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Polymers 2017, 9(6), 224; doi:10.3390/polym9060224

Polyamidoamine (PAMAM) Dendrimers Modified with Cathepsin-B Cleavable Oligopeptides for Enhanced Gene Delivery

Department of Biochemistry, Chungnam National University, Daejeon 305-764, Korea
Hazards Monitoring BNT Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB), 125 Gwahak-ro, Yuseong-gu, Daejeon 34141, Korea
Graduate School of Analytical Science and Technology, Chungnam National University, Daejeon 34134, Korea
Department of Nanobiotechnology, KRIBB School of Biotechnology, Korea University of Science and Technology (UST), 217 Gajeong-ro, Yuseong-gu, Daejeon 34113, Korea
Authors to whom correspondence should be addressed.
Academic Editor: Ravin Narain
Received: 15 March 2017 / Revised: 4 June 2017 / Accepted: 12 June 2017 / Published: 14 June 2017
(This article belongs to the Special Issue Polymers and Nanogels for Gene Therapy)
View Full-Text   |   Download PDF [4002 KB, uploaded 14 June 2017]   |  


Because of the complex mechanisms mediating cancer onset, prognosis, and metastatic behavior, different therapeutic approaches targeting these mechanisms have been investigated. Recent advancements in nanocarrier-based drug and gene delivery methods have encouraged scientific groups to investigate various novel therapeutic techniques. In this study, a poly(amidoamine) (PAMAM) polymer-based gene carrier containing the cathepsin B-enzyme sensitive sequence (glycine-phenylalanine-leucine-glycine, GFLG) was evaluated to determine transfection efficiency. Following the GFLG sequence, the surface of PAMAM generation 4 (G4) was conjugated with histidine (H) and arginine (R) for improved endosomal escape and cellular uptake, respectively. The successful synthesis of G4-GLFG-H-R was confirmed by 1H-nuclear magnetic resonance spectroscopy. The polyplex composed of G4-GLFG-H-R and pDNA was simulated by the enzyme cathepsin B and induced endosomal escape of pDNA, which was confirmed by gel electrophoresis. Compared with the G4 control, enzyme-sensitive G4-GLFG-H-R showed higher transfection efficiency and lower cytotoxicity in HeLa cells. These results demonstrated that G4-GLFG-H-R may be a highly potent and efficient carrier for gene therapy applications. View Full-Text
Keywords: gene delivery; polyplex; poly(amidoamine) dendrimer; GFLG peptide; cathepsin B; histidine; arginine gene delivery; polyplex; poly(amidoamine) dendrimer; GFLG peptide; cathepsin B; histidine; arginine

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Lee, S.; Son, S.J.; Song, S.J.; Ha, T.H.; Choi, J.S. Polyamidoamine (PAMAM) Dendrimers Modified with Cathepsin-B Cleavable Oligopeptides for Enhanced Gene Delivery. Polymers 2017, 9, 224.

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