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

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.

SUBMITTER: Gilliam AJ

PROVIDER: S-EPMC5529100 | biostudies-literature | 2016 Apr

REPOSITORIES: biostudies-literature

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

Gilliam Amanda J H AJ Smith Joshua N JN Flather Dylan D Johnston Kevin M KM Gansmiller Andrew M AM Fishman Dmitry A DA Edgar Joshua M JM Balk Mark M Majumdar Sudipta S Weiss Gregory A GA

Journal of medicinal chemistry 20160411 8

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. ...[more]

PMID: 27010220

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