Journal article
Probing the penetration of antimicrobial polymyxin lipopeptides into gram-negative bacteria
ZZ Deris, JD Swarbrick, KD Roberts, MAK Azad, J Akter, AS Horne, RL Nation, KL Rogers, PE Thompson, T Velkov, J Li
Bioconjugate Chemistry | AMER CHEMICAL SOC | Published : 2014
DOI: 10.1021/bc500094d
Abstract
The dry antibiotic development pipeline coupled with the emergence of multidrug resistant Gram-negative â€̃superbugs has driven the revival of the polymyxin lipopeptide antibiotics. Polymyxin resistance implies a total lack of antibiotics for the treatment of life-threatening infections. The lack of molecular imaging probes that possess native polymyxin-like antibacterial activity is a barrier to understanding the resistance mechanisms and the development of a new generation of polymyxin lipopeptides. Here we report the regioselective modification of the polymyxin B core scaffold at the N-terminus with the dansyl fluorophore to generate an active probe that mimics polymyxin B pharmacological..
View full abstractGrants
Awarded by National Institute of Allergy and Infectious Diseases
Funding Acknowledgements
J.L., T.V., R.L.N., P.E.T., and K.D.R. are supported by a research grant from the National Institute of Allergy and Infectious Diseases of the National Institutes of Health (R01AI098771). J.L., TV., R.L.N., and P.E.T. are also supported by the Australian National Health and Medical Research Council (NHMRC). The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Institute of Allergy and Infectious Diseases or the National Institutes of Health. J.L. is an Australian NHMRC Senior Research Fellow. T.V. is an Australian NHMRC Industry Career Development Level 1 Research Fellow.