Cyclic and macrocyclic peptides as chemical tools to recognise protein surfaces and probe protein-protein interactions

Teresa A. F. Cardote, Alessio Ciulli (Lead / Corresponding author)

Research output: Contribution to journalArticlepeer-review

87 Citations (Scopus)
174 Downloads (Pure)

Abstract

Targeting protein surfaces and protein-protein interactions (PPIs) with small molecules is a frontier goal of chemical biology and provides attractive therapeutic opportunities in drug discovery. The molecular properties of protein surfaces, including their shallow features and lack of deep binding pockets, pose significant challenges, and as a result have proved difficult to target. Peptides are ideal candidates for this mission due to their ability to closely mimic many structural features of protein interfaces. However, their inherently low intracellular stability and permeability and high in vivo clearance have thus far limited their biological applications. One way to improve these properties is to constrain the secondary structure of linear peptides by cyclisation. Herein we review various classes of cyclic and macrocyclic peptides as chemical probes of protein surfaces and modulators of PPIs. The growing interest in this area and recent advances provide evidence of the potential of developing peptide-like molecules that specifically target these interactions.

Original languageEnglish
Pages (from-to)787-794
Number of pages8
JournalChemMedChem
Volume11
Issue number8
Early online date13 Nov 2015
DOIs
Publication statusPublished - 19 Apr 2016

Keywords

  • Chemical probes
  • Chemical tools
  • Cyclic peptides
  • Macrocycles
  • Protein-protein interactions

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