Improved Tumor Targeting and Longer Retention Time of NIR Fluorescent Probes Using Bioorthogonal Chemistry

doi:10.7150/thno.20912

CORC > 自动化研究所 > 中国科学院自动化研究所 > 中国科学院分子影像重点实验室

	Improved Tumor Targeting and Longer Retention Time of NIR Fluorescent Probes Using Bioorthogonal Chemistry
	Zhang, Xianghan 1; Wang, Bo 1; Zhao, Na 1; Tian, Zuhong 3; Dai, Yunpeng 1; Nie, Yongzhan 3; Tian, Jie1,2 ; Wang, Zhongliang 1; Chen, Xiaoyuan 4
刊名	THERANOSTICS
	2017
卷号	7 期号:15 页码:3794-3802
关键词	Click Chemistry Nir Fluorescence Probes Gebp11 Gastric Cancer
DOI	10.7150/thno.20912
文献子类	Article
英文摘要	The traditional labeling method for targeted NIR fluorescence probes requires directly covalent-bonded conjugation of targeting domains and fluorophores in vitro. Although this strategy works well, it is not sufficient for detecting or treating cancers in vivo, due to steric hindrance effects that relatively large fluorophore molecules exert on the configurations and physiological functions of specific targeting domains. The copper-free, "click-chemistry"-assisted assembly of small molecules in living systems may enhance tumor accumulation of fluorescence probes by improving the binding affinities of the targeting factors. Here, we employed a vascular homing peptide, GEBP11, as a targeting factor for gastric tumors, and we demonstrate its effectiveness for in vivo imaging via click-chemistry-mediated conjugation with fluorescence molecules in tumor xenograft mouse models. This strategy showed higher binding affinities than those of the traditional conjugation method, and our results showed that the tumor accumulation of click-chemistry-mediated probes are 11-fold higher than that of directly labeled probes. The tracking life was prolonged by 12-fold, and uptake of the probes into the kidney was reduced by 6.5-fold. For lesion tumors of different sizes, click-chemistry-mediated probes can achieve sufficient signal-to-background ratios (3.5-5) for in vivo detection, and with diagnostic sensitivity approximately 3.5 times that of traditional labeling probes. The click-chemistry-assisted detection strategy utilizes the advantages of "small molecule" probes while not perturbing their physiological functions; this enables tumor detection with high sensitivity and specific selectivity.
WOS关键词	GUIDED CANCER-SURGERY ; GASTRIC-CANCER ; VIVO ; PEPTIDE ; BINDING ; MICE
WOS研究方向	Research & Experimental Medicine
语种	英语
WOS记录号	WOS:000408444200014
资助机构	Program of the National Basic Research and Development Program of China (973)(2013CB733803) ; National Natural Science Foundation of China(81227901 ; national 1000 Young Talents Program of China ; 81402467 ; 81671753)
内容类型	期刊论文
源URL	[http://ir.ia.ac.cn/handle/173211/20723]
专题	自动化研究所_中国科学院分子影像重点实验室
作者单位	1.Xidian Univ, Engn Res Ctr Mol Imaging & Neuroimaging, Minist Educ, Sch Life Sci & Technol, Xian 710026, Shaanxi, Peoples R China 2.Chinese Acad Sci, Inst Automat, Beijing 100190, Peoples R China 3.Fourth Mil Med Univ, Inst Digest Dis, Xijing Hosp, Xian 710032, Shaanxi, Peoples R China 4.Natl Inst Biomed Imaging & Bioengn, Lab Mol Imaging & Nanomed, NIH, Bethesda, MD 20892 USA
推荐引用方式 GB/T 7714	Zhang, Xianghan,Wang, Bo,Zhao, Na,et al. Improved Tumor Targeting and Longer Retention Time of NIR Fluorescent Probes Using Bioorthogonal Chemistry[J]. THERANOSTICS,2017,7(15):3794-3802.
APA	Zhang, Xianghan.,Wang, Bo.,Zhao, Na.,Tian, Zuhong.,Dai, Yunpeng.,...&Chen, Xiaoyuan.(2017).Improved Tumor Targeting and Longer Retention Time of NIR Fluorescent Probes Using Bioorthogonal Chemistry.THERANOSTICS,7(15),3794-3802.
MLA	Zhang, Xianghan,et al."Improved Tumor Targeting and Longer Retention Time of NIR Fluorescent Probes Using Bioorthogonal Chemistry".THERANOSTICS 7.15(2017):3794-3802.