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Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation
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Methodologies for Backbone Macrocyclic Peptide Synthesis Compatible With Screening Technologies.

Koki Shinbara1, Wenyu Liu1, Renier Herman Pieter van Neer1

  • 1Department of Chemistry, Graduate School of Science, The University of Tokyo, Tokyo, Japan.

Frontiers in Chemistry
|July 7, 2020
PubMed
Summary

Backbone macrocyclic peptides offer enhanced stability and drug-like properties. Recent synthetic advancements and compatible screening methods accelerate the discovery of novel peptide therapeutics.

Keywords:
OBOC screeningSICLOPPSbackbone macrocyclic peptideenzymatic peptide backbone cyclizationin vitro screeningnon-proteinogenic amino acidpeptide library

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Area of Science:

  • Medicinal Chemistry
  • Synthetic Biology
  • Drug Discovery

Background:

  • Backbone macrocyclic peptides possess superior conformational rigidity, peptidase resistance, and membrane permeability compared to linear peptides.
  • These properties make macrocyclic peptides attractive scaffolds for developing novel therapeutic agents.
  • Advances in synthesis have enabled the exploration of diverse peptide drug candidates.

Purpose of the Study:

  • To provide an overview of recent technical advancements in the synthesis of backbone macrocyclic peptides.
  • To discuss screening methodologies compatible with these advanced synthetic approaches.
  • To highlight the potential of macrocyclic peptides in drug discovery.

Main Methods:

  • Enzymatic synthesis
  • Chemical synthesis
  • Split-intein circular ligation of peptides and proteins (SICLOPPS)
  • In vitro translation systems with genetic code reprogramming
  • One-beads one-compound (OBOC) screening
  • Cell-based assays
  • Limiting-dilution PCR
  • mRNA display

Main Results:

  • Several advanced synthetic methodologies for backbone macrocyclic peptides have been developed.
  • Specific screening techniques are compatible with each synthetic approach, facilitating efficient candidate identification.
  • These combined methods offer powerful tools for discovering new peptide drugs.

Conclusions:

  • Technical advancements in macrocyclic peptide synthesis are rapidly expanding drug discovery capabilities.
  • Integrated synthetic and screening strategies are crucial for identifying novel peptide therapeutics.
  • Macrocyclic peptides represent a promising class of molecules for future drug development.