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Synthesis and Kinetic evaluation of an azido analogue of methylerythritol phosphate: a Novel Inhibitor of E. coli YgbP/IspD.
Scientific Reports ( IF 3.8 ) Pub Date : 2018-12-17 , DOI: 10.1038/s41598-018-35586-y Zoljargal Baatarkhuu 1, 2 , Philippe Chaignon 2 , Franck Borel 3 , Jean-Luc Ferrer 3 , Alain Wagner 1 , Myriam Seemann 2
Scientific Reports ( IF 3.8 ) Pub Date : 2018-12-17 , DOI: 10.1038/s41598-018-35586-y Zoljargal Baatarkhuu 1, 2 , Philippe Chaignon 2 , Franck Borel 3 , Jean-Luc Ferrer 3 , Alain Wagner 1 , Myriam Seemann 2
Affiliation
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As multidrug resistant pathogenic microorganisms are a serious health menace, it is crucial to continuously develop novel medicines in order to overcome the emerging resistance. The methylerythritol phosphate pathway (MEP) is an ideal target for antimicrobial development as it is absent in humans but present in most bacteria and in the parasite Plasmodium falciparum. Here, we report the synthesis and the steady-state kinetics of a novel potent inhibitor (MEPN3) of Escherichia coli YgbP/IspD, the third enzyme of the MEP pathway. MEPN3 inhibits E. coli YgbP/IspD in mixed type mode regarding both substrates. Interestingly, MEPN3 shows the highest inhibitory activity when compared to known inhibitors of E. coli YgbP/IspD. The mechanism of this enzyme was also studied by steady-state kinetic analysis and it was found that the substrates add to the enzyme in sequential manner.
中文翻译：
甲基赤藓糖醇磷酸叠氮基类似物的合成和动力学评估：一种新型的大肠杆菌YgbP / IspD抑制剂。
由于多药耐药的病原微生物是严重的健康威胁，因此不断开发新药以克服新出现的耐药性至关重要。甲基赤藓糖醇磷酸途径（MEP）是抗微生物发展的理想目标，因为它在人类中不存在，但在大多数细菌和寄生虫恶性疟原虫中都存在。在这里，我们报告了一种新型的强效抑制剂（MEPN3），它是大肠杆菌YgbP / IspD（MEP途径的第三种酶）的合成和稳态动力学。关于两种底物，MEPN3以混合型模式抑制大肠杆菌YgbP / IspD。有趣的是，与已知的大肠杆菌YgbP / IspD抑制剂相比，MEPN3表现出最高的抑制活性。
更新日期：2018-12-17
中文翻译：
甲基赤藓糖醇磷酸叠氮基类似物的合成和动力学评估：一种新型的大肠杆菌YgbP / IspD抑制剂。
由于多药耐药的病原微生物是严重的健康威胁，因此不断开发新药以克服新出现的耐药性至关重要。甲基赤藓糖醇磷酸途径（MEP）是抗微生物发展的理想目标，因为它在人类中不存在，但在大多数细菌和寄生虫恶性疟原虫中都存在。在这里，我们报告了一种新型的强效抑制剂（MEPN3），它是大肠杆菌YgbP / IspD（MEP途径的第三种酶）的合成和稳态动力学。关于两种底物，MEPN3以混合型模式抑制大肠杆菌YgbP / IspD。有趣的是，与已知的大肠杆菌YgbP / IspD抑制剂相比，MEPN3表现出最高的抑制活性。
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