2. Academic Validation
  3. Affinity-Guided Design of Caveolin-1 Ligands for Deoligomerization

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.
Amanda J H Gilliam 1,  Joshua N Smith 1,  Dylan Flather 1,  Kevin M Johnston 1,  Andrew M Gansmiller 1,  Dmitry A Fishman 1,  Joshua M Edgar 1,  Mark Balk 1,  Sudipta Majumdar 1,  Gregory A Weiss 1
Affiliations

Affiliation

  • 1 Department of Chemistry, and ‡Department of Molecular Biology and Biochemistry, University of California , Irvine, California 92697-2025, United States.
PMID: 27010220 DOI: 10.1021/acs.jmedchem.5b01536
Abstract

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.

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