Tackling Fungal Resistance by Biofilm Inhibitors.

Tackling Fungal Resistance by Biofilm Inhibitors.
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通过生物膜抑制剂应对真菌耐药性。

DOI:
10.1021/acs.jmedchem.6b01203
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发表时间:
2017-01
影响因子:
7.3
通讯作者:
Sheng Chunquan
Sheng Chunquan
中科院分区:
医学1区
文献类型:
--
作者:
Wu Shanchao;Wang Yan;Liu Na;Dong Guoqiang;Sheng Chunquan

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侵袭性真菌感染的高发病率和死亡率以及严重的耐药性已成为全球性的公共卫生问题。真菌细胞形成生物被膜的能力是导致对大多数临床可用抗真菌剂出现严重耐药性的重要原因。通过小分子靶向真菌生物膜的形成是开发新型抗真菌药物的一个有前途的新策略。这一观点将提供一个全面的审查真菌生物膜抑制剂。特别是,发现策略,化学结构,抗菌膜/抗真菌活性,和结构-活性关系的研究将进行讨论。开发治疗生物膜相关耐药真菌感染的抑制剂是一种新的但临床上尚未开发的范式,距离临床应用还有很长的路要走。更好地了解真菌生物膜结合系统的药物发现工作将为潜在的临床应用铺平道路。
The high incidence and mortality of invasive fungal infections and serious drug resistance have become a global public health issue. The ability of fungal cells to form biofilms is an important reason for the emergence of severe resistance to most clinically available antifungal agents. Targeting fungal biofilm formation by small molecules represents a promising new strategy for the development of novel antifungal agents. This perspective will provide a comprehensive review of fungal biofilm inhibitors. In particular, discovery strategies, chemical structures, antibiofilm/antifungal activities, and structure-activity relationship studies will be discussed. Development of inhibitors to treat biofilm-related resistant fungal infections is a new yet clinically unexploited paradigm, and there is still a long way to go to clinical application. Better understanding of fungal biofilms in combination with systematic drug discovery efforts will pave the way for potential clinical applications.
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