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Article

Specific Inhibition of VanZ-Mediated Resistance to Lipoglycopeptide Antibiotics

by
Vishma Pratap Sur
1,†,
Aninda Mazumdar
2,†,
Vladimir Vimberg
2,†,
Tommaso Stefani
2,
Ladislav Androvic
3,
Lucie Kracikova
3,4,
Richard Laga
3,
Zdenek Kamenik
2 and
Katerina Komrskova
1,5,*
1
Laboratory of Reproductive Biology, Institute of Biotechnology of the Czech Academy of Sciences, BIOCEV, Prumyslova 595, 252 50 Vestec, Czech Republic
2
Laboratory for Biology of Secondary Metabolism, Institute of Microbiology of the Czech Academy of Sciences, Videnska 1083, 142 20 Prague, Czech Republic
3
Department of Polymer and Colloid Immunotherapeutics, Institute of Macromolecular Chemistry of the Czech Academy of Sciences, Heyrovskeho namesti 2, 162 06 Prague, Czech Republic
4
Department of Polymers, Faculty of Chemical Technology, University of Chemistry and Technology, Technicka 5, 166 28 Prague, Czech Republic
5
Department of Zoology, Faculty of Science, Charles University, Vinicna 7, 128 44 Prague, Czech Republic
*
Author to whom correspondence should be addressed.
†
These authors contributed equally to this work.
Int. J. Mol. Sci. 2022, 23(1), 97; https://doi.org/10.3390/ijms23010097
Submission received: 22 November 2021 / Revised: 17 December 2021 / Accepted: 19 December 2021 / Published: 22 December 2021
(This article belongs to the Special Issue New Antibacterial Agents)
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Abstract

Teicoplanin is a natural lipoglycopeptide antibiotic with a similar activity spectrum as vancomycin; however, it has with the added benefit to the patient of low cytotoxicity. Both teicoplanin and vancomycin antibiotics are actively used in medical practice in the prophylaxis and treatment of severe life-threatening infections caused by gram-positive bacteria, including methicillin-resistant Staphylococcus aureus, Enterococcus faecium and Clostridium difficile. The expression of vancomycin Z (vanZ), encoded either in the vancomycin A (vanA) glycopeptide antibiotic resistance gene cluster or in the genomes of E. faecium, as well as Streptococcus pneumoniae and C. difficile, was shown to specifically compromise the antibiotic efficiency through the inhibition of teicoplanin binding to the bacterial surface. However, the exact mechanisms of this action and protein structure remain unknown. In this study, the three-dimensional structure of VanZ from E. faecium EnGen0191 was predicted by using the I-TASSER web server. Based on the VanZ structure, a benzimidazole based ligand was predicted to bind to the VanZ by molecular docking. Importantly, this new ligand, named G3K, was further confirmed to specifically inhibit VanZ-mediated resistance to teicoplanin in vivo.
Keywords: antibiotic resistance; benzimidazole; docking; Enterococcus faecium; ligands; lipoglycopeptide antibiotic; MD simulation; Staphylococcus aureus; teicoplanin VanZ antibiotic resistance; benzimidazole; docking; Enterococcus faecium; ligands; lipoglycopeptide antibiotic; MD simulation; Staphylococcus aureus; teicoplanin VanZ

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MDPI and ACS Style

Sur, V.P.; Mazumdar, A.; Vimberg, V.; Stefani, T.; Androvic, L.; Kracikova, L.; Laga, R.; Kamenik, Z.; Komrskova, K. Specific Inhibition of VanZ-Mediated Resistance to Lipoglycopeptide Antibiotics. Int. J. Mol. Sci. 2022, 23, 97. https://doi.org/10.3390/ijms23010097

AMA Style

Sur VP, Mazumdar A, Vimberg V, Stefani T, Androvic L, Kracikova L, Laga R, Kamenik Z, Komrskova K. Specific Inhibition of VanZ-Mediated Resistance to Lipoglycopeptide Antibiotics. International Journal of Molecular Sciences. 2022; 23(1):97. https://doi.org/10.3390/ijms23010097

Chicago/Turabian Style

Sur, Vishma Pratap, Aninda Mazumdar, Vladimir Vimberg, Tommaso Stefani, Ladislav Androvic, Lucie Kracikova, Richard Laga, Zdenek Kamenik, and Katerina Komrskova. 2022. "Specific Inhibition of VanZ-Mediated Resistance to Lipoglycopeptide Antibiotics" International Journal of Molecular Sciences 23, no. 1: 97. https://doi.org/10.3390/ijms23010097

APA Style

Sur, V. P., Mazumdar, A., Vimberg, V., Stefani, T., Androvic, L., Kracikova, L., Laga, R., Kamenik, Z., & Komrskova, K. (2022). Specific Inhibition of VanZ-Mediated Resistance to Lipoglycopeptide Antibiotics. International Journal of Molecular Sciences, 23(1), 97. https://doi.org/10.3390/ijms23010097

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