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Affinity-Guided Design of Caveolin-1 Ligands for Deoligomerization.

J Med Chem.. 2016-04; 
Gilliam AJ, Smith JN, Flather D, Johnston KM, Gansmiller AM, Fishman DA, Edgar JM, Balk M, Majumdar S, Weiss GA.
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Peptide Library Services ... Since evolution and library screening identified key sidechain functionalities, a library was synthesized omitting Gly and Phe and shuffling the remaining residues using the GenScript Scrambled Library Peptide Library Design Tool.27 A total of 17 shuffled sequences were ... Get A Quote

摘要

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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