中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
Novel HER2-Targeted Peptide for NIR-II Imaging of Tumor

文献类型:期刊论文

作者Cao, Rui3; Li, Renda3; Shi, Hui2; Liu, Hongguang3; Cheng, Zhen1,2
刊名MOLECULAR PHARMACEUTICS
出版日期2023-02-06
卷号20期号:2页码:1394-1403
关键词NIR-II peptide HER2 tumor optical imaging
DOI10.1021/acs.molpharmaceut.2c00964
文献子类Article
英文摘要Molecular targets serve a crucial role in drug development. Herein, we discovered a novel peptide that can specifically target the human epidermal growth factor receptor 2 (HER2) and thus named it Herceptide. In our study, Herceptide was conjugated to the near-infrared fluorescent dye indocyanine green (ICG) to obtain a probe, ICG-Herceptide. Importantly, specific binding to HER2 was revealed by molecular docking, surface plasmon resonance analysis, and competition assays. The probe showed high binding affinity (KD = 1.03 nM) and fast binding property (kon = 0.44 min-1). In vivo near-infrared window two (NIR-II, 1000-1700 nm) imaging in HER2-overexpressed SKOV3 tumor-bearing mice demonstrated a high tumor-to-normal tissue signal ratio (T/N = 7.3) at 8 h postinjection. In the blocking study, ICG-Herceptide coinjected with Herceptide only showed a weak tumor signal. In other HER2 high-expression tumors, such as non-small-cell lung cancer A549 and gastric cancer MKN45, the tumor-to-normal tissue signal ratios (T/N) were 4.1 and 4.7, respectively. In contrast, HER2 low-expression tumor MDAMB231 shows no imaging contrast between the tumor and normal tissues. Furthermore, tumor resection was successfully performed under the guidance of the ICG-Herceptide-based NIR-II imaging in subcutaneous SKOV3 mice models. The biocompatibility study indicated that the probe had no observable toxicity to cells and tissues. Overall, these results demonstrate that ICG-Herceptide is a promising optical probe for the diagnosis and localization of HER2-overexpressing tumors. Moreover, Herceptide is a novel HER2-targeting peptide and can be further used for developing theranostic agents.
WOS关键词HER2 EXPRESSION ; BREAST-CANCER ; THERAPY
WOS研究方向Research & Experimental Medicine ; Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000927727500001
出版者AMER CHEMICAL SOC
源URL[http://119.78.100.183/handle/2S10ELR8/309704]  
专题新药研究国家重点实验室
通讯作者Shi, Hui; Liu, Hongguang; Cheng, Zhen
作者单位1.Bohai Rim Adv Res Inst Drug Discovery, Shandong Lab Yantai Drug Discovery, Yantai 264117, Shandong, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Mat Med, Mol Imaging Ctr, State Key Lab Drug Res, Shanghai 201203, Peoples R China;
3.Northeastern Univ, Inst Mol Med, Coll Life & Hlth Sci, Shenyang 110167, Peoples R China;
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Cao, Rui,Li, Renda,Shi, Hui,et al. Novel HER2-Targeted Peptide for NIR-II Imaging of Tumor[J]. MOLECULAR PHARMACEUTICS,2023,20(2):1394-1403.
APA Cao, Rui,Li, Renda,Shi, Hui,Liu, Hongguang,&Cheng, Zhen.(2023).Novel HER2-Targeted Peptide for NIR-II Imaging of Tumor.MOLECULAR PHARMACEUTICS,20(2),1394-1403.
MLA Cao, Rui,et al."Novel HER2-Targeted Peptide for NIR-II Imaging of Tumor".MOLECULAR PHARMACEUTICS 20.2(2023):1394-1403.

入库方式: OAI收割

来源:上海药物研究所

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