An FGFR1-Binding Peptide Modified Liposome for siRNA Delivery in Lung Cancer

Liposome modification by targeting ligands has been used to mediate specific interactions and drug delivery to target cells. In this study, a new peptide ligand, CP7, was found to be able to effectively bind to FGFR1 through reverse molecular docking and could cooperate with VEGFR3 to achieve target...

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Main Authors: Zhipeng Dong, Yunxue Yin, Jun Luo, Bingxia Li, Fangning Lou, Qiyan Wang, Qingfa Zhou, Baofen Ye, Yue Wang
Format: Article
Language:English
Published: MDPI AG 2022-07-01
Series:International Journal of Molecular Sciences
Subjects:
Online Access:https://www.mdpi.com/1422-0067/23/15/8380
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author Zhipeng Dong
Yunxue Yin
Jun Luo
Bingxia Li
Fangning Lou
Qiyan Wang
Qingfa Zhou
Baofen Ye
Yue Wang
author_facet Zhipeng Dong
Yunxue Yin
Jun Luo
Bingxia Li
Fangning Lou
Qiyan Wang
Qingfa Zhou
Baofen Ye
Yue Wang
author_sort Zhipeng Dong
collection DOAJ
description Liposome modification by targeting ligands has been used to mediate specific interactions and drug delivery to target cells. In this study, a new peptide ligand, CP7, was found to be able to effectively bind to FGFR1 through reverse molecular docking and could cooperate with VEGFR3 to achieve targeting of A549 cells. CP7 was modified on the surface of the liposome to construct a targeted and safe nanovehicle for the delivery of a therapeutic gene, Mcl-1 siRNA. Due to the specific binding between CP7 and A549 cells, siRNA-loaded liposome-PEG-CP7 showed increased cellular uptake in vitro, resulting in significant apoptosis of tumor cells through silencing of the Mcl-1 gene, which is associated with apoptosis and angiogenesis. This gene delivery system also showed significantly better antitumor activity in tumor-bearing mice in vivo. All of these suggested that siRNA-loaded liposome-PEG-CP7 could be a promising gene drug delivery system with good bioavailability and minimal side effects for treatment.
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spelling doaj.art-802861294996476081b0dc58273cf6c92023-11-30T22:26:29ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672022-07-012315838010.3390/ijms23158380An FGFR1-Binding Peptide Modified Liposome for siRNA Delivery in Lung CancerZhipeng Dong0Yunxue Yin1Jun Luo2Bingxia Li3Fangning Lou4Qiyan Wang5Qingfa Zhou6Baofen Ye7Yue Wang8Key Laboratory of Biomedical Functional Materials, School of Sciences, China Pharmaceutical University, Nanjing 211198, ChinaKey Laboratory of Biomedical Functional Materials, School of Sciences, China Pharmaceutical University, Nanjing 211198, ChinaKey Laboratory of Biomedical Functional Materials, School of Sciences, China Pharmaceutical University, Nanjing 211198, ChinaKey Laboratory of Biomedical Functional Materials, School of Sciences, China Pharmaceutical University, Nanjing 211198, ChinaKey Laboratory of Biomedical Functional Materials, School of Sciences, China Pharmaceutical University, Nanjing 211198, ChinaKey Laboratory of Biomedical Functional Materials, School of Sciences, China Pharmaceutical University, Nanjing 211198, ChinaKey Laboratory of Biomedical Functional Materials, School of Sciences, China Pharmaceutical University, Nanjing 211198, ChinaKey Laboratory of Biomedical Functional Materials, School of Sciences, China Pharmaceutical University, Nanjing 211198, ChinaKey Laboratory of Biomedical Functional Materials, School of Sciences, China Pharmaceutical University, Nanjing 211198, ChinaLiposome modification by targeting ligands has been used to mediate specific interactions and drug delivery to target cells. In this study, a new peptide ligand, CP7, was found to be able to effectively bind to FGFR1 through reverse molecular docking and could cooperate with VEGFR3 to achieve targeting of A549 cells. CP7 was modified on the surface of the liposome to construct a targeted and safe nanovehicle for the delivery of a therapeutic gene, Mcl-1 siRNA. Due to the specific binding between CP7 and A549 cells, siRNA-loaded liposome-PEG-CP7 showed increased cellular uptake in vitro, resulting in significant apoptosis of tumor cells through silencing of the Mcl-1 gene, which is associated with apoptosis and angiogenesis. This gene delivery system also showed significantly better antitumor activity in tumor-bearing mice in vivo. All of these suggested that siRNA-loaded liposome-PEG-CP7 could be a promising gene drug delivery system with good bioavailability and minimal side effects for treatment.https://www.mdpi.com/1422-0067/23/15/8380CP7liposometarget deliveryFGFR1gene drug
spellingShingle Zhipeng Dong
Yunxue Yin
Jun Luo
Bingxia Li
Fangning Lou
Qiyan Wang
Qingfa Zhou
Baofen Ye
Yue Wang
An FGFR1-Binding Peptide Modified Liposome for siRNA Delivery in Lung Cancer
International Journal of Molecular Sciences
CP7
liposome
target delivery
FGFR1
gene drug
title An FGFR1-Binding Peptide Modified Liposome for siRNA Delivery in Lung Cancer
title_full An FGFR1-Binding Peptide Modified Liposome for siRNA Delivery in Lung Cancer
title_fullStr An FGFR1-Binding Peptide Modified Liposome for siRNA Delivery in Lung Cancer
title_full_unstemmed An FGFR1-Binding Peptide Modified Liposome for siRNA Delivery in Lung Cancer
title_short An FGFR1-Binding Peptide Modified Liposome for siRNA Delivery in Lung Cancer
title_sort fgfr1 binding peptide modified liposome for sirna delivery in lung cancer
topic CP7
liposome
target delivery
FGFR1
gene drug
url https://www.mdpi.com/1422-0067/23/15/8380
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