Positive and negative regulation of IkappaB kinase activity through IKKbeta subunit phosphorylation.

Article Details

Citation

Delhase M, Hayakawa M, Chen Y, Karin M

Positive and negative regulation of IkappaB kinase activity through IKKbeta subunit phosphorylation.

Science. 1999 Apr 9;284(5412):309-13.

PubMed ID
10195894 [ View in PubMed
]
Abstract

IkappaB [inhibitor of nuclear factor kappaB (NF-kappaB)] kinase (IKK) phosphorylates IkappaB inhibitory proteins, causing their degradation and activation of transcription factor NF-kappaB, a master activator of inflammatory responses. IKK is composed of three subunits-IKKalpha and IKKbeta, which are highly similar protein kinases, and IKKgamma, a regulatory subunit. In mammalian cells, phosphorylation of two sites at the activation loop of IKKbeta was essential for activation of IKK by tumor necrosis factor and interleukin-1. Elimination of equivalent sites in IKKalpha, however, did not interfere with IKK activation. Thus, IKKbeta, not IKKalpha, is the target for proinflammatory stimuli. Once activated, IKKbeta autophosphorylated at a carboxyl-terminal serine cluster. Such phosphorylation decreased IKK activity and may prevent prolonged activation of the inflammatory response.

DrugBank Data that Cites this Article

Polypeptides
NameUniProt ID
Inhibitor of nuclear factor kappa-B kinase subunit betaO14920Details
Inhibitor of nuclear factor kappa-B kinase subunit alphaO15111Details