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  • Title: A simple and efficient maleimide-based approach for peptide extension with a cysteine-containing peptide phage library.
    Author: Santoso B, Lam S, Murray BW, Chen G.
    Journal: Bioorg Med Chem Lett; 2013 Oct 15; 23(20):5680-3. PubMed ID: 23992863.
    Abstract:
    Although peptide-based molecules are known to have therapeutic potential, the generation of phage focused libraries to optimize peptides is effort-consuming. A chemical method is developed to extend a maleimide-conjugated peptide with a cysteine-containing random-peptide phage display library. As a proof of concept, a 15-mer epidermal growth factor receptor (EGFR)-binding peptide was synthesized with a maleimide group at its C-terminus and then conjugated to the cysteine-containing library. After panning and screening, several extended peptides were discovered and tested to have a higher affinity to EGFR. This strategy can have broad utility to optimize pharmacophores of any modalities (peptides, unnatural peptides, drug conjugates) capable of bearing a maleimide group.
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