An update on new methods to synthesize cyclotetrapeptides

Org Biomol Chem. 2015 Jul 7;13(25):6906-21. doi: 10.1039/c5ob00880h. Epub 2015 May 29.


Cyclotetrapeptides are important bioactive lead drug molecules that display a wide spectrum of pharmacological activities. However, the synthesis of cyclotetrapeptides from their linear precursors is challenging due to the highly constrained conformation required for cyclisation, thus hampering their progress to a clinical setting. This review provides an account of the reported methods used for the synthesis of cyclotetrapeptides.

Publication types

  • Review

MeSH terms

  • Amino Acid Sequence
  • Chemistry Techniques, Synthetic / methods*
  • Cyclization
  • Oligopeptides / chemical synthesis*
  • Oligopeptides / chemistry
  • Peptides, Cyclic / chemical synthesis*
  • Peptides, Cyclic / chemistry


  • Oligopeptides
  • Peptides, Cyclic