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Peptide ligand‐mediated endocytosis of nanoparticles to cancer cells: Cell receptor‐binding‐ versus cell membrane‐penetrating peptides
Authors:Eunji Jo  June Seok Heo  Ja‐Yun Lim  Bo‐Ram Lee  Chul Joo Yoon  Jinkwan Kim  Jeewon Lee
Affiliation:1. Department of Chemical and Biological Engineering, College of Engineering, Korea University, Seoul, Republic of Korea;2. Department of Integrated Biomedical and Life Sciences, College of Health Science, Korea University, Seoul, Republic of Korea;3. Department of Biomedical Laboratory Science, College of Health Science, Jungwon University, Chung‐buk, Republic of Korea
Abstract:The endocytosis‐mediating performances of two types of peptide ligands, cell receptor binding peptide (CRBP) and cell membrane penetrating peptide (CMPP), were analyzed and compared using a common carrier of peptide ligands‐human ferritin heavy chain (hFTH) nanoparticle. Twenty‐four copies of a CMPP(human immunodeficiency virus‐derived TAT peptide) and/or a CRBP (peptide ligand with strong and specific affinity for either human integrin(αvβ3) or epidermal growth factor receptor I (EGFR) that is overexpressed on various cancer cells) were genetically presented on the surface of each hFTH nanopariticle. The quantitative level of endocytosis and intracellular localization of fluorescence dye‐labeled CRBP‐ and CMPP‐presenting nanoparticles were estimated in the in vitro cultures of integrin‐ and EGFR‐overexpressing cancer and human dermal fibroblast cells(control). From the cancer cell cultures treated with the CMPP‐ and CRBP‐presenting nanoparticles, it was notable that CRBPs resulted in quantitatively higher level of endocytosis than CMPP (TAT) and successfully transported the nanoparticles to the cytosol of cancer cells depending on concentration and treatment period of time, whereas TAT‐mediated endocytosis localized most of the nanoparticles within endosomal vesicles under the same conditions. These novel findings provide highly useful informations to many researchers both in academia and in industry who are interested in developing anticancer drug delivery systems/carriers.
Keywords:cancer targeting  cancer cell receptor‐binding peptide  cancer cell membrane‐penetrating peptide  peptide ligand‐mediated endocytosis  protein nanoparticle carrier
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