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Inside Cover: A One‐Pot Chemically Cleavable Bis‐Linker Tether Strategy for the Synthesis of Heterodimeric Peptides (Angew. Chem. Int. Ed. 47/2016)
Nitin A Patil, Julien Tailhades, John A Karas, Frances Separovic, John D Wade, Mohammed Akhter Hossain
Angewandte Chemie International Edition
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.