A Brief Guide to Preparing a Peptide–Drug Conjugate

Assembly instructions: Peptide–drug conjugates (PDCs) are constituted of a peptide/peptidomimetic unit and a drug/probe unit. The conjugation between these two portions can be performed either in a click or a non-click reaction, based on the available functional groups on both the peptide/drug residues.

Abstract

Peptide–drug conjugates (PDCs) have recently emerged as interesting hybrid constructs not only for targeted therapy, but also for the early diagnosis of different pathologies. In most cases, the crucial step in the PDC synthesis is the final conjugation step, where a specific drug is bound to a particular peptide-/peptidomimetic-targeting unit. Thus, this concept paper aims to give a short guide to determining the finest conjugation reaction, by considering in particular the reaction conditions, the stability of the linker and the major pros and cons of each reaction. Based on the recent PDCs reported in literature, the most common and efficient conjugation methods will be systematically presented and compared, generating a short guide to consult while planning the synthesis of a novel peptide–drug conjugate.

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