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A Novel Estrogen Receptor alpha-Targeted Near-Infrared Fluorescent Probe for in Vivo Detection of Breast Tumor

文献类型：期刊论文

作者Tang, Chu1,2; Du, Yang2,3,4; Liang, Qian2; Cheng, Zhen5,6; Tian, Jie1,2,3,4
刊名MOLECULAR PHARMACEUTICS
出版日期2018-10-01
卷号15期号:10页码:4702-4709
关键词breast cancer NIR fluorescent probe ER alpha-targeted imaging in vivo detection
ISSN号1543-8384
DOI10.1021/acs.molpharmaceut.8b00684
通讯作者Cheng, Zhen(zcheng@stanford.edu) ; Tian, Jie(jie.tian@ia.ac.cn)
英文摘要The ability to detect breast cancer early in its progression is essential to improve patient survival and quality of life. The noninvasive and dynamic imaging and functional assessments of estrogen receptor-alpha (ER alpha), which is commonly expressed at high levels in breast cancer, are important for effective diagnosis and treatment. Hence, the development of a specific ER alpha-targeted probe is a major research goal. To that end, in the present study, we created a novel near-infrared (NIR) fluorescent probe, IRDye800CW-E-2, for targeted ER alpha imaging in breast-tumor-bearing mice. IRDye800CW-E-2 consisted of a cyanine dye IRDye800CW as the NIR fluorophore and the E-2 analogue ethinyl estradiol amine as an ERa targeting ligand. The ethinyl estradiol amine was initially labeled with fluorescein isothiocyanate (FITC) to evaluate the binding specificity to human breast-tumor cells in vitro. Flow chamber and in vitro confocal laser endomicroscopy imaging experiments demonstrated that FITC-E-2 was specifically taken up by MCF-7 cells. Furthermore, NIR fluorescence imaging revealed the ability of IRDye800CW-E-2 to rapidly target tumors and to achieve good contrast between tumors and background signal 4-48 h postinjection. The fluorescent signal of IRDye800CW-E-2 in tumors was successfully blocked by the coinjection of the endogenous ER alpha-ligand 17 beta-estradiol (E-2) and the probe. Ex vivo fluorescent imaging further confirmed high uptake of the probe by tumors. These results indicated that IRDye800CW-E-2 has great potential as an ER alpha-targeted imaging probe for early breast-tumor detection and has potential for clinical translation.
WOS关键词BIOLOGICAL EVALUATION ; INTERNATIONAL-UNION ; ENDOCRINE TREATMENT ; CANCER ; DESIGN ; RESISTANCE ; THERAPY ; LIGANDS ; CORE ; TOOL
资助项目Ministry of Science and Technology of China[2017YFA0205200] ; Ministry of Science and Technology of China[2017YFC1309100] ; Ministry of Science and Technology of China[2016YFC0102000] ; National Natural Science Foundation of China[81470083] ; National Natural Science Foundation of China[81527805] ; National Natural Science Foundation of China[61231004] ; National Natural Science Foundation of China[81601548] ; National Natural Science Foundation of China[81772011] ; National Natural Science Foundation of China[81701771] ; International Innovation Team of CAS[20140491524] ; Beijing Municipal Science & Technology Commission[Z161100002616022] ; China Postdoctoral Science Foundation[2017M613084] ; Shaanxi Postdoctoral Science Foundation funded project[2017BSHEDZZ91]
WOS研究方向Research & Experimental Medicine ; Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000446413400038
出版者AMER CHEMICAL SOC
资助机构Ministry of Science and Technology of China ; National Natural Science Foundation of China ; International Innovation Team of CAS ; Beijing Municipal Science & Technology Commission ; China Postdoctoral Science Foundation ; Shaanxi Postdoctoral Science Foundation funded project
源URL[http://ir.ia.ac.cn/handle/173211/28121]  
专题自动化研究所_中国科学院分子影像重点实验室
通讯作者Cheng, Zhen; Tian, Jie
作者单位1.Xidian Univ, Sch Life Sci & Technol, Minist Educ, Engn Res Ctr Mol & Neuro Imaging, Xian 710126, Shaanxi, Peoples R China
2.Chinese Acad Sci, Inst Automat, State Key Lab Management & Control Complex Syst, CAS Key Lab Mol Imaging, Beijing 100190, Peoples R China
3.Beijing Key Lab Mol Imaging, Beijing 100190, Peoples R China
4.Univ Chinese Acad Sci, Beijing 100080, Peoples R China
5.Stanford Univ, Dept Radiol, Mol Imaging Program Stanford MIPS, Stanford, CA 94305 USA
6.Stanford Univ, Bio X Program, Canary Ctr, Stanford Canc Early Detect, Stanford, CA 94305 USA
推荐引用方式
GB/T 7714		 Tang, Chu,Du, Yang,Liang, Qian,et al. A Novel Estrogen Receptor alpha-Targeted Near-Infrared Fluorescent Probe for in Vivo Detection of Breast Tumor[J]. MOLECULAR PHARMACEUTICS,2018,15(10):4702-4709.
APA Tang, Chu,Du, Yang,Liang, Qian,Cheng, Zhen,&Tian, Jie.(2018).A Novel Estrogen Receptor alpha-Targeted Near-Infrared Fluorescent Probe for in Vivo Detection of Breast Tumor.MOLECULAR PHARMACEUTICS,15(10),4702-4709.
MLA Tang, Chu,et al."A Novel Estrogen Receptor alpha-Targeted Near-Infrared Fluorescent Probe for in Vivo Detection of Breast Tumor".MOLECULAR PHARMACEUTICS 15.10(2018):4702-4709.

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