Synthesis and Characterization of Dual-Sensitive PAMAM Derivatives Conjugated with Enzyme Cleavable Peptides as Gene Carriers

Lee, Jeil; Park, Seunghye; Kwon, Yong-Eun; Oh, Eugeney; Kim, Dong Ho; Guim, Hwanuk; Yeon, Jehyeong; Kim, Jin-Cheol; Choi, Ji Soo

doi:10.1007/s13233-021-9078-4

Cited by 2 publications

(4 citation statements)

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“…In addition, the primary amines of Lys and terminal ends of the peptides contribute to the positive charge of the micelles. A combination of basic amino acids with hydrophobic amino acids is also a general approach for designing antibacterial polymers [ 43 , 44 , 45 ].…”

Section: Discussionmentioning

confidence: 99%

“…Membrane penetration was demonstrated using NPN [ 43 ]. Both the Gram-negative E. coli and Gram-positive S. aureus cells treated with FKFL-G2 exhibited the highest fluorescence.…”

Section: Discussionmentioning

confidence: 99%

“…The degradation of germs in the macrophage was aided by active cathepsins, such as cathepsin B, which served as a proteolytic or lipolytic agent [ 36 ]. Cathepsin B-sensitive peptides have been used to deliver anticancer genes or medications [ 39 , 40 , 41 , 42 , 43 ]. Among them, the Phe-Lys-Phe-Leu (FKFL) sequence was selected in this study as a potential AMP derivative when it was introduced multivalently at the peripheral ends of the PAMAM dendrimer [ 43 ].…”

Section: Introductionmentioning

confidence: 99%

“…Cathepsin B-sensitive peptides have been used to deliver anticancer genes or medications [ 39 , 40 , 41 , 42 , 43 ]. Among them, the Phe-Lys-Phe-Leu (FKFL) sequence was selected in this study as a potential AMP derivative when it was introduced multivalently at the peripheral ends of the PAMAM dendrimer [ 43 ]. Lysine’s cationic property makes it easier for the peptide to bind to the cell membrane [ 44 ].…”

Section: Introductionmentioning

confidence: 99%

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Conjugation of Short Oligopeptides to a Second-Generation Polyamidoamine Dendrimer Shows Antibacterial Activity

et al. 2023

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The growing evolution of bacterial resistance to antibiotics represents a global issue that not only impacts healthcare systems but also political and economic processes. This necessitates the development of novel antibacterial agents. Antimicrobial peptides have shown promise in this regard. Thus, in this study, a new functional polymer was synthesized by joining a short oligopeptide sequence (Phe-Lys-Phe-Leu, FKFL) to the surface of a second-generation polyamidoamine (G2 PAMAM) dendrimer as an antibacterial component. This method of synthesis proved simple and resulted in a high conjugation yield of the product FKFL-G2. To determine its antibacterial potential, FKFL-G2 was subsequently analyzed via mass spectrometry, a cytotoxicity assay, bacterial growth assay, colony-forming unit assay, membrane permeabilization assay, transmission electron microscopy, and biofilm formation assay. FKFL-G2 was found to exhibit low toxicity to noncancerous NIH3T3 cells. Additionally, FKFL-G2 had an antibacterial effect on Escherichia coli and Staphylococcus aureus strains by interacting with and disrupting the bacterial cell membrane. Based on these findings, FKFL-G2 shows promise as a potential antibacterial agent.

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Section: Discussionmentioning

confidence: 99%

“…Membrane penetration was demonstrated using NPN [ 43 ]. Both the Gram-negative E. coli and Gram-positive S. aureus cells treated with FKFL-G2 exhibited the highest fluorescence.…”

Section: Discussionmentioning

confidence: 99%