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IκB kinase 1 (IKK1), also known as IKK-α or CHUK, is a catalytic subunit of the IκB kinase complex, which is a serine/threonine protein kinase central to regulating the NF-κB signaling pathway[1][3][5]. The IKK complex consists of two catalytic subunits—IKK1 (IKK-α) and IKK2 (IKK-β)—alongside a regulatory subunit (NEMO/IKK-γ)[1][3][4]. IKK1 is required for phosphorylation of IκB proteins, leading to their degradation and subsequent release of NF-κB transcription factors to the nucleus, orchestrating gene expression related to immunity, inflammation, cell proliferation, and survival[1][2][3][4]. IKK1 is implicated in diseases with dysregulated NF-κB signaling, such as cancer and chronic inflammation, making it a therapeutic target for modulators that inhibit or alter its kinase function[2]. Safety challenges may arise due to the central role of NF-κB in immune defense and tissue homeostasis.
Inhibition of IκB kinase activity, blocking NF-κB activation; prevention of IκB phosphorylation and degradation; modulation of inflammatory and immune gene transcription.
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