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Concerns in the Design and Development of Novel Antimicrobial Peptides

机译:新型抗菌肽设计与开发中的问题

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Peptide and protein based therapeutics are the most promising approaches in today medicine. Bioactive peptides can be valuable drugs in the treatment of various illnesses, such as cardiovascular and neurodegenerative diseases. Cell toxic peptides can be considered for cancer or infection therapy. Antimicrobial peptides (AMPs) are one of the most interesting antibiotic groups in this regard, especially in drug resistance infections. Numerous AMPs have been discovered from the natural source; however, artificial synthetic ones have been also developed based on rational design or bioinformatics modeling. Physicochemical features of AMPs are highly important in their antibacterial activity as well as their toxicity. The best AMP is the one that has selective potent antimicrobial bioactivity and no or least hemolytic and cytotoxic effect. In this review, various structural factors affecting the AMPs bioactivity, such as AMPs size, charge, amphipathicity, and amino acid sequence are illustrated considering the most recently published articles. Finally, the trends in AMP design and development are discussed. HIGHLIGHTS ?Antimicrobial peptides are highly interesting antibiotics in multi-drug resistance infections. ?Antimicrobial peptides are short peptides with less than 50 amino acids and overall positive charge. ?First and second structural features of AMPs are important factors in their bioactivities. ?Cyclization and branching of AMPs could affect their pharmacokinetic and pharmacodynamics.
机译:基于肽和蛋白质的疗法是当今医学中最有前途的方法。生物活性肽可能是治疗各种疾病(例如心血管疾病和神经退行性疾病)的有价值的药物。可以考虑将细胞毒性肽用于癌症或感染治疗。在这方面,抗菌肽(AMPs)是最有趣的抗生素组之一,尤其是在耐药性感染中。从自然资源中发现了许多AMP。然而,基于合理设计或生物信息学模型也已经开发了人工合成的合成材料。 AMP的理化特性在其抗菌活性和毒性方面非常重要。最好的AMP是具有选择性强效抗微生物生物活性且无溶血作用和细胞毒作用的药物。在这篇综述中,考虑到最新发表的文章,举例说明了影响AMPs生物活性的各种结构因素,例如AMPs的大小,电荷,两亲性和氨基酸序列。最后,讨论了AMP设计和开发的趋势。亮点?抗菌肽是引起多药耐药性感染的令人非常感兴趣的抗生素。抗菌肽是少于50个氨基酸且总带正电荷的短肽。 AMPs的第一和第二结构特征是其生物活性的重要因素。 AMPs的环化和分支化可能影响其药代动力学和药效学。

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