Department of Biochemical and Pharmaceutical Technology, University of São Paulo, Av. Prof. LineuPrestes n 580 Bl. 16, 05508-000 São Paulo, SP Brazil.
Department of Chemical Engineering, Faculty of Engineering and Science, Universidad de La Frontera, Temuco, Chile.
J Mater Chem B. 2022 May 18;10(19):3587-3600. doi: 10.1039/d1tb02757c.
Antimicrobial peptides (AMPs) are ubiquitous host defense peptides characterized by their antibiotic activity and lower propensity for developing resistance compared to classic antibiotics. While several AMPs have shown activity against antibiotic-sensitive and even multi-drug resistant strains, some bottlenecks to further development and clinical applications are still present, for instance, low antimicrobial activity, instability under physiological conditions, systemic toxicity and the potential for compromising the innate host defense immunity. Conjugation to molecules such as proteins, synthetic polymers, small molecules and nanoparticles are strategies under investigation to boost the therapeutic efficacy of AMPs. This review focuses on the design and application of AMPs' conjugates. tools for creating new AMPs and AMPs' conjugates and their clinical development are also discussed. Furthermore, key future considerations regarding the major achievements and challenges of AMPs' conjugates in the antimicrobial resistance context are presented as a take-home message.
抗菌肽（AMPs）是普遍存在的宿主防御肽，其特点是具有抗生素活性，并且比经典抗生素更不容易产生耐药性。虽然有几种 AMP 对对抗生素敏感甚至多药耐药菌株具有活性，但进一步开发和临床应用仍存在一些瓶颈，例如抗菌活性低、生理条件下不稳定、全身毒性以及破坏固有宿主防御免疫的潜力。与蛋白质、合成聚合物、小分子和纳米颗粒等分子缀合是提高 AMP 治疗效果的研究策略。本综述重点介绍了 AMP 缀合物的设计和应用。还讨论了用于创建新的 AMP 和 AMP 缀合物的工具及其临床开发。此外，作为一个要点，还提出了关于 AMP 缀合物在抗菌药物耐药性背景下的主要成就和挑战的未来关键考虑因素。
