Targeting Intracellular Pathogenic Bacteria Through N-Terminal Modification of Cationic Amphiphilic Polyproline Helices

Intracellular pathogens can thrive within mammalian cells and are inaccessible to many antimicrobial agents. Herein, we present a facile method of enhancing the cell penetrating and antibacterial properties of cationic amphiphilic polyproline helices (CAPHs) with modifications to the hydrophobic moi...

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Veröffentlicht in:Journal of organic chemistry 2020-06, Vol.85 (11), p.7468-7475
Hauptverfasser: Dietsche, Thomas A, Eldesouky, Hassan E, Zeiders, Samantha M, Seleem, Mohamed N, Chmielewski, Jean
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container_end_page 7475
container_issue 11
container_start_page 7468
container_title Journal of organic chemistry
container_volume 85
creator Dietsche, Thomas A
Eldesouky, Hassan E
Zeiders, Samantha M
Seleem, Mohamed N
Chmielewski, Jean
description Intracellular pathogens can thrive within mammalian cells and are inaccessible to many antimicrobial agents. Herein, we present a facile method of enhancing the cell penetrating and antibacterial properties of cationic amphiphilic polyproline helices (CAPHs) with modifications to the hydrophobic moiety at the N-terminus. These altered CAPHs display superior cell penetration within macrophage cells, and in some cases, minimal cytotoxicity. Furthermore, one CAPH, exhibited excellent antibacterial activity against multiple strains of pathogenic bacteria and promoted the clearance of intracellular within macrophages.
doi_str_mv 10.1021/acs.joc.0c00871
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title Targeting Intracellular Pathogenic Bacteria Through N-Terminal Modification of Cationic Amphiphilic Polyproline Helices
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