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Generation of membrane-permeable cyclic peptides inhibiting protein-protein interaction - PubMed

4 hours ago
  • #protein-protein interaction inhibitors
  • #cyclic peptides
  • #cell permeability
  • Small cyclic peptides are promising for targeting difficult protein-protein interactions (PPIs) due to their ability to bind targets and cross cell membranes.
  • The research demonstrates that screening diverse cyclic peptide libraries can identify inhibitors of PPIs, exemplified by discovering an inhibitor for Keap1-Nrf2.
  • Optimization through design-build-test cycles yields membrane-permeable compounds active in live cells, enabling discovery of cell-permeable PPI inhibitors from scratch.
  • Large, structurally diverse cyclic peptide libraries provide a pathway to harness small cyclic peptides for intracellular interactions.
  • Funding from Swiss National Science Foundation and EU Framework Programme supports the study.