A simple and efficient maleimide-based approach for peptide extension with a cysteine-containing peptide phage library

作者：Santoso Buyung; Lam Son; Murray Brion W^*; Chen Gang

来源：Bioorganic & Medicinal Chemistry Letters, 2013, 23(20): 5680-5683.

DOI：10.1016/j.bmcl.2013.08.032

• Epidermal growth factor receptor
• Peptide phage display library
• CovX body
• Maleimide
• Conjugation

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 strat