In Vitro Screening of an FDA-Approved Library Against ESKAPE Pathogens.
In Vitro Screening of an FDA-Approved Library Against ESKAPE Pathogens.
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DOI：
10.2174/1381612823666170209154745
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发表时间：
2017
影响因子：
3.1
通讯作者：
Seleem MN
中科院分区：
文献类型：
--
作者：
Younis W;AbdelKhalek A;Mayhoub AS;Seleem MN
细菌对常规抗生素的耐药性是全球公共健康日益严重的威胁，需要立即探索和开发新的抗菌化合物。药物再利用是一种廉价和尚未开发的新的抗菌药物的来源，它具有许多吸引人的特征，值得进一步关注抗菌药物的发现。为了改变药物的用途并探索抗菌药物发现领域的新线索，我们对1600种美国食品和药物管理局(FDA)批准的针对屎肠球菌、金黄色葡萄球菌、肺炎克雷伯菌、鲍曼不动杆菌、铜绿假单胞菌和阴沟肠杆菌(ESKAPE)的药物进行了全细胞筛选试验。体外筛选确定了49种非抗菌药，它们对至少一种ESKAPE病原体有活性。尽管其中一些药物已知具有抗菌活性，但许多以前从未报道过。特别是含磺酰胺的结构代表了一种值得进一步研究的新型药物支架。这些药物作为抗菌剂的特点可能为目前治疗细菌感染的方法提供安全、有效和快速的补充。
Bacterial resistance to conventional antibiotics is an increasingly serious threat to public health worldwide that requires immediate exploration and the development of novel antimicrobial compounds. Drug repurposing is an inexpensive and untapped source of new antimicrobial leads, and it holds many attractive features warranting further attention for antimicrobial drug discovery. In an effort to repurpose drugs and explore new leads in the field of antimicrobial drug discovery, we performed a whole-cell screening assay of 1,600 Food and Drug Administration (FDA) approved drugs against Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacter cloacae (ESKAPE) pathogens. The in vitro screening identified 49 non-antimicrobial drugs that were active against at least one species of ESKAPE pathogen. Although some of these drugs were known to have antibacterial activity, many have never been reported before. In particular, sulfonamide-containing structures represent a novel drug scaffold that should be investigated further. The characteristics of these drugs as antimicrobial agents may offer a safe, effective, and quick supplement to current approaches to treating bacterial infections.
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影响因子：
7.3
作者：
Perlmutter JI;Forbes LT;Krysan DJ;Ebsworth-Mojica K;Colquhoun JM;Wang JL;Dunman PM;Flaherty DP
通讯作者：
Flaherty DP
影响因子：
3.1
作者：
Thangamani S;Mohammad H;Younis W;Seleem MN
通讯作者：
Seleem MN
影响因子：
8.8
作者：
Fordy, C;Glover, C;Allen-Mersh, TG
通讯作者：
Allen-Mersh, TG
影响因子：
7.3
作者：
Gordon, Christopher P.;Williams, Paul;Chan, Weng C.
通讯作者：
Chan, Weng C.
重新利用Ebselen治疗多药抗性葡萄球菌感染。
影响因子：
4.6
作者：
Thangamani S;Younis W;Seleem MN
通讯作者：
Seleem MN