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Peptide PHSCNK as an integrin alpha(5)beta(1) antagonist targets stealth liposomes to integrin-overexpressing melanoma
Dai, Wenbing; Yang, Tingyuan; Wang, Yiguang; Wang, Xueqing; Wang, Jiancheng; Zhang, Xuan; Zhang, Qiang
关键词Targeted delivery system Liposomes Doxorubicin PHSCNK Integrins
刊名NANOMEDICINE-NANOTECHNOLOGY BIOLOGY AND MEDICINE
2012-10-01
DOI10.1016/j.nano.2012.01.003
8期:7页:1152-1161
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Nanoscience & Nanotechnology ; Medicine, Research & Experimental
研究领域[WOS]Science & Technology - Other Topics ; Research & Experimental Medicine
关键词[WOS]STERICALLY STABILIZED LIPOSOMES ; IMPROVED ANTITUMOR EFFICACY ; LOADED LIPOSOMES ; IN-VIVO ; INTRACELLULAR DELIVERY ; TUMOR NEOVASCULATURE ; BREAST-CANCER ; RGD PEPTIDE ; DOXORUBICIN ; CELLS
英文摘要

As an integrin alpha(5)beta(1) antagonist, N-acetyl-proline-histidine-serine-cysteine-asparagine-amide (Ac-PHSCN-NH2) is currently in phase II trials for various cancer therapies. In this study Ac-PHSCNK-NH2 (PHSCNK) was used as a novel homing peptide to prepare ligand-targeted liposomes loaded with doxorubicin (PHSCNK-PL-DOX), with the hypothesis that the therapy target of integrin alpha(5)beta(1) may also serve as a delivery target. The stealth liposomes loaded with doxorubicin (PL-DOX) were used as the control. PHSCNK-PL-DOX demonstrated an enhanced intracellular uptake and a greater cytotoxicity against melanoma B16F10 cells in comparison with PL-DOX. The novel targeted formulation displayed stronger tumor inhibition and prolonged survival time in comparison with controls in C57BL/6mice bearing B16F10 tumors, and it exhibited less heart toxicity in hematoxylin-eosin (H&E) staining of tissues. Taking the pharmacokinetics and biodistribution results into account, the authors conclude that alpha(5)beta(1) integrin-mediated liposomes might be used as a potential delivery system for targeted tumor therapy.

From the Clinical Editor: Lactosyl-norcantharidin TMC nanoparticles were found superior in comparison with Lac-NCTD and Lac-NCTD chitosan nanoparticles from the standpoint of antitumor activity on murine hepatocarcinoma 22 subcutaneous model. (C) 2012 Elsevier Inc. All rights reserved.

语种英语
WOS记录号WOS:000309216300013
项目编号2009CB930300 ; 2009zx09310-001
资助机构National Basic Research Program of China ; National Key program of New Drug innovation
引用统计
被引频次:20[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/65495
专题北京大学药学院
北京大学药学院_药剂学系
作者单位Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
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GB/T 7714
Dai, Wenbing,Yang, Tingyuan,Wang, Yiguang,et al. Peptide PHSCNK as an integrin alpha(5)beta(1) antagonist targets stealth liposomes to integrin-overexpressing melanoma[J]. NANOMEDICINE-NANOTECHNOLOGY BIOLOGY AND MEDICINE,2012,8(7):1152-1161.
APA Dai, Wenbing.,Yang, Tingyuan.,Wang, Yiguang.,Wang, Xueqing.,Wang, Jiancheng.,...&Zhang, Qiang.(2012).Peptide PHSCNK as an integrin alpha(5)beta(1) antagonist targets stealth liposomes to integrin-overexpressing melanoma.NANOMEDICINE-NANOTECHNOLOGY BIOLOGY AND MEDICINE,8(7),1152-1161.
MLA Dai, Wenbing,et al."Peptide PHSCNK as an integrin alpha(5)beta(1) antagonist targets stealth liposomes to integrin-overexpressing melanoma".NANOMEDICINE-NANOTECHNOLOGY BIOLOGY AND MEDICINE 8.7(2012):1152-1161.
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