一种新型 Hsp110 抑制剂作为潜在抗真菌剂的表征。

IF 4.2 2区 生物学 Q2 MICROBIOLOGY
Cancan Sun, Yi Li, Justin M Kidd, Jizhong Han, Liangliang Ding, Aaron E May, Lei Zhou, Qinglian Liu
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引用次数: 0

摘要

真菌感染是全球健康面临的重大挑战,促使人们不断研究发现创新的抗真菌药物。110 kDa 热休克蛋白(Hsp110s)是真核生物维持细胞蛋白质平衡所必需的分子伴侣。真菌 Hsp110s 已成为创新抗真菌策略的一个有前途的靶标。值得注意的是,2H 是针对 Hsp110s 和抗真菌感染的一个有前途的候选靶标。我们的研究发现,2H 具有广谱抗真菌活性,能有效破坏白色念珠菌 Hsp110 的体外伴侣活性,抑制新生隐球菌的生长。药代动力学分析表明,与静脉给药相比,口服 2H 可提高疗效,这强调了优化 AUC/MIC 比值对推进其临床治疗的重要性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Characterization of a New Hsp110 Inhibitor as a Potential Antifungal.

Fungal infections present a significant global health challenge, prompting ongoing research to discover innovative antifungal agents. The 110 kDa heat shock proteins (Hsp110s) are molecular chaperones essential for maintaining cellular protein homeostasis in eukaryotes. Fungal Hsp110s have emerged as a promising target for innovative antifungal strategies. Notably, 2H stands out as a promising candidate in the endeavor to target Hsp110s and combat fungal infections. Our study reveals that 2H exhibits broad-spectrum antifungal activity, effectively disrupting the in vitro chaperone activity of Hsp110 from Candida auris and inhibiting the growth of Cryptococcus neoformans. Pharmacokinetic analysis indicates that oral administration of 2H may offer enhanced efficacy compared to intravenous delivery, emphasizing the importance of optimizing the AUC/MIC ratio for advancing its clinical therapy.

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来源期刊
Journal of Fungi
Journal of Fungi Medicine-Microbiology (medical)
CiteScore
6.70
自引率
14.90%
发文量
1151
审稿时长
11 weeks
期刊介绍: Journal of Fungi (ISSN 2309-608X) is an international, peer-reviewed scientific open access journal that provides an advanced forum for studies related to pathogenic fungi, fungal biology, and all other aspects of fungal research. The journal publishes reviews, regular research papers, and communications in quarterly issues. Our aim is to encourage scientists to publish their experimental and theoretical results in as much detail as possible. Therefore, there is no restriction on paper length. Full experimental details must be provided so that the results can be reproduced.
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