Inside Cover: A One‐Pot Chemically Cleavable Bis‐Linker Tether Strategy for the Synthesis of Heterodimeric Peptides (Angew. Chem. Int. Ed. 47/2016). Issue 47 (20th September 2016)

• Record Type: Journal Article
• Authors: Patil, Nitin A.; Tailhades, Julien; Karas, John A.; Separovic, Frances; Wade, John D.; Hossain, Mohammed Akhter
• Is Part Of: Angewandte Chemie international edition. Volume 55:Issue 47(2016)
• Page Start: 14472
• Page End: 14472
• Publication Date: 2016-09-20
• Subjects: conjugation -- heterodimeric peptides -- N-terminal linkers -- peptides -- solid-phase synthesis; Chemistry -- Periodicals; 540
• DOI: 10.1002/anie.201608906
• Languages: English
• ISSNs: 1433-7851

Abstract

Abstract : Cystine‐Rich heterodimeric peptides or proteins (e.g. insulin) are attractive drug targets. However, their chemical assembly and correct folding is complex, time consuming, and often low yielding. In their Communication on page 14552 ff., J. Tailhades, J. D. Wade, M. A. Hossain, and co‐workers describe a novel strategy in which two peptide chains are sequentially assembled on a solid support separated by a bis‐linker tether. Following folding, the tether is removed by hydrazinolysis to produce the peptide in high yield and less time.