Late-Stage Peptide Amination Protocol for Drug Discovery and Catalyst Development

Franziska Thomas presents a protocol for introducing amines into peptides via an on-resin iodination-substitution approach. The method is compatible with primary and secondary amines, anilines, and heteroaromatic N-nucleophiles, yielding good to excellent results. As a proof-of-concept, the metal ligand tris(2-aminoethyl)amine was introduced into a tryptophan zipper scaffold, resulting in a thermal stabilization of more than 30 K.

Use Cases

• Generate libraries of peptide mimetics for drug discovery based on the described late-stage amination approach.
• Develop peptide-based catalysts based on the method's compatibility with metal-binding amines.
• Explore metal-induced stapling in peptide scaffolds based on the proof-of-concept with the tren ligand.
• Screen amine building blocks for peptide modification based on the protocol's wide amine compatibility.

Strengths

• Protocol demonstrates a thermal stabilization of more than 30 K in a proof-of-concept tryptophan zipper design.
• Method is compatible with a wide variety of amines, including primary and secondary amines, anilines, and heteroaromatic N-nucleophiles.

Limitations

• Column-level documentation is absent; field semantics must be inferred after download.
• Row count is unknown, which may limit suitability assessment.

Provenance

Source

heiDATA Harvested Dataverse

Collection Method

Likely contains experimental protocol and results data from the described chemical synthesis approach.

Freshness

Last updated 2026-07-12 07:10:15; freshness should be verified.