Yang Shihua, Wang Mingge, Wang Tianye, Sun Mengchi, Huang Hanwei, Shi Xianbao, Duan Shijie, Wu Ying, Zhu Jiaming, Liu Funan
Department of Surgical Oncology and General Surgery, The First Hospital of China Medical University, Key Laboratory of Precision Diagnosis and Treatment of Gastrointestinal Tumors, China Medical University, Ministry of Education, Shenyang, 110001, China.
Department of Phase I Clinical Trials Center, The First Hospital of China Medical University, Shenyang, 110102, China.
Mater Today Bio. 2023 Apr 25;20:100644. doi: 10.1016/j.mtbio.2023.100644. eCollection 2023 Jun.
Self-assembled short peptides have intrigued scientists due to the convenience of synthesis, good biocompatibility, low toxicity, inherent biodegradability and fast response to change in the physiological environment. Therefore, it is necessary to present a comprehensive summary of the recent advances in the last decade regarding the construction, route of administration and application of self-assembled short peptides based on the knowledge on their unique and specific ability of self-assembly. Herein, we firstly explored the molecular mechanisms of self-assembly of short peptides, such as non-modified amino acids, as well as Fmoc-modified, N-functionalized, and C-functionalized peptides. Next, cell penetration, fusion, and peptide targeting in peptide-based drug delivery were characterized. Then, the common administration routes and the potential pharmaceutical applications (drug delivery, antibacterial activity, stabilizers, imaging agents, and applications in bioengineering) of peptide drugs were respectively summarized. Last but not least, some general conclusions and future perspectives in the relevant fields were briefly listed. Although with certain challenges, great opportunities are offered by self-assembled short peptides to the fascinating area of drug development.
自组装短肽因其合成方便、生物相容性好、毒性低、具有内在的生物可降解性以及对生理环境变化的快速响应能力而引起了科学家们的兴趣。因此,有必要基于自组装短肽独特的自组装能力方面的知识,对过去十年中有关自组装短肽的构建、给药途径和应用的最新进展进行全面总结。在此,我们首先探讨了短肽自组装的分子机制,例如未修饰的氨基酸以及芴甲氧羰基(Fmoc)修饰的、N-官能化的和C-官能化的肽。接下来,对基于肽的药物递送中的细胞穿透、融合和肽靶向进行了表征。然后,分别总结了肽类药物的常见给药途径和潜在的药物应用(药物递送、抗菌活性、稳定剂、成像剂以及在生物工程中的应用)。最后但同样重要的是,简要列出了相关领域的一些一般性结论和未来展望。尽管存在一定挑战,但自组装短肽为引人入胜的药物开发领域提供了巨大机遇。