Department of Microbiology and Molecular Genetics, The University of Texas Health Science Center at Houston, Houston, TX, 77030, USA.
BioZone, Department of Chemical Engineering and Applied Chemistry, University of Toronto, Toronto, ON, M5S 3E5, Canada.
Nat Commun. 2022 Oct 13;13(1):6047. doi: 10.1038/s41467-022-33613-1.
Fungal pathogens are a continuing challenge due to few effective antifungals and a rise in resistance. In previous work, we described the inhibition of Candida albicans virulence following exposure to the 68 amino acid bacteriocin, EntV, secreted by Enterococcus faecalis. Here, to optimize EntV as a potential therapeutic and better understand its antifungal features, an X-ray structure is obtained. The structure consists of six alpha helices enclosing a seventh 16 amino acid helix (α7). The individual helices are tested for antifungal activity using in vitro and nematode infection assays. Interestingly, α7 retains antifungal, but not antibacterial activity and is also effective against Candida auris and Cryptococcus neoformans. Further reduction of α7 to 12 amino acids retains full antifungal activity, and excellent efficacy is observed in rodent models of C. albicans oropharyngeal, systemic, and venous catheter infections. Together, these results showcase EntV-derived peptides as promising candidates for antifungal therapeutic development.
真菌病原体是一个持续存在的挑战,因为有效的抗真菌药物很少,而且耐药性不断上升。在之前的工作中,我们描述了在暴露于肠球菌分泌的 68 个氨基酸细菌素 EntV 后,白色念珠菌毒力的抑制作用。在这里,为了优化 EntV 作为一种潜在的治疗方法,并更好地了解其抗真菌特性,我们获得了一个 X 射线结构。该结构由六个α螺旋围绕着第七个 16 个氨基酸的螺旋(α7)组成。使用体外和线虫感染实验测试了各个螺旋的抗真菌活性。有趣的是,α7 保留了抗真菌活性,但没有抗菌活性,对耳念珠菌和新型隐球菌也有效。进一步将α7 减少到 12 个氨基酸保留了完全的抗真菌活性,在白色念珠菌口咽、全身和静脉导管感染的啮齿动物模型中观察到了极好的疗效。总之,这些结果表明 EntV 衍生肽是抗真菌治疗开发的有前途的候选药物。