The development of solid phase peptide synthesis has released tremendous opportunities for using synthetic peptides in medicinal applications. In the last decades, peptide therapeutics became an emerging market in pharmaceutical industry. The need for synthetic strategies in order to improve peptidic properties, such as longer half-life, higher bioavailability, increased potency and efficiency is accordingly rising. In this mini-review, we present a toolbox of modifications in peptide chemistry for overcoming the main drawbacks during the transition from natural peptides to peptide therapeutics. Modifications at the level of the peptide backbone, amino acid side chains and higher orders of structures are described. Furthermore, we are discussing the future of peptide therapeutics development and their impact on the pharmaceutical market.

固相肽合成的发展为在医学应用中使用合成肽释放了巨大的机会。在过去的几十年中，肽治疗剂已成为制药行业的新兴市场。因此，对合成策略以改善肽特性，例如更长的半衰期，更高的生物利用度，增加的效能和效率的需求正在增加。在此小型审查中，我们介绍了一种肽化学修饰工具箱，用于克服从天然肽向肽治疗剂过渡过程中的主要弊端。描述了在肽主链，氨基酸侧链和更高阶结构上的修饰。此外，我们正在讨论肽疗法的未来发展及其对制药市场的影响。