A novel small peptide as an epidermal growth factor receptor targeting ligand for nanodelivery in vitro

Cui-yan Han,1,2 Li-ling Yue,2 Ling-yu Tai,1 Li Zhou,2 Xue-yan Li,2 Gui-hua Xing,2 Xing-gang Yang,1 Ming-shuang Sun,1 Wei-san Pan1 1School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, People’s Republic of China; 2Qiqihar Medical University, Qiqihar, People’s Republic...

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Autores principales:	Han CY, Yue LL, Tai LY, Zhou L, Li XY, Xing GH, Yang XG, Sun MS, Pan WS
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2013
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/3641d1a781064acbaa84f716209607ab
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spelling	oai:doaj.org-article:3641d1a781064acbaa84f716209607ab2021-12-02T05:55:48ZA novel small peptide as an epidermal growth factor receptor targeting ligand for nanodelivery in vitro1176-91141178-2013https://doaj.org/article/3641d1a781064acbaa84f716209607ab2013-04-01T00:00:00Zhttp://www.dovepress.com/a-novel-small-peptide-as-an-epidermal-growth-factor-receptor-targeting-a12821https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Cui-yan Han,1,2 Li-ling Yue,2 Ling-yu Tai,1 Li Zhou,2 Xue-yan Li,2 Gui-hua Xing,2 Xing-gang Yang,1 Ming-shuang Sun,1 Wei-san Pan1 1School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, People’s Republic of China; 2Qiqihar Medical University, Qiqihar, People’s Republic of China Abstract: The epidermal growth factor receptor (EGFR) serves an important function in the proliferation of tumors in humans and is an effective target for the treatment of cancer. In this paper, we studied the targeting characteristics of small peptides (AEYLR, EYINQ, and PDYQQD) that were derived from three major autophosphorylation sites of the EGFR C-terminus domain in vitro. These small peptides were labeled with fluorescein isothiocyanate (FITC) and used the peptide LARLLT as a positive control, which bound to putative EGFR selected from a virtual peptide library by computer-aided design, and the independent peptide RALEL as a negative control. Analyses with flow cytometry and an internalization assay using NCI-H1299 and K562 with high EGFR and no EGFR expression, respectively, indicated that FITC-AEYLR had high EGFR targeting activity. Biotin-AEYLR that was specifically bound to human EGFR proteins demonstrated a high affinity for human non-small-cell lung tumors. We found that AEYLR peptide-conjugated, nanostructured lipid carriers enhanced specific cellular uptake in vitro during a process that was apparently mediated by tumor cells with high-expression EGFR. Analysis of the MTT assay indicated that the AEYLR peptide did not significantly stimulate or inhibit the growth activity of the cells. These findings suggest that, when mediated by EGFR, AEYLR may be a potentially safe and efficient delivery ligand for targeted chemotherapy, radiotherapy, and gene therapy. Keywords: EGFR, small peptide, tumor targeting, lung cancer, NLCHan CYYue LLTai LYZhou LLi XYXing GHYang XGSun MSPan WSDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2013, Iss default, Pp 1541-1549 (2013)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Han CY Yue LL Tai LY Zhou L Li XY Xing GH Yang XG Sun MS Pan WS A novel small peptide as an epidermal growth factor receptor targeting ligand for nanodelivery in vitro
description	Cui-yan Han,1,2 Li-ling Yue,2 Ling-yu Tai,1 Li Zhou,2 Xue-yan Li,2 Gui-hua Xing,2 Xing-gang Yang,1 Ming-shuang Sun,1 Wei-san Pan1 1School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, People’s Republic of China; 2Qiqihar Medical University, Qiqihar, People’s Republic of China Abstract: The epidermal growth factor receptor (EGFR) serves an important function in the proliferation of tumors in humans and is an effective target for the treatment of cancer. In this paper, we studied the targeting characteristics of small peptides (AEYLR, EYINQ, and PDYQQD) that were derived from three major autophosphorylation sites of the EGFR C-terminus domain in vitro. These small peptides were labeled with fluorescein isothiocyanate (FITC) and used the peptide LARLLT as a positive control, which bound to putative EGFR selected from a virtual peptide library by computer-aided design, and the independent peptide RALEL as a negative control. Analyses with flow cytometry and an internalization assay using NCI-H1299 and K562 with high EGFR and no EGFR expression, respectively, indicated that FITC-AEYLR had high EGFR targeting activity. Biotin-AEYLR that was specifically bound to human EGFR proteins demonstrated a high affinity for human non-small-cell lung tumors. We found that AEYLR peptide-conjugated, nanostructured lipid carriers enhanced specific cellular uptake in vitro during a process that was apparently mediated by tumor cells with high-expression EGFR. Analysis of the MTT assay indicated that the AEYLR peptide did not significantly stimulate or inhibit the growth activity of the cells. These findings suggest that, when mediated by EGFR, AEYLR may be a potentially safe and efficient delivery ligand for targeted chemotherapy, radiotherapy, and gene therapy. Keywords: EGFR, small peptide, tumor targeting, lung cancer, NLC
format	article
author	Han CY Yue LL Tai LY Zhou L Li XY Xing GH Yang XG Sun MS Pan WS
author_facet	Han CY Yue LL Tai LY Zhou L Li XY Xing GH Yang XG Sun MS Pan WS
author_sort	Han CY
title	A novel small peptide as an epidermal growth factor receptor targeting ligand for nanodelivery in vitro
title_short	A novel small peptide as an epidermal growth factor receptor targeting ligand for nanodelivery in vitro
title_full	A novel small peptide as an epidermal growth factor receptor targeting ligand for nanodelivery in vitro
title_fullStr	A novel small peptide as an epidermal growth factor receptor targeting ligand for nanodelivery in vitro
title_full_unstemmed	A novel small peptide as an epidermal growth factor receptor targeting ligand for nanodelivery in vitro
title_sort	novel small peptide as an epidermal growth factor receptor targeting ligand for nanodelivery in vitro
publisher	Dove Medical Press
publishDate	2013
url	https://doaj.org/article/3641d1a781064acbaa84f716209607ab
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A novel small peptide as an epidermal growth factor receptor targeting ligand for nanodelivery in vitro

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