Title:The Development of New Small-Molecule Inhibitors Targeting Bacterial Metallo-β-lactamases
Volume: 18
Issue: 10
Author(s): Ping Wang, Jing Cheng, Cong-Cong Liu, Kai Tang, Feng Xu, Zhiqiang Yu, Bin Yu*Junbiao Chang*
Affiliation:
- Co-Innovation Center of Henan Province for New Drug R & D and Preclinical Safety, Zhengzhou 450001,China
- Co-Innovation Center of Henan Province for New Drug R & D and Preclinical Safety, Zhengzhou 450001,China
Keywords:
Metallo-β-lactamases, thiol derivatives, dicarboxylic acid derivatives, cyclic Boronates, triazoles, natural products,
peptide inhibitors.
Abstract: Metallo-β-lactamases (MBLs) are a family of Zn(II)-dependent enzymes that can hydrolyze
almost all β-lactam antibiotics. Horizontal transfer of the genes encoding MBLs among Gram-negative
bacteria pathogens has led to the emergence of extensively drug-resistant pathogens, which now represent
a major threat to human health. As there is not to date yet a clinically available MBL inhibitor, the
discovery of new MBL inhibitors has great urgency. This review highlights the recent developments in
the discovery of small-molecule MBL inhibitors.
