Affinity-Guided Design of Caveolin-1 Ligands for Deoligomerization

J Med Chem. 2016 Apr 28;59(8):4019-25. doi: 10.1021/acs.jmedchem.5b01536. Epub 2016 Apr 11.


Caveolin-1 is a target for academic and pharmaceutical research due to its many cellular roles and associated diseases. We report peptide WL47 (1), a small, high-affinity, selective disrupter of caveolin-1 oligomers. Developed and optimized through screening and analysis of synthetic peptide libraries, ligand 1 has 7500-fold improved affinity compared to its T20 parent ligand and an 80% decrease in sequence length. Ligand 1 will permit targeted study of caveolin-1 function.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, N.I.H., Extramural

MeSH terms

  • Biopolymers / metabolism*
  • Caveolin 1 / metabolism*
  • Ligands


  • Biopolymers
  • Caveolin 1
  • Ligands