title: β-Lactamase inhibitors: an update.
abstract: 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 inhibitor discovery.
authors.affiliation: School of Life Science and Technology, China Pharmaceutical University, Nanjing 210009, P.R. China. zhengh18@hotmail.com.
authors.forename: Jiao
authors.initials: J
authors.lastname: Chen
authors.forename: Xiaohui
authors.initials: X
authors.lastname: Shang
authors.forename: Feng
authors.initials: F
authors.lastname: Hu
authors.forename: Xingzhen
authors.initials: X
authors.lastname: Lao
authors.forename: Xiangdong
authors.initials: X
authors.lastname: Gao
authors.forename: Heng
authors.initials: H
authors.lastname: Zheng
authors.forename: Wenbing
authors.initials: W
authors.lastname: Yao
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D055808:Drug Discovery; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008969:Molecular Sequence Data; D065093:beta-Lactamase Inhibitors; D001618:beta-Lactamases / Q000737:chemistry / Q000378:metabolism
chemical_list: D004791:Enzyme Inhibitors; D065093:beta-Lactamase Inhibitors; D001618:beta-Lactamases