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Related Experiment Video

Updated: Mar 7, 2026

Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation
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Cyclic peptide therapeutics: past, present and future.

Alessandro Zorzi1, Kaycie Deyle1, Christian Heinis1

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Cyclic peptides offer therapeutic advantages like high binding affinity and low toxicity. Novel de novo design methods are expanding their use beyond natural products for future drug development.

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Area of Science:

  • Pharmaceutical Science
  • Medicinal Chemistry
  • Drug Discovery

Background:

  • Cyclic peptides possess desirable therapeutic properties including high binding affinity, target selectivity, and low toxicity.
  • Over 40 cyclic peptide drugs are in clinical use, with approximately one new drug approved annually.
  • The majority of approved cyclic peptides originate from natural products like antimicrobials and peptide hormones.

Purpose of the Study:

  • To highlight the growing importance of cyclic peptides in therapeutic development.
  • To discuss the impact of novel design techniques on expanding the scope of cyclic peptide applications.
  • To project the future clinical use of de novo designed cyclic peptides.

Main Methods:

  • Review of existing literature on cyclic peptide therapeutics.
  • Analysis of trends in cyclic peptide drug approval and clinical evaluation.
  • Examination of rational design and in vitro evolution techniques for de novo cyclic peptide development.

Main Results:

  • Cyclic peptides are a well-established therapeutic modality with a consistent market entry rate.
  • Natural products remain the primary source for approved cyclic peptides.
  • Emerging de novo design techniques are yielding novel cyclic peptide ligands for challenging targets.

Conclusions:

  • De novo designed cyclic peptides represent a significant advancement, offering solutions for targets lacking natural ligands.
  • The increasing number of de novo developed cyclic peptides in clinical evaluation suggests their future therapeutic importance.
  • Cyclic peptides, both natural and de novo designed, are poised for continued growth in the pharmaceutical landscape.