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结核分枝杆菌 FosM 耐药酶的小分子抑制剂。

Small molecule inhibitors of the fosfomycin resistance enzyme FosM from Mycobacterium abscessus.

机构信息

Department of Chemistry & Biochemistry, The University of Alabama, 250 Hackberry Lane, Tuscaloosa, AL 35487, United States of America.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 South Limestone St., Lexington, KY 40536, United States of America.

出版信息

Biochim Biophys Acta Gen Subj. 2023 Oct;1867(10):130444. doi: 10.1016/j.bbagen.2023.130444. Epub 2023 Aug 12.

Abstract

Fosfomycin is a safe broad-spectrum antibiotic that has not achieved widespread use because of the emergence of fosfomycin-modifying enzymes. Inhibition of fosfomycin-modifying enzymes could be used to help combat pathogens like Mycobacterium abscessus. Our previous work identified several inhibitors for the enzyme FosB from Staphylococcus aureus. We have tested those same compounds for inhibition of FosM, the fosfomycin-modifying enzyme from M. abscessus. The work described here will be used as the basis for more detailed studies into the inhibition of FosM.

摘要

磷霉素是一种安全的广谱抗生素,但由于磷霉素修饰酶的出现,尚未得到广泛应用。抑制磷霉素修饰酶可用于帮助对抗像脓肿分枝杆菌这样的病原体。我们之前的工作从金黄色葡萄球菌中鉴定出几种酶 FosB 的抑制剂。我们已经测试了这些相同的化合物对 M. abscessus 的磷霉素修饰酶 FosM 的抑制作用。这里描述的工作将作为更详细研究 FosM 抑制作用的基础。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/da6c/10727124/c3238456ab8c/nihms-1927970-f0001.jpg

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Small molecule inhibitors of the fosfomycin resistance enzyme FosM from Mycobacterium abscessus.结核分枝杆菌 FosM 耐药酶的小分子抑制剂。
Biochim Biophys Acta Gen Subj. 2023 Oct;1867(10):130444. doi: 10.1016/j.bbagen.2023.130444. Epub 2023 Aug 12.
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Nature. 2021 Aug;596(7873):583-589. doi: 10.1038/s41586-021-03819-2. Epub 2021 Jul 15.
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Non-tuberculous mycobacteria and the rise of Mycobacterium abscessus.非结核分枝杆菌与脓肿分枝杆菌的崛起。
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