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dc.contributor.authorAlsuri, Maruthi Ram
dc.contributor.authorBower, Benjamin D.
dc.contributor.authorBurns, Dennis H.
dc.contributor.authorFraire, Guadalupe
dc.contributor.authorSeelam, Bhusi R.
dc.contributor.authorShaban, Rima
dc.contributor.authorShaban, Sara
dc.contributor.authorSchneegurt, Mark A.
dc.identifier.citationAlsuri, M., Bower, B.D., Burns, D.H. et al. The broad antibacterial activity of a small synthetic receptor for cellular phosphatidylglycerol lipids. Folia Microbiol (2023).
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dc.description.abstractA small receptor molecule composed of a porphyrin core with tetrakis-ammonium glycine pickets (liptin 3e) appears to target anionic phosphatidylglycerol (PG) lipid head groups through multifunctional binding-pocket complementarity. Although a major component of bacterial cell membranes, PG is not widely found in animal cells, making PG potentially selective for bacterial targeting. Growth of microbial isolates was monitored in liquid cultures treated with liptin 3e by dilution plate counts and turbidity. Inhibition of growth by liptin 3e was observed for the ESKAPE human pathogens (Enterobacter aerogenes, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterococcus faecium), Escherichia coli, Mycobacterium smegmatis, Streptococcus sobrinus, and methicillin-resistant S. aureus (MRSA), with certain species suppressed at <1 ?g/mL (sub-?M) concentrations. Prolonged lag phases were observed, although cell viability was mainly unaffected, suggesting that liptin treatment caused bacteriostasis. Cultures treated with liptin 3e eventually recovered, resumed growth, and reached the same final densities as untreated cultures. Growth of the fungus Candida albicans was not appreciably inhibited by liptin 3e. If liptins exhibit bacteriostasis through broad extracellular binding to PG head groups, thereby disrupting cellular processes, liptins may be considered for development into preclinical drug candidates or be useful as a targeting system for molecular beacons or antibacterial drugs.
dc.description.sponsorshipThe experimental work was supported by awards from Kansas Institutional Development Award (IDeA) Networks of Biomedical Research Excellence (KINBRE) of the National Institute of General Medical Sciences (NIGMS) of the National Institutes of Health (NIH) (P20 GM103418) and from WSU.
dc.publisherSpringer Link
dc.relation.ispartofseriesFolia Microbiologica
dc.titleThe broad antibacterial activity of a small synthetic receptor for cellular phosphatidylglycerol lipids
dc.rights.holder© Institute of Microbiology, Academy of Sciences of the Czech Republic, v.v.i. 2023

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