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Constructing Cyclic Peptides Using an On-Tether Sulfonium Center
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Global analysis of peptide cyclization efficiency.

Amit Thakkar1, Thi Ba Trinh, Dehua Pei

  • 1Department of Chemistry and Biochemistry, The Ohio State University, 100 West 18th Avenue, Columbus, Ohio 43210, United States.

ACS Combinatorial Science
|December 26, 2012
PubMed
Summary
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Macrocyclization of peptides is key for drug discovery. This study found that large cyclic peptides cyclize efficiently, while smaller ones require aqueous additives for successful synthesis.

Area of Science:

  • Medicinal Chemistry
  • Biotechnology
  • Peptide Synthesis

Background:

  • Cyclic peptides are vital in drug discovery and nanotechnology.
  • Macrocyclization is often challenging, with yields affected by ring size, sequence, and conditions.

Purpose of the Study:

  • To analyze cyclization efficiency across >2 million peptide sequences.
  • To determine the impact of ring size, peptide sequence, and solvent on backbone cyclization.

Main Methods:

  • Screening of combinatorial peptide libraries.
  • Analysis of on-resin backbone (N-to-C) cyclization efficiency.
  • Investigating the effects of PyBOP, ring size, and sequence composition.

Main Results:

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Last Updated: May 15, 2026

Constructing Cyclic Peptides Using an On-Tether Sulfonium Center
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Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation
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Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation

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  • On-resin cyclization of medium/large rings (cyclohexapeptides+) is highly efficient (>99.96%).
  • Small rings (cyclotetrapeptides, cyclopentapeptides) show significant dimer formation.
  • Difficult sequences often contain Lys(Boc), Arg(Pbf), or sterically hindered N-terminal residues.

    • Conclusions:

    • Large cyclic peptide synthesis is highly efficient.
    • Small cyclic peptide synthesis is challenging but can be improved with aqueous additives.
    • Sequence composition significantly impacts cyclization success, especially for smaller rings.