibited endogenous IKK activity following TNF-alpha stimulation Homo sapiens noraristeromycin