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Title: A dual-function antibiotic-transporter conjugate exhibits superior activity in sterilizing MRSA biofilms and killing persister cells
Authors: Antonoplis, Alexandra
Zang, Xiaoyu
Huttner, Melanie A.
Chong, Kelvin Kian Long
Lee, Yu B.
Co, Julia Y.
Amieva, Manuel R.
Kline, Kimberly A.
Wender, Paul A.
Cegelski, Lynette
Keywords: Science::Biological sciences
Issue Date: 2018
Source: Antonoplis, A., Zang, X., Huttner, M. A., Chong, K. K. L., Lee, Y. B., Co, J. Y., . . . Cegelski, L. (2018). A dual-function antibiotic-transporter conjugate exhibits superior activity in sterilizing MRSA biofilms and killing persister cells. Journal of the American Chemical Society, 140(47), 16140-16151. doi:10.1021/jacs.8b08711
Journal: Journal of the American Chemical Society
Abstract: New strategies are urgently needed to target MRSA, a major global health problem and the leading cause of mortality from antibiotic-resistant infections in many countries. Here, we report a general approach to this problem exemplified by the design and synthesis of a vancomycin-d-octaarginine conjugate (V-r8) and investigation of its efficacy in addressing antibiotic-insensitive bacterial populations. V-r8 eradicated MRSA biofilm and persister cells in vitro, outperforming vancomycin by orders of magnitude. It also eliminated 97% of biofilm-associated MRSA in a murine wound infection model and displayed no acute dermal toxicity. This new dual-function conjugate displays enhanced cellular accumulation and membrane perturbation as compared to vancomycin. Based on its rapid and potent activity against biofilm and persister cells, V-r8 is a promising agent against clinical MRSA infections.
ISSN: 0002-7863
DOI: 10.1021/jacs.8b08711
Schools: School of Biological Sciences 
Interdisciplinary Graduate School (IGS) 
Research Centres: Singapore Centre for Environmental Life Sciences and Engineering 
Rights: This document is the Accepted Manuscript version of a Published Work that appeared in final form in Journal of the American Chemical Society, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see
Fulltext Permission: open
Fulltext Availability: With Fulltext
Appears in Collections:SCELSE Journal Articles

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