β-Lactamase Inhibitors: An Update
Jiao Chen, Xiaohui Shang, Feng Hu, Xingzhen Lao, Xiangdong Gao, Heng Zheng and Wenbing Yao
Affiliation: School of Life Science and Technology, China Pharmaceutical University, Nanjing 210009, P.R. China.
β-lactamase-mediated resistance to β-lactam antibiotics is an increasing threat to clinical antimicrobial
chemotherapy. The combinations of β-lactam antibiotics and β-lactamase inhibitors (such as sulbactam, tazobactam and
clavulanic acid) have been successfully used for overcoming class A β-lactamase-mediated resistance. However, none of
the inhibitors effective against class B, C or D β-lactamases are available in the clinic, which alarms an urgent need to
discover/design broad-spectrum β-lactamase inhibitors or new β-lactam antibiotics capable of evading bacterial enzymatic
inactivation. In recent years, inhibitors targeted to serine β-lactamases have been developed rapidly with a few of them
under clinical trials. In contrast, none promising class B β-lactamase (metallo-β-lactamase) inhibitors with good
druggability have been discovered, despite the increasing number of active molecules reported. In this review, we
summarized the potential β-lactamase inhibitors reported in recent years and updated the current status of β-lactamase
Keywords: Antibiotic resistance, β-lactam antibiotics, β-lactamases, inhibitors, broad spectrum, drug discovery.
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