Do Peptide Drugs Need Acylation Blocking at Nα?

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Alice Beily

Abstract

The formation of 2,5-diketopiperazine (DKP) with a bicyclic structure is one of the most detrimental side reactions and degradation pathways affecting peptide synthesis. Despite its crucial role as a versatile building block in drug discovery, the formation of DKP reactions is highly undesirable in the production of peptide drugs. DKP formation can occur during the process of peptide drug formulation, as well as in the storage of starting materials and finished products, and may even occur under solid phase synthesis conditions.

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