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Updated: Jun 12, 2026

Microwave-assisted Functionalization of Poly(ethylene glycol) and On-resin Peptides for Use in Chain Polymerizations and Hydrogel Formation

Microwave-assisted Functionalization of Poly(ethylene glycol) and On-resin Peptides for Use in Chain Polymerizations and Hydrogel Formation

Published on: October 29, 2013

Late-Stage Functionalization of Peptides on the Solid Phase.

Marius Werner^1,2, Truc Lam Pham³, Franziska Thomas¹

¹Institute of Organic Chemistry, Heidelberg University, Heidelberg, Germany.

Angewandte Chemie (International Ed. in English)

|June 11, 2026

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Chemical modification of peptides using on-resin late-stage functionalization offers efficient ways to develop new peptide therapeutics. This review highlights chemical methods that streamline peptide drug development and enhance bioactivity.

Area of Science:

Medicinal Chemistry
Organic Chemistry
Biotechnology

Background:

Peptide modification is crucial for tailoring structure and function, especially in peptide drug development.
Developing methods for incorporating non-canonical residues into peptides is highly sought after.
On-resin late-stage functionalization provides a cost- and time-efficient approach for peptide modification.

Purpose of the Study:

To provide an overview of chemical approaches for on-resin late-stage peptide functionalization.
To highlight recent advancements in the field, particularly those developed in the past decade.
To showcase the potential of these methods in streamlining peptide therapeutics development.

Main Methods:

Review of various chemical strategies including nucleophilic substitution, carbonyl chemistry, metal catalysis, and photocatalysis.

Keywords:

late‐stage functionalization non‐canonical amino acids peptide therapeutics peptides solid phase peptide synthesis

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Last Updated: Jun 12, 2026

Microwave-assisted Functionalization of Poly(ethylene glycol) and On-resin Peptides for Use in Chain Polymerizations and Hydrogel Formation

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Published on: October 29, 2013

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Discussion of methods compatible with both short and long peptides.

Examination of applications in high-throughput peptide library synthesis.

Main Results:

Numerous chemical approaches for on-resin late-stage peptide functionalization have been developed.
These methods are effective for modifying peptides and modulating their bioactivity.
Successful synthesis of peptide libraries in high-throughput formats has been demonstrated.

Conclusions:

On-resin late-stage peptide functionalization is a powerful tool for peptide drug development.
The reviewed chemical methods offer efficiency and versatility for peptide modification.
These techniques hold significant promise for the future of peptide therapeutics.