Please use this identifier to cite or link to this item:
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
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

Files in This Item:
File Description SizeFormat 
A dual function antibiotic-transporter.pdf2.46 MBAdobe PDFThumbnail


Updated on Jan 23, 2021


Updated on Jan 21, 2021

Page view(s)

Updated on Jan 27, 2021

Download(s) 50

Updated on Jan 27, 2021

Google ScholarTM




Items in DR-NTU are protected by copyright, with all rights reserved, unless otherwise indicated.