Kontou Maria, Pournaras Spyros, Kristo Ioulia, Ikonomidis Alexandros, Maniatis Antonios N, Stathopoulos Constantinos
Department of Biochemistry and Biotechnology, University of Thessaly, 26 Ploutonos st., 41221 Larissa, Greece.
Biochemistry. 2007 Nov 13;46(45):13170-8. doi: 10.1021/bi701258w. Epub 2007 Oct 18.
Metallo-beta-lactamases (MBLs) are considered an emerging family of Zn2+-dependent enzymes that significantly contribute to the resistance of many nosocomial pathogens against beta-lactam antimicrobials. Since these plasmid-encoded enzymes constitute specific molecular targets for beta-lactams, their exact mode of action is greatly important in deploying efficient anti-infective treatments and for the control of severe multi-resistant nosocomial infections, which becomes a global problem. A novel hybrid VIM-1/VIM-2-type beta-lactamase (named VIM-12) has recently been identified in a clinical isolate of Klebsiella pneumoniae in Greece. The sequence of this enzyme is highly similar with that of VIM-1 at its N-terminal region and with that of VIM-2 at its C-terminal region, raising the question of whether this sequence similarity reflects also a similar functional role. Moreover, the possible contribution of this novel beta-lactamase to the overall antibiotic resistance of this specific clinical isolate was investigated. The gene encoding VIM-12 was cloned and expressed, and the recombinant enzyme was used for detailed kinetic analysis, using a variety of beta-lactam antibiotics. VIM-12 was found to exhibit narrow substrate specificity, compared to other known beta-lactamases, limited mainly to penicillin and to a much lesser extent to imipenen. Interestingly, meropenem was found to act as a noncompetitive inhibitor of the enzyme, although the active site of VIM-12 exhibited complete conservation of residues among VIM enzymes. We conclude that VIM-12 represents a novel and unique member of the family of known metallo-beta-lactamases, exhibiting atypical substrate specificity.
金属β-内酰胺酶(MBLs)被认为是一类新出现的锌离子依赖性酶,它们在许多医院病原体对β-内酰胺类抗菌药物的耐药性中起重要作用。由于这些质粒编码的酶构成了β-内酰胺类药物的特定分子靶点,其确切作用模式对于开展有效的抗感染治疗以及控制严重的多重耐药医院感染极为重要,而这已成为一个全球性问题。最近在希腊一株肺炎克雷伯菌临床分离株中鉴定出一种新型杂合VIM-1/VIM-2型β-内酰胺酶(命名为VIM-12)。该酶的序列在其N端区域与VIM-1高度相似,在C端区域与VIM-2高度相似,这就引发了一个问题,即这种序列相似性是否也反映了相似的功能作用。此外,还研究了这种新型β-内酰胺酶对该特定临床分离株总体抗生素耐药性的可能贡献。克隆并表达了编码VIM-12的基因,使用多种β-内酰胺类抗生素对重组酶进行了详细的动力学分析。结果发现,与其他已知的β-内酰胺酶相比,VIM-12具有较窄的底物特异性,主要限于青霉素,对亚胺培南的作用程度要小得多。有趣的是,虽然VIM-12的活性位点在VIM酶之间表现出残基的完全保守,但美罗培南被发现是该酶的非竞争性抑制剂。我们得出结论,VIM-12代表了已知金属β-内酰胺酶家族中的一个新颖独特的成员,具有非典型的底物特异性。