An intramolecular tryptophan-condensation approach for peptide stapling†,Organic & Biomolecular Chemistry

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An intramolecular tryptophan-condensation approach for peptide stapling†
Organic & Biomolecular Chemistry ( IF 3.2 ) Pub Date : 2017-12-08 00:00:00 , DOI: 10.1039/c7ob02667f
Eunice Y.-L. Hui _{1,

2,

3,

4} , Bhimsen Rout _{5,

6,

7,

8} , Yaw Sing Tan _{3,

9,

10} , Chandra S. Verma _{3,

9,

10,

11,

12} , Kok-Ping Chan _{1,

2,

3,

4} , Charles W. Johannes _{1,

2,

3,

4}

Affiliation

Stapled peptides are gaining tremendous interest as next-generation therapeutic agents to target protein–protein interactions. Herein, we report an intramolecular peptide stapling method which links two tryptophan residues at the C2 position of the indole moieties via acid-mediated condensation with an aldehyde.

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