Journal
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 57, Issue 28, Pages 8483-8487Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201802837
Keywords
antimicrobial agents; chemical space; dendrimers; peptides; virtual screening
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Funding
- Swiss National Science Foundation [200020159941, IZLCZ2155982, 407240167048]
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We used nearest-neighbor searches in chemical space to improve the activity of the antimicrobial peptide dendrimer (AMPD) G3KL and identified dendrimer T7, which has an expanded activity range against Gram-negative pathogenic bacteria including Klebsiellae pneumoniae, increased serum stability, and promising activity in an invivo infection model against a multidrug-resistant strain of Acinetobacter baumannii. Imaging, spectroscopic studies, and a structural model from molecular dynamics simulations suggest that T7 acts through membrane disruption. These experiments provide the first example of using virtual screening in the field of dendrimers and show that dendrimer size does not limit the activity of AMPDs.
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