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研究性真菌Cyp51抑制剂VT-1129对新型隐球菌和格特隐球菌具有强大的体外活性。

The Investigational Fungal Cyp51 Inhibitor VT-1129 Demonstrates Potent In Vitro Activity against Cryptococcus neoformans and Cryptococcus gattii.

作者信息

Lockhart Shawn R, Fothergill Annette W, Iqbal Naureen, Bolden Carol B, Grossman Nina T, Garvey Edward P, Brand Stephen R, Hoekstra William J, Schotzinger Robert J, Ottinger Elizabeth, Patterson Thomas F, Wiederhold Nathan P

机构信息

Mycotic Diseases Branch, Centers for Disease Control and Prevention, Atlanta, Georgia, USA.

University of Texas Health Science Center at San Antonio, San Antonio, Texas, USA.

出版信息

Antimicrob Agents Chemother. 2016 Mar 25;60(4):2528-31. doi: 10.1128/AAC.02770-15. Print 2016 Apr.

DOI:10.1128/AAC.02770-15
PMID:26787697
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4808209/
Abstract

Thein vitroactivities of the novel fungal Cyp51 inhibitor VT-1129 were evaluated against a large panel ofCryptococcus neoformansandCryptococcus gattiiisolates. VT-1129 demonstrated potent activities against bothCryptococcusspecies as demonstrated by low MIC50and MIC90values. ForC. gattii, thein vitropotency was maintained against all genotypes. In addition, significantly lower geometric mean MICs were observed for VT-1129 than for fluconazole againstC. neoformans, including isolates with reduced fluconazole susceptibility.

摘要

新型真菌Cyp51抑制剂VT-1129的体外活性针对大量新型隐球菌和格特隐球菌分离株进行了评估。VT-1129对这两种隐球菌均显示出强效活性，其MIC50和MIC90值较低即证明了这一点。对于格特隐球菌，其体外活性对所有基因型均保持有效。此外，观察到VT-1129针对新型隐球菌的几何平均MIC显著低于氟康唑，包括对氟康唑敏感性降低的分离株。

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本文引用的文献

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The clinical candidate VT-1161 is a highly potent inhibitor of Candida albicans CYP51 but fails to bind the human enzyme.临床候选药物VT-1161是白色念珠菌CYP51的高效抑制剂，但无法与人源酶结合。
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Design and optimization of highly-selective fungal CYP51 inhibitors.高选择性真菌CYP51抑制剂的设计与优化
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In vitro antifungal susceptibilities and amplified fragment length polymorphism genotyping of a worldwide collection of 350 clinical, veterinary, and environmental Cryptococcus gattii isolates.对全球范围内 350 株临床、兽医和环境分离的隐球菌的体外抗真菌药敏试验和扩增片段长度多态性基因分型研究。
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Cryptococcus.隐球菌。
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Antifungal susceptibility, serotyping, and genotyping of clinical Cryptococcus neoformans isolates collected during 18 years in a single institution in Madrid, Spain.西班牙马德里一家单家医疗机构 18 年间收集的临床新型隐球菌分离株的抗真菌药敏性、血清型和基因分型。
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Clinical practice guidelines for the management of cryptococcal disease: 2010 update by the infectious diseases society of america.《隐球菌病治疗指南：美国传染病学会 2010 年更新版》
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