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Updated: May 31, 2026

Constructing Cyclic Peptides Using an On-Tether Sulfonium Center

Constructing Cyclic Peptides Using an On-Tether Sulfonium Center

Published on: September 28, 2022

Contemporary strategies for peptide macrocyclization.

Christopher J White¹, Andrei K Yudin

¹University of Toronto, Chemistry, 80 St. George Street, Toronto, Ontario M5S 3H6, Canada.

Nature Chemistry

|June 24, 2011

Summary

This summary is machine-generated.

Synthesizing cyclic peptides, or peptide macrocycles, is challenging due to unfavorable conformations. Recent synthetic strategies overcome these hurdles, enabling new applications in drug discovery and nanomaterials.

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Published on: September 19, 2022

Area of Science:

Organic Chemistry
Medicinal Chemistry
Materials Science

Background:

Peptide macrocycles are versatile ring-shaped molecules with applications in drug discovery and nanomaterials.
Their utility stems from the ability to fine-tune molecular conformation via chemical synthesis.
Traditional methods struggle with macrocyclization due to entropically disfavored pre-cyclization states.

Purpose of the Study:

To review recent advancements in overcoming synthetic challenges for peptide macrocycles.
To highlight novel strategies for efficient macrocyclization.

Main Methods:

Review of contemporary synthetic methodologies for cyclic peptide preparation.
Analysis of techniques enabling entropically disfavored conformations for cyclization.

Main Results:

Identification of key breakthroughs in peptide macrocycle synthesis.
Demonstration of improved yields and accessibility of cyclic peptides.

Conclusions:

Recent synthetic solutions have significantly advanced the preparation of peptide macrocycles.
These advancements expand the potential of cyclic peptides in diverse scientific fields.