IkB Kinase Inhibitors Small Molecules and Peptides

IκB Kinase (IKK) is an enzyme complex that forms part of the NF-κB signaling pathway. The complex is comprised of three subunits (IKKα (IKK1), IKKβ (IKK2) and IKKγ (NEMO)), the α- and β-subunits are catalytically active whereas the γ-subunit serves a regulatory function.

Activation of NF-κB occurs via degradation of IκB, a process that is initiated by its phosphorylation by IκB kinase (IKK). Phosphorylated IκB becomes dissociated from NF-κB, unmasking the nuclear localization signal (NLS). Phosphorylation also results in IκB ubiquitination and targeting to the proteasome. NF-κB can now enter the nucleus and regulate gene expression.