首页 / 院系成果 / 成果详情页

Enhanced Glioblastoma Targeting Ability of Carfilzomib Enabled by a (D)A7R-Modified Lipid Nanodisk 期刊论文

编号：

f2d64340-634e-4489-8347-0c0a754d4bbe
作者：

Zhang, Mingfei(张明菲)#^[1,2,3,4]Lu, Linwei^[5,6];Ying, Man(应曼)^[1,2,3,4]Ruan, Huitong^[1,2,3,4];Wang, Xiaoyi^[1,2,3,4];Wang, Huan^[1,2,3,4];Chai, Zhilan^[1,2,3,4];Wang, Songli^[1,2,3,4];Zhan, Changyou(占昌友)^[7,8]Pan, Jun(潘俊)^[1,2,3,4]Lu, Weiyue(陆伟跃)*^{[1,2,3,4,9,10]}
语种：

English
期刊：

MOLECULAR PHARMACEUTICS ISSN：1543-8384 2018 年 15 卷 6 期 (2437 - 2447) ; JUN
收录：
关键词：

(D)A7R peptide nanodisk carfilzomib glioma neovasculature target therapy
摘要：

The robust proliferation of tumors relies on a rich neovasculature for nutrient supplies. Therefore, a basic strategy of tumor targeting therapy should include not only killing regular cancer cells but also blocking tumor neovasculature. D-peptide (D)A7R, which was previously reported to specifically bind vascular endothelial growth factor receptor 2 (VEGFR2) and neuropilin-1 (NRP-1), could achieve the goal of multitarget recognition. Accordingly, the main purposes of this work were to establish a carfilzomib-loaded lipid nanodisk modified with multifunctional peptide (D)A7R ((D)A7R-ND/CFZ) and to evaluate its anti-glioblastoma efficacy in vitro and in vivo. It is testified that the (D)A7R peptide-conjugated lipid nanodisk can be specifically taken up by U87MG cells and HUVECs. Furthermore, (D)A7R-ND demonstrated a more enhanced penetration than that of the nonmodified formulation on the tumor spheroid model in vitro and more tumor region accumulation in vivo on the subcutaneous and intracranial tumor-bearing nude mice model. (D)A7R-ND was shown to co-localize with tumor neovasculature in vivo. When loaded with proteasome inhibitor carfilzomib, the (D)A7R-decorated nanodisk could remarkably suppress tumor proliferation, extend survival time of nude mice bearing an intracranial tumor, and inhibit neovasculature formation with an efficacy higher than that of the nonmodified nanodisk in vitro and in vivo. The present study verified that the heptapeptide (D)A7R-conjugated nanodisk is a promising nanocarrier for glioblastoma targeting therapy.
推荐引用方式
GB/T 7714：

Zhang Mingfei,Lu Linwei,Ying Man, et al. Enhanced Glioblastoma Targeting Ability of Carfilzomib Enabled by a (D)A7R-Modified Lipid Nanodisk [J].MOLECULAR PHARMACEUTICS,2018,15(6):2437-2447.
APA：

Zhang Mingfei,Lu Linwei,Ying Man,Ruan Huitong,&Lu Weiyue.(2018).Enhanced Glioblastoma Targeting Ability of Carfilzomib Enabled by a (D)A7R-Modified Lipid Nanodisk .MOLECULAR PHARMACEUTICS,15(6):2437-2447.
MLA：

Zhang Mingfei, et al. "Enhanced Glioblastoma Targeting Ability of Carfilzomib Enabled by a (D)A7R-Modified Lipid Nanodisk" .MOLECULAR PHARMACEUTICS 15,6(2018):2437-2447.

浏览次数：7  下载次数：0

分享到：

浏览次数：7

下载次数：0

打印次数：0