Department of Inorganic Chemistry, Faculty of Pharmacy, Medical University of Gdańsk, Al. Gen. J. Hallera 107, 80-416, Gdańsk, Poland.
Polpharma Biologics, Gdańsk, Poland.
Protein J. 2018 Feb;37(1):2-12. doi: 10.1007/s10930-018-9755-0.
Antimicrobial peptides are promising candidates for anti-infective pharmaceuticals. Unfortunately, because of their low proteolytic and chemical stability, their usage is generally narrowed down to topical formulations. Until now, numerous approaches to increase peptide stability have been proposed. One of them, peptide hydrocarbon stapling, a modification based on stabilizing peptide secondary structure with a side-chain covalent hydrocarbon bridge, have been successfully applied to many peptides. Moreover, constraining secondary structure of peptides have also been proven to increase their biological activity. This review article describes studies on hydrocarbon stapled antimicrobial peptides with respect to improved drug-like properties.
抗菌肽是很有前途的抗感染药物候选物。遗憾的是,由于其蛋白酶和化学稳定性低,其用途通常局限于局部制剂。迄今为止,已经提出了许多增加肽稳定性的方法。其中之一是肽的烃链稳定化,这是一种通过侧链共价烃桥稳定肽二级结构的修饰方法,已成功应用于许多肽。此外,约束肽的二级结构也已被证明可以提高其生物活性。本文综述了烃链稳定化抗菌肽在改善药物性质方面的研究。