Lombardi Lucia, Genio Valentina Del, Albericio Fernando, Williams Daryl R
Department of Chemical Engineering, Imperial College London, South Kensington, London SW7 2AZ, U.K.
School of Biological Sciences, Queen's University Belfast, 19 Chlorine Gardens, Belfast, BT9 5DL, U.K.
Chem Rev. 2025 Aug 13;125(15):7099-7166. doi: 10.1021/acs.chemrev.4c00989. Epub 2025 Jul 23.
Over the past two decades, peptide drug discovery has experienced a remarkable renaissance, with organic chemistry and biotechnology emerging as pivotal tools for developing peptidomimetics that exhibit improved stability, specificity, and bioavailability compared to conventional peptides. This review systematically examines methodologies for modifying peptide backbones to achieve targeted properties, highlighting recent advances facilitated by modern biotechnological innovations for novel molecular transformations. Additionally, the review emphasizes the practical applications of peptides and peptidomimetics, showcasing their successful integration into medicine and pharmacology. This manuscript evaluates achievements and challenges in the field and identifies critical areas for further research. Its overarching aim is to synthesize current knowledge and propose strategic directions for advancing peptide-based therapeutics.
在过去二十年中,肽类药物研发经历了显著的复兴,有机化学和生物技术成为开发肽模拟物的关键工具,与传统肽相比,这些肽模拟物具有更高的稳定性、特异性和生物利用度。本综述系统地研究了修饰肽主链以实现目标特性的方法,突出了现代生物技术创新促进新型分子转化的最新进展。此外,该综述强调了肽和肽模拟物的实际应用,展示了它们成功融入医学和药理学的情况。本文评估了该领域的成就和挑战,并确定了进一步研究的关键领域。其总体目标是综合当前知识,并为推进基于肽的治疗方法提出战略方向。