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Antifungal Drugs
Metabolites ( IF 3.4 ) Pub Date : 2020-03-12 , DOI: 10.3390/metabo10030106
Jiří Houšť , Jaroslav Spížek , Vladimír Havlíček

We reviewed the licensed antifungal drugs and summarized their mechanisms of action, pharmacological profiles, and susceptibility to specific fungi. Approved antimycotics inhibit 1,3-β-d-glucan synthase, lanosterol 14-α-demethylase, protein, and deoxyribonucleic acid biosynthesis, or sequestrate ergosterol. Their most severe side effects are hepatotoxicity, nephrotoxicity, and myelotoxicity. Whereas triazoles exhibit the most significant drug–drug interactions, echinocandins exhibit almost none. The antifungal resistance may be developed across most pathogens and includes drug target overexpression, efflux pump activation, and amino acid substitution. The experimental antifungal drugs in clinical trials are also reviewed. Siderophores in the Trojan horse approach or the application of siderophore biosynthesis enzyme inhibitors represent the most promising emerging antifungal therapies.

中文翻译:

抗真菌药

我们审查了许可的抗真菌药物,并总结了它们的作用机制,药理学特征以及对特定真菌的敏感性。批准的抗真菌药抑制1,3-β- d-葡聚糖合酶,羊毛甾醇14-α-脱甲基酶,蛋白质和脱氧核糖核酸生物合成,或螯合麦角固醇。它们最严重的副作用是肝毒性,肾毒性和骨髓毒性。三唑显示出最显着的药物相互作用,而棘球and素则几乎不显示。可能在大多数病原体上产生抗真菌耐药性,包括药物靶标过表达,外排泵激活和氨基酸取代。还对临床试验中的实验性抗真菌药物进行了综述。特洛伊木马方法中的铁载体或铁载体生物合成酶抑制剂的应用代表了最有希望的新兴抗真菌疗法。
更新日期:2020-04-20
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