文献类型：期刊文献

英文题名：AMP-guided tumour-specific nanoparticle delivery via adenosine A1 receptor

作者：Dai, Tongcheng[1];Li, Na[1];Han, Fajun[1];Zhang, Hua[1];Zhang, Yuanxing[1,2];Liu, Qin[1,2]

机构：[1]E China Univ Sci & Technol, State Key Lab Bioreactor Engn, 130 Meilong Rd, Shanghai 200237, Peoples R China;[2]Shanghai Collaborat Innovat Ctr Biomfg Technol, Shanghai 200237, Peoples R China

年份：2016

卷号：83

起止页码：37

外文期刊名：BIOMATERIALS

收录：;EI(收录号：20160801962150);WOS:【SCI-EXPANDED(收录号:WOS:000371651700004)】；

基金：We thank Dr. Jianghong Rao and Dr. Hexin Xie for helpful discussions and suggestions, and Dr. Liqin Xiong for her guidance in the synthesis and characterization of nanoparticles. This work was supported by the National Special Fund for State Key Laboratory of Bioreactor Engineering, Grant No. 2060204.

语种：英文

外文关键词：AMP ligand; Tumour target; Nanoparticle; A(1)R; Imaging

摘要：Active targeting-ligands have been increasingly used to functionalize nanoparticles for tumour-specific clinical applications. Here we utilize nucleotide adenosine 5'-monophosphate (AMP) as a novel ligand to functionalize polymer-based fluorescent nanoparticles (NPs) for tumour-targeted imaging. We demonstrate that AMP-conjugated NPs (NPs-AMP) efficiently bind to and are following internalized into colon cancer cell CW-2 and breast cancer cell MDA-MB-468 in vitro. RNA interference and inhibitor assays reveal that the targeting effects mainly rely on the specific binding of AMP to adenosine A(1) receptor (A(1)R), which is greatly up-regulated in cancer cells than in matched normal cells. More importantly, NPs-AMP specifically accumulate in the tumour site of colon and breast tumour xenografts and are further internalized into the tumour cells in vivo via tail vein injection, confirming that the high in vitro specificity of AMP can be successfully translated into the in vivo efficacy. Furthermore, NPs-AMP exhibit an active tumour-targeting behaviour in various colon and breast cancer cells, which is positively related to the up-regulation level of A1R in cancer cells, suggesting that AMP potentially suits for more extensive A(1)R-overexpressing cancer models. This work establishes AMP to be a novel tumour-targeting ligand and provides a promising strategy for future diagnostic or therapeutic applications. (C) 2016 Elsevier Ltd. All rights reserved.