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	Spect/ct imaging of the novel her2-targeted peptide probe tc-99m-hynic-h6f in breast cancer mouse models
	Li, Liqiang1,2; Wu, Yue1,2; Wang, Zihua3; Jia, Bing1,2,4; Hu, Zhiyuan3; Dong, Chengyan5; Wang, Fan1,2,5
刊名	Journal of nuclear medicine
	2017-05-01
卷号	58期号:5页码:821-826
关键词	Her2 Breast cancer Spect Targeting peptide Trastuzumab
ISSN号	0161-5505
DOI	10.2967/jnumed.116.183863
通讯作者	Wang, fan(wangfan@bjmu.edu.cn)
英文摘要	Overexpression of human epidermal growth factor receptor 2 (her2) plays important roles in tumorigenesis and tumor progression in breast cancer. nuclear imaging of her2 expression in tumors might detect all her2-positive tumors throughout the body and guide her2-targeted therapies for patients. we therefore aimed to develop a her2-targeted peptide probe for breast cancer imaging. a novel spect imaging probe, tc-99m-hynic-h6f, was prepared and then evaluated in breast cancer animal models. methods: the her2-targeted peptide h6f (ylffvfer) was conjugated with the bifunctional chelator hydrazinonicotinamide (hynic). tc-99m-hynic-h6f was prepared, and the in vivo characteristics of tc-99m-hynic-h6f were investigated in mda-mb-453 (her2-positive) and mda-mb-231 (her2-negative) models using small-animal spect/ct. moreover, to investigate the specificity of the h6f peptide toward her2 and the potential applications in monitoring therapies involving trastuzumab, unlabeled h6f and trastuzumab were used as blocking agents in cell competition studies and spect imaging. results: a standard tricine/trisodium triphenylphosphine-3,3',3 ''-trisulfonate labeling procedure demonstrated that the radiochemical purity was greater than 95%. tc-99m-hynic-h6f displayed excellent her2-binding specificity both in vitro and in vivo. spect/ct imaging revealed that the mda-mb-453 tumors were clearly visualized (percentage injected dose per gram, 3.58 +/- 0.01 at 30 min after injection), whereas the signals in her2-negative mda-mb-231 tumors were much lower (0.73 +/- 0.22 at 30 min after injection). tumor uptake of mda-mb-453 was blocked by the coinjection of excess h6f but not by excess trastuzumab. conclusion: the tc-99m-hynic-h6f peptide probe specifically accumulates in her2-positive tumors and is therefore promising for the diagnosis of her2-positive cancers. because (99m)-hynic-h6f and trastuzumab target different regions of the her2 receptor, this radiotracer also has great potential for monitoring the therapeutic efficacy of trastuzumab by rechecking the expression level of her2 without blocking effect during therapy.
WOS关键词	FACTOR RECEPTOR 2 ; IN-VIVO ; HER2 ; TUMOR ; TRASTUZUMAB ; GROWTH ; EXPRESSION ; THERAPIES ; MORTALITY ; DELIVERY
WOS研究方向	Radiology, Nuclear Medicine & Medical Imaging
WOS类目	Radiology, Nuclear Medicine & Medical Imaging
语种	英语
出版者	SOC NUCLEAR MEDICINE INC
WOS记录号	WOS:000400633500027
内容类型	期刊论文
URI标识	http://www.corc.org.cn/handle/1471x/2177204
专题	高能物理研究所
通讯作者	Wang, Fan
作者单位	1.Peking Univ, Med Isotopes Res Ctr, 38 Xueyuan Rd, Beijing 100191, Peoples R China 2.Peking Univ, Sch Basic Med Sci, Dept Radiat Med, Beijing, Peoples R China 3.Natl Ctr Nanosci & Technol China, CAS Key Lab Biomed Effects Nanomat & Nanosafety, Beijing, Peoples R China 4.Peking Univ, Med & Hlth Analyt Ctr, Beijing, Peoples R China 5.Chinese Acad Sci, Inst Biophys, CAS Ctr Excellence Biomacromol, Key Lab Prot & Peptide Pharmaceut, Beijing, Peoples R China
推荐引用方式 GB/T 7714	Li, Liqiang,Wu, Yue,Wang, Zihua,et al. Spect/ct imaging of the novel her2-targeted peptide probe tc-99m-hynic-h6f in breast cancer mouse models[J]. Journal of nuclear medicine,2017,58(5):821-826.
APA	Li, Liqiang.,Wu, Yue.,Wang, Zihua.,Jia, Bing.,Hu, Zhiyuan.,...&Wang, Fan.(2017).Spect/ct imaging of the novel her2-targeted peptide probe tc-99m-hynic-h6f in breast cancer mouse models.Journal of nuclear medicine,58(5),821-826.
MLA	Li, Liqiang,et al."Spect/ct imaging of the novel her2-targeted peptide probe tc-99m-hynic-h6f in breast cancer mouse models".Journal of nuclear medicine 58.5(2017):821-826.

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