Metallo-β-lactamases (MBLs) are an emerging class of antimicrobial resistance enzymes that degrade β-lactam antibiotics, including last-resort carbapenems. Infections caused by carbapenemase-producing Enterobacteriaceae (CPE) are increasingly prevalent, but treatment options are limited. While several serine-dependent β-lactamase inhibitors are formulated with commonly prescribed β-lactams, no MBL inhibitors are currently approved for combinatorial therapies. New compounds that target MBLs to restore carbapenem activity against CPE are therefore urgently needed. Herein we identified and characterized novel synthetic peptide inhibitors that bound to and inhibited NDM-1, which is an emerging β-lactam resistance mechanism in CPE.

中文翻译：

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新德里金属-β-内酰胺酶-1 抑制剂肽的发现和表征，可增强美罗培南依赖性杀死产碳青霉烯酶的肠杆菌科细菌。

金属-β-内酰胺酶 (MBL) 是一类新兴的抗微生物酶，可降解 β-内酰胺类抗生素，包括最后的碳青霉烯类抗生素。由产碳青霉烯酶肠杆菌科 (CPE) 引起的感染越来越普遍，但治疗选择有限。虽然几种丝氨酸依赖性 β-内酰胺酶抑制剂与常用的 β-内酰胺类药物一起配制，但目前尚无 MBL 抑制剂被批准用于组合疗​​法。因此，迫切需要靶向 MBL 以恢复碳青霉烯类抗 CPE 活性的新化合物。在此，我们鉴定并表征了结合并抑制 NDM-1 的新型合成肽抑制剂，NDM-1 是 CPE 中一种新兴的 β-内酰胺耐药机制。