Department of Pharmacy, Jaypee University of Information Technology, Waknaghat-173234, Distt. Solan (HP) India.
Curr Pharm Des. 2013;19(32):5809-23. doi: 10.2174/13816128113199990003.
Rapid increase in the emergence and spread of microbes resistant to conventionally used antibiotics has become a major threat to global health care. Antimicrobial peptides (AMPs) are considered as a potential source of novel antibiotics because of their numerous advantages such as broad-spectrum activity, lower tendency to induce resistance, immunomodulatory response and unique mode of action. However, AMPs have several drawbacks such as; susceptibility to protease degradation, toxicity and high costs of manufacturing. Therefore, extensive research efforts are underway to explore the therapeutic potential of these fascinating natural compounds. This review highlights the potential of small cationic antimicrobial peptidomimetics (SCAMPs; M.W. ≅ 700 Da) as new generation antibiotics. In particular, we focused on recently identified small active pharmacophore from bulky templates of native AMPs, β-peptides, and lipopeptides. In addition, various design strategies recently undertaken to improve the physicochemical properties (proteolytic stability & plasma protein binding) of small cationic peptides have also been discussed.
传统抗生素耐药性微生物的迅速出现和传播,已成为全球医疗保健的主要威胁。抗菌肽(AMPs)因其具有广谱活性、较低的耐药诱导倾向、免疫调节反应和独特的作用模式等诸多优点,被认为是新型抗生素的潜在来源。然而,AMPs 也存在一些缺点,如易被蛋白酶降解、毒性和制造成本高。因此,人们正在进行广泛的研究,以探索这些迷人的天然化合物的治疗潜力。本综述强调了小阳离子抗菌肽模拟物(SCAMPs;分子量 ≈ 700 Da)作为新一代抗生素的潜力。特别是,我们专注于最近从天然 AMPs、β-肽和脂肽的大体积模板中鉴定出的小活性药效团。此外,还讨论了最近为改善小阳离子肽的物理化学性质(蛋白酶稳定性和血浆蛋白结合)而采取的各种设计策略。