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ZHU Zhixi, ZHANG Jielin, CHEN Yijun. Recent advances in research on chelators as metallo-β-lactamase inhibitors[J]. Journal of China Pharmaceutical University, 2022, 53(4): 410-422. DOI: 10.11665/j.issn.1000-5048.20220404
Citation: ZHU Zhixi, ZHANG Jielin, CHEN Yijun. Recent advances in research on chelators as metallo-β-lactamase inhibitors[J]. Journal of China Pharmaceutical University, 2022, 53(4): 410-422. DOI: 10.11665/j.issn.1000-5048.20220404
shu

Recent advances in research on chelators as metallo-β-lactamase inhibitors

  • School of Life Science and Technology, China Pharmaceutical University, Nanjing 211198, China

Funds: This study was supported by the National Natural Science Foundation of China (No.82003627) and the Natural Science Foundation of Jiangsu Province (No.BK20200565)
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  • Received Date: January 27, 2022
  • Revised Date: May 22, 2022
    Graphical Abstract
    • Abstract
  • The major reason for the resistance of Gram-negative bacteria to β-lactam antibiotics is the expression of β-lactamases.Metallo-β-lactamases (MBL) hydrolyze almost all types of β-lactam antibiotics including carbapenems, posing a challenge to global public health. Developing MBL inhibitors is an important method to treat the infections caused by resistant bacteria. As an important type of MBL inhibitors, chelating agents can inhibit MBL by chelating, stripping, and binding Zn2+ in the active center of MBL.This review summarizes recent publications on chelators as MBL inhibitors, discussing their chemical structures, inhibitory potency, synergistic effects with antibiotics, selectivity and mechanism of action, including EDTA and related compounds, aspergillomarasmine A (AMA) and its derivatives, NOTA and related compounds, pyridine carboxylic acid and pyridine methylamine compounds, aiming to provide reference for future development of potent, selective and safe clinical MBL inhibitors.
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    • References (61)
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