Target intelligence / Profile preview

Transforming growth factor-β-activated kinase 1–TAK1-binding protein 1 complex (TAK1-TAB1 complex)

Target
TAK1-TAB1 complex
Molecular classification
Enzyme (Serine/threonine kinase; TAK1 is MAP3K7), Adapter protein (TAB1 is an adapter/regulatory protein), Signalosome (multi-protein signaling complex)
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Overview

The TAK1-TAB1 complex is a central mediator of inflammatory and stress signaling in mammalian cells. TAK1 (MAP3K7) is a serine/threonine kinase activated by cytokines and receptor ligands, leading to activation of NF-κB and MAPK pathways. TAB1 acts as an adapter that binds to TAK1, enhancing its kinase activity and facilitating downstream signaling. The complex is regulated by post-translational modifications, including phosphorylation and ubiquitination, and is essential for mediating cellular responses to proinflammatory stimuli, regulating cell death pathways, and modulating immune and stress responses in health and disease.

Other names
TAK1–TAB1 complexMAP3K7–TAB1 complexTGF-β-activated kinase 1–TAB1 complex
02

Mechanism of action

Kinase inhibition (drugs inhibit TAK1's kinase activity, blocking NF-κB and MAPKs activation); Disruption of protein–protein interaction (e.g., agents interfering with TAK1–TAB1 binding)

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Biological functions

Signal transduction (key mediator of inflammatory signaling)Cell death regulation (regulates apoptosis, necroptosis, and ferroptosis)Immune response (critical in innate immunity and cytokine signaling)Cell proliferation
04

Disease associations

Inflammation (central role in inflammatory signaling)Cancer (implicated in tumorigenesis)Cardiovascular disease (linked through inflammatory pathways)Infection (modulates immune response to pathogens)
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Safety considerations

Broad inhibition may suppress essential inflammatory and immune responses, increasing risk of infection or impairing tissue repairPotential for off-target toxicity due to close homology with other MAPKKKs
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Interacting drugs

5Z-7-oxozeaenol

1 more in the full profile.

07

Biomarkers

Phosphorylation status of TAK1, TAB1, or downstream molecules such as IKKβ and JNKNF-κB activation profile

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