快速高通量分析鉴定吉西他滨及其衍生物是抗多重耐药金黄色葡萄球菌的有效抑制剂。

IF 1.6 4区医学 Q4 BIOCHEMICAL RESEARCH METHODS

Assay and drug development technologies Pub Date : 2022-05-01 DOI:10.1089/adt.2022.034

Zhao Chen, Jinxiu Li, Yue Wan, Ruisong Bai, Wenjuan Wang, Xuan Gao, Di Li, Qingfeng Hu, Yong Li, Benfang Helen Ruan

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引用次数: 0

摘要

耐甲氧西林金黄色葡萄球菌(MRSA)是具有挑战性的致病菌，可引起严重感染，导致高死亡率。我们发现临床分离的耐氧西林和头孢西林金黄色葡萄球菌均表现出多重耐药(MDR)特征。通过化合物文库的快速高通量筛选(HTS)，发现吉西他滨和6个化合物能有效抑制金黄色葡萄球菌的生长。为了进一步改进，我们合成了含硒的吉西他滨，它在体外对几种MDR MRSA表现出相对有效的抗菌活性。HTS试验和吉西他滨selen衍生物为探索治疗MDR MRSA的有效分子靶点提供了有用的工具。

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Rapid High-Throughput Assay Identified Gemcitabine and Derivatives As Potent Inhibitors Against Multidrug-Resistant Staphylococcus aureus.

Methicillin-resistant Staphylococcus aureus (MRSA) are challenging pathogenic bacteria that can cause severe infection leading to high mortality rates. We found that both the oxacillin- and cefoxitin-resistant S. aureus strains isolated from clinic showed multidrug-resistant (MDR) characteristics. Through rapid high-throughput screen (HTS) of a compound library, gemcitabine and selen compounds were found to effectively inhibit S. aureus growth. For further improvement, we synthesized selen-containing gemcitabine that demonstrated relatively potent antimicrobial activity against several MDR MRSA in vitro. The HTS assay and gemcitabine selen derivative provided a useful tool to explore an effective molecular target to treat MDR MRSA.

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来源期刊

Assay and drug development technologies 医学-生化研究方法

CiteScore

3.60

自引率

0.00%

发文量

审稿时长

>12 weeks

期刊介绍： ASSAY and Drug Development Technologies provides access to novel techniques and robust tools that enable critical advances in early-stage screening. This research published in the Journal leads to important therapeutics and platforms for drug discovery and development. This reputable peer-reviewed journal features original papers application-oriented technology reviews, topical issues on novel and burgeoning areas of research, and reports in methodology and technology application. ASSAY and Drug Development Technologies coverage includes: -Assay design, target development, and high-throughput technologies- Hit to Lead optimization and medicinal chemistry through preclinical candidate selection- Lab automation, sample management, bioinformatics, data mining, virtual screening, and data analysis- Approaches to assays configured for gene families, inherited, and infectious diseases- Assays and strategies for adapting model organisms to drug discovery- The use of stem cells as models of disease- Translation of phenotypic outputs to target identification- Exploration and mechanistic studies of the technical basis for assay and screening artifacts