Affinity-Guided Design of Caveolin-1 Ligands for Deoligomerization

作者:Gilliam Amanda J H; Smith Joshua N; Flather Dylan; Johnston Kevin M; Gansmiller Andrew M; Fishman Dmitry A; Edgar Joshua M; Balk Mark; Majumdar Sudipta; Weiss Gregory A*
来源:Journal of Medicinal Chemistry, 2016, 59(8): 4019-4025.
DOI:10.1021/acs.jmedchem.5b01536

摘要

Caveoliu-1 is a target for academic and pharmaceutical research due to its many cellular roles and associated diseases. We report peptide W147 (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 caveoliri-1 function.

  • 出版日期2016-4-28