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Directed evolution of bicyclic peptides for therapeutic application
Philippe Diderich, Christian Heinis1
1Institute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne, CH-1015 Lausanne, Switzerland.
Chimia
|March 6, 2014
Summary
Cyclic peptides are effective therapeutics due to high affinity and low toxicity. Researchers are developing novel bicyclic peptide ligands using directed evolution for diverse therapeutic applications.
Area of Science:
- Medicinal Chemistry
- Biotechnology
- Pharmacology
Background:
- Naturally occurring cyclic peptides like vasopressin and vancomycin are established therapeutics.
- Their therapeutic success stems from high target affinity, selectivity, and low toxicity.
- Nature offers limited cyclic peptides for specific disease targets, necessitating de novo ligand generation.
Purpose of the Study:
- To review recent advancements in evolving bicyclic peptide ligands.
- To discuss the binding and pharmacokinetic properties of these peptides.
- To highlight efforts in developing bicyclic peptides for therapeutic use.
Main Methods:
- Directed evolution using phage display to generate bicyclic peptide ligands.
- In vitro evolution of bicyclic peptide antagonists.
- Characterization of binding and pharmacokinetic properties.
Main Results:
- Successful in vitro evolution of bicyclic peptide antagonists.
- Detailed analysis of binding affinities and pharmacokinetic profiles.
- Demonstrated potential for therapeutic applications.
Conclusions:
- Directed evolution is a powerful strategy for generating novel bicyclic peptide therapeutics.
- Bicyclic peptides exhibit promising binding and pharmacokinetic properties.
- Further development holds potential for new therapeutic agents.
