MAPK kinase kinases (MKKKs) as a target class for small-molecule inhibition to modulate signaling networks and gene expression.

@article{Johnson2005MAPKKK,
  title={MAPK kinase kinases (MKKKs) as a target class for small-molecule inhibition to modulate signaling networks and gene expression.},
  author={Gary Leon Johnson and Henrik G. Dohlman and Lee M Graves},
  journal={Current opinion in chemical biology},
  year={2005},
  volume={9 3},
  pages={325-31}
}
MAPKs are members of a three-kinase phosphorelay system composed of the MAPK, MAPK kinase (MKK) and MAPK kinase kinase (MKKK). MKKKs phosphorylate and activate MKKs, which in turn phosphorylate and activate MAPKs. Scaffolding proteins organize MKK-MAPK complexes for activation by specific MKKKs and do so in specific locations in the cell. It is the MKKK associated with the scaffolded complex that provides selectivity for activation by upstream stimuli including GTPases, additional kinases and… CONTINUE READING

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