The effect of lipidation and glycosylation on short cationic antimicrobial peptides

Biochimica Et Biophysica Acta. Biomembranes
Elizabeth GrimseyKai Hilpert

Abstract

The global health threat surrounding bacterial resistance has resulted in antibiotic researchers shifting their focus away from 'traditional' antibiotics and concentrating on other antimicrobial agents, including antimicrobial peptides. These low molecular weight proteins exhibit broad-spectrum activity against bacteria, including multi-drug resistant strains, viruses, fungi and protozoa and constitute a major element of the innate-immune system of many multicellular organisms. Some naturally occurring antimicrobial peptides are lipidated and/or glycosylated and almost all antimicrobial peptides in clinical use are either lipopeptides (Daptomycin and Polymyxin E and B) or glycopeptides (Vancomycin). Lipidation, glycosylation and PEGylation are an option for improving stability and activity in serum and for reducing the rapid clearing via the kidneys and liver. Two broad-spectrum antimicrobial peptides NH2-RIRIRWIIR-CONH2 (A1) and NH2-KRRVRWIIW-CONH2 (B1) were conjugated via a linker, producing A2 and B2, to individual fatty acids of C8, C10, C12 and C14 and in addition, A2 was conjugated to either glucose, N-acetyl glucosamine, galactose, mannose, lactose or polyethylene glycol (PEG). Antimicrobial activity against two Gram-pos...Continue Reading

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Citations

Sep 23, 2020·Journal of Enzyme Inhibition and Medicinal Chemistry·Rosa BellavitaStefania Galdieroa
Jan 11, 2021·European Journal of Medicinal Chemistry·Chao ZhongJingman Ni
Dec 20, 2020·Colloids and Surfaces. B, Biointerfaces·Tahereh Seifi, Ali Reza Kamali
Dec 24, 2020·International Journal of Molecular Sciences·Taylor Rounds, Suzana K Straus
Aug 8, 2021·International Journal of Molecular Sciences·Federica ArmasMarco Scocchi
Aug 10, 2020·Toxicon : Official Journal of the International Society on Toxinology·Zhongjie LiYong Wang
Oct 16, 2021·Chemical Communications : Chem Comm·Samilla B RezendeMarlon H Cardoso

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