Recent Progress in the Discovery of Antifungal Agents Targeting the Cell Wall
Recent Progress in the Discovery of Antifungal Agents Targeting the Cell Wall
复制标题
针对细胞壁的抗真菌药物的发现最新进展
DOI：
10.1021/acs.jmedchem.0c00748
复制
发表时间：
2020-11-12
影响因子：
7.3
通讯作者：
Wang, Shengzheng
中科院分区：
文献类型：
--
作者：
Liu, Wei;Yuan, Lin;Wang, Shengzheng
由于临床上可用治疗方法的限制和耐药性的出现，侵袭性真菌感染是一个棘手的问题，具有高发病率和死亡率。细胞壁作为真菌特有的结构，是发现和开发新型低毒抗真菌药物的一个有吸引力的靶点。为了加速新型细胞壁靶向药物的发现，本展望将对真菌细胞壁抑制剂的开发进展进行全面综述。本文就其作用靶点、发现过程、化学结构、抗真菌活性及构效关系等方面进行综述。虽然目前已有两类细胞壁抗真菌药物在临床上上市或处于临床试验阶段，但其他细胞壁靶向抑制剂的临床应用仍有很长的路要走。未来的努力应集中在识别抑制剂对新的保守的细胞壁目标。
Due to the limit of available treatments and the emergence of drug resistance in the clinic, invasive fungal infections are an intractable problem with high morbidity and mortality. The cell wall, as a fungi-specific structure, is an appealing target for the discovery and development of novel and low-toxic antifungal agents. In an attempt to accelerate the discovery of novel cell wall targeted drugs, this Perspective will provide a comprehensive review of the progress made to date on the development of fungal cell wall inhibitors. Specifically, this review will focus on the targets, discovery process, chemical structures, antifungal activities, and structure-activity relationships. Although two types of cell wall antifungal agents are clinically available or in clinical trials, it is still a long way for the other cell wall targeted inhibitors to be translated into clinical applications. Future efforts should be focused on the identification of inhibitors against novel conserved cell wall targets.