The gatekeeper residue controls autoactivation of ERK2 via a pathway of intramolecular connectivity.

@article{Emrick2006TheGR,
  title={The gatekeeper residue controls autoactivation of ERK2 via a pathway of intramolecular connectivity.},
  author={Michelle A Emrick and Thomas C. Lee and Paul J Starkey and Marc C. Mumby and Katheryn A. Resing and Natalie G Ahn},
  journal={Proceedings of the National Academy of Sciences of the United States of America},
  year={2006},
  volume={103 48},
  pages={18101-6}
}
Studies of protein kinases have identified a "gatekeeper" residue, which confers selectivity for binding nucleotides and small-molecule inhibitors. We report that, in the MAP kinase ERK2, mutations at the gatekeeper residue unexpectedly lead to autoactivation due to enhanced autophosphorylation of regulatory Tyr and Thr sites within the activation lip that control kinase activity. This occurs through an intramolecular mechanism, indicating that the gatekeeper residue indirectly constrains… CONTINUE READING

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