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  • RESEARCH HIGHLIGHT

A peptide-guided strategy for kinase activation

By
  1. M. Teresa Villanueva

PAK1 is a serine/threonine kinase that regulates cardiac homeostasis and is maintained in an inactive state through an autoinhibitory interaction between its regulatory and kinase domains. Activation occurs when this interaction is disrupted by small GTPases such as Cdc42 or Rac1, providing a discrete regulatory interface that can be targeted allosterically. A previously described bioactive PAK1-activating peptide (PAP), derived from the autoinhibitory region, offered a starting point to map this interface.

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doi: https://doi.org/10.1038/d41573-026-00080-y

References

  1. He, Y. et al. Rational discovery of therapeutic PAK1 allosteric activators. Cell https://doi.org/10.1016/j.cell.2026.03.008 (2026)

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