Kosikowska Paulina, Lesner Adam
a Faculty of Chemistry , University of Gdansk , Gdansk , Poland.
Expert Opin Ther Pat. 2016 Jun;26(6):689-702. doi: 10.1080/13543776.2016.1176149. Epub 2016 Apr 22.
Antimicrobial peptides (AMPs) represent the large group of endogenous compounds widely distributed in nature. Due to their broad spectrum of antibiotic activity, as well as anti-inflammatory and immunomodulatory properties, AMPs became a model for the discovery of novel antimicrobial drugs that could answer the problem of the increasing antibiotic resistance of pathogenic microorganisms.
The review represents a comprehensive analysis of patents and patent applications from the year 2003 to 2015 referring to the therapeutic use of AMPs. The article highlights the general trends in the design, potential mode of action, and methods of biological evaluation of AMPs.
The existing discord between the upcoming list of antimicrobial peptides claimed in the patents or related scientific articles as the potent drug candidates and the frequent failures of AMPs in clinical trials emphasize the need of a better understanding of their pleiotropic nature and mechanisms of host defense in general. Nevertheless, the encouraging examples of AMPs already introduced into the market, like Polymyxin or Fuzeon®, give some reason for optimism that development of AMPs as a novel class of antibiotics is still considered viable.
抗菌肽(AMPs)是一大类广泛分布于自然界的内源性化合物。由于其广谱的抗菌活性以及抗炎和免疫调节特性,抗菌肽成为了发现新型抗菌药物的模型,这类新型抗菌药物有望解决致病微生物抗生素耐药性不断增加的问题。
本综述全面分析了2003年至2015年期间涉及抗菌肽治疗用途的专利和专利申请。文章突出了抗菌肽设计的总体趋势、潜在作用模式以及生物学评估方法。
专利或相关科学文章中声称的作为潜在药物候选物的抗菌肽名单不断增加,与抗菌肽在临床试验中频繁失败之间存在的现有矛盾,凸显了更深入了解其多效性本质和宿主防御机制的必要性。尽管如此,已上市的抗菌肽,如多粘菌素或福泽昂(Fuzeon®),这些令人鼓舞的例子让人们有理由乐观地认为,将抗菌肽开发为一类新型抗生素仍然是可行的。