Discovery of a new chemical scaffold for the treatment of superbug Candida auris infections.
Discovery of a new chemical scaffold for the treatment of superbug Candida auris infections.
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DOI：
10.1080/22221751.2023.2208687
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发表时间：
2023-12
影响因子：
13.2
通讯作者：
中科院分区：
文献类型：
--
作者：
念珠菌具有耐多药、高传染性和高致死率等特点，已成为严重的公共卫生威胁，并在全球流行。为了应对这一具有挑战性的超级真菌，通过表型筛选、命中优化、抗真菌试验和机制探索等综合策略，发现了新型苯并苯胺类抗真菌药物。其中最有希望的化合物A1在体外和体内对耳念珠菌均有较强的抗感染作用。机制研究表明，化合物A1通过抑制糖基磷脂酰肌醇（GPI）和GPI锚定蛋白阻断毒力因子和真菌细胞壁的生物合成。因此，化合物A1是一种很有前途的抗耐药念珠菌病先导化合物。
Candida auris has emerged as a serious threat of public health and caused global epidemic due to multi-drug resistance, remarkable transmissibility and high mortality. To tackle the challenging super fungus, novel benzoanilide antifungal agents were discovered by an integrated strategy of phenotypic screen, hit optimization, antifungal assays and mechanism exploration. The most promising compound A1 showed potent in vitro and in vivo efficacy against Candida auris infection. Mechanism investigation revealed that compound A1 blocked the biosynthesis of virulence factors and fungal cell walls through the inhibition of glycosylphosphatidylinositol (GPI) and GPI-anchored proteins. Thus, compound A1 represents a promising lead compound to combat drug-resistant candidiasis.
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DOI：
10.3390/jof7070556
发表时间：
2021-07-13
期刊：
Journal of fungi (Basel, Switzerland)
影响因子：
--
作者：
Frías-De-León MG;Pinto-Almazán R;Hernández-Castro R;García-Salazar E;Meza-Meneses P;Rodríguez-Cerdeira C;Arenas R;Conde-Cuevas E;Acosta-Altamirano G;Martínez-Herrera E
通讯作者：
Martínez-Herrera E
影响因子：
6.7
作者：
Du H;Bing J;Hu T;Ennis CL;Nobile CJ;Huang G
通讯作者：
Huang G
影响因子：
4.9
作者：
Castanheira, Mariana;Duncanson, Frederick P.;Pfaller, Michael A.
通讯作者：
Pfaller, Michael A.
紫檀芪对抗白色念珠菌生物膜的体外和体内活性
影响因子：
4.9
作者：
Li, De-Dong;Zhao, Lan-Xue;Jiang, Yuan-Ying
通讯作者：
Jiang, Yuan-Ying
影响因子：
4.5
作者：
Billamboz M;Fatima Z;Hameed S;Jawhara S
通讯作者：
Jawhara S