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CHAPTER 5

Macrocyclic Peptides for Intracellular Drug Targets

There has been sustained interest in cyclic peptides as new modalities in medicinal chemistry research. The amino acid composition and greater molecular size of cyclic peptides, compared to conventional small-molecule drugs, has made cyclic peptides viable molecules for interrogating difficult targets such as protein–protein interactions. However, these binding and screening advantages of cyclic peptides also lead to poor pharmacokinetic properties. Cellular permeability and, more importantly, the ability to engage with intracellular targets remains an ongoing challenge. This chapter covers recent developments for passive cellular permeability of cyclic peptides by intramolecular hydrogen bonding, scaffold design, and peptide modifications. Notable examples and strategies in the active transport of cyclic peptides are also discussed.

Publication details


Print publication date
26 Jun 2017
Copyright year
2017
Print ISBN
978-1-78262-732-6
PDF eISBN
978-1-78801-153-2
ePub eISBN
978-1-78801-171-6
From the book series:
Drug Discovery