Cellular uptake on N- and C-termini conjugated FITC of Rath cell penetrating peptides and its consequences for gene-expression profiling in U-937 human macrophages and HeLa cervical cancer cells

doi:10.3109/1061186X.2013.824456

CNU IR > Pharmacy and Science > Dept. of Pharmacy > Periodical Articles > Item 310902800/27794

Please use this identifier to cite or link to this item: https://ir.cnu.edu.tw/handle/310902800/27794

Title:	Cellular uptake on N- and C-termini conjugated FITC of Rath cell penetrating peptides and its consequences for gene-expression profiling in U-937 human macrophages and HeLa cervical cancer cells
Authors:	Kuo, Jung-hua Steven Lin, Chia-Wei
Contributors:	藥學系
Keywords:	Cell Penetrating Peptides Conjugation Fluorescein-5-Isothiocynate Microarray Rath
Date:	2013-11
Issue Date:	2014-05-26 10:43:57 (UTC+8)
Publisher:	Informa Healthcare
Abstract:	Rath peptide has been introduced as a delivery vector that transports various membrane-impermeable cargoes in a non-covalent fashion. In this paper, we present a study on Rath peptide conjugated with fluorescein-5-isothiocynate (FITC) differing in its N- and C-termini. We conducted cellular toxicity and uptake experiments in U-937 and HeLa cells to analyze biocompatibility profiles and translocation efficiencies of Rath peptide with FITC serving as both a cargo and a fluorescent marker. We found that the conjugation of FITC on Rath peptide at N- terminus (FITC-Rath) led to more rapid cellular uptake in U-937 cells and significantly higher cellular uptake in HeLa cells than that which occurred at C-terminus. From DNA microarray analysis, FITC-Rath induced gene expression changes in both U-937 and HeLa cells. Five overlapping regulated genes were identified, and this overlap indicated that FITC-Rath displayed some degree of generality regarding gene responses in the two cell lines used. A real-time quantitative reverse transcriptase-polymerase chain reaction was used to confirm which regulated genes were affected by FITC-Rath. Cell communication, signal transduction, cell surface receptor signaling pathway, signal transducer activity and cellular process, were identified as overlapping biological themes. These data provide useful information on molecular mechanisms for using Rath-based delivery systems.
Relation:	Journal of Drug Targeting, v.21 n.9, pp.801-808
Appears in Collections:	[Dept. of Pharmacy] Periodical Articles

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