Optimized Fmoc solid‐phase synthesis of the cysteine‐rich peptide linaclotide

  title={Optimized Fmoc solid‐phase synthesis of the cysteine‐rich peptide linaclotide},
  author={Miriam G{\'o}ngora-Ben{\'i}tez and J. Tulla-Puche and Marta Parad{\'i}s-Bas and O. Werbitzky and M. Giraud and F. Albericio},
  journal={Peptide Science},
  • Miriam Góngora-Benítez, J. Tulla-Puche, +3 authors F. Albericio
  • Published 2011
  • Chemistry, Medicine
  • Peptide Science
  • Linaclotide, a small 14‐mer peptide highly rich in cysteines, is currently in phase III clinical trials for the treatment of gastrointestinal disorders. The challenge in the assembly of linaclotide consists of achieving the correct and clean folding of its three disulfide bridges. For this purpose, a number of regioselective, semiregioselective, and random strategies have been studied. In addition to selecting distinct protecting groups for the thiol function, their position in the sequence… CONTINUE READING
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