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学科主题: 公共卫生
题名:
Tc-99m-Labeled Dimeric Octreotide Peptide: A Radiotracer with High Tumor Uptake for Single-Photon Emission Computed Tomography Imaging of Somatostatin Receptor Subtype 2-Positive Tumors
作者: Dong, Chengyan1,2; Zhao, Huiyun1,3; Yang, Sujuan1,2; Shi, Jiyun1,3; Huang, Jinming1,2; Cui, Liyang1,2; Zhong, Lijun3; Jin, Xiaona4; Li, Fang4; Liu, Zhaofei1,2; Jia, Bing1,2; Wang, Fan1,2
关键词: [Tyr(3)]octreotide ; dimer ; SSTR2-positive tumor ; Tc-99m ; SPECT
刊名: MOLECULAR PHARMACEUTICS
发表日期: 2013-08-01
DOI: 10.1021/mp400040z
卷: 10, 期:8, 页:2925-2933
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Medicine, Research & Experimental ; Pharmacology & Pharmacy
研究领域[WOS]: Research & Experimental Medicine ; Pharmacology & Pharmacy
关键词[WOS]: GLIOMA INTEGRIN-ALPHA(V)BETA(3) EXPRESSION ; TETRAMERIC RGD PEPTIDE ; RADIOLABELED PEPTIDES ; RADIONUCLIDE THERAPY ; BREAST-CANCER ; INTEGRIN ; ANALOG ; MICROPET ; RADIOPHARMACEUTICALS ; PHARMACOKINETICS
英文摘要:

There is growing interest in the development of radiolabeled multivalent ligands because of their higher tumor uptake versus that of the corresponding monomer. This report presents the synthesis of a [Tyr(3)]octreotide dimer conjugate, HYNIC-E([Tyr(3)]octreotide)(2) {HYNIC-TOC2, HYNIC = 6-[2-(2-sulfonatobenzaldehyde)hydrazono]nicotiny1}, and its biological evaluation in the AR42J tumor model. The binding affinity of HYNIC-TOC2 for somatostatin receptor subtype 2 (SSTR2) was determined in AR42J rat pancreatic cancer cells, using I-125-[Tyr(3)]octreotide as the radiotracer. Tc-99m-HYNIC-TOC2 was prepared by using tricine and EDDA as coligands (EDDA =- ethylenediamine-N,N′ -diacetic acid). Biodistribution and gamma imaging were performed in nude mice bearing AR42J tumors. Tc-99m-HYNIC-TOC2 was obtained in >95% labeling yield with favorable stability. Compared with those of HYNIC-TOC (IC50 = 3.74 +/- 0.82 nM), HYNIC-TOC2 showed significantly increased SSTR2 binding affinity (IC50 = 0.74 +/- 0.19 nM), and Tc-99m-HYNIC-TOC2 showed significantly increased tumor uptake [13.31 +/- 3.14%ID/g vs 5.32 +/- 0.94%ID/g 1 h postinjection (p.i.) and 12.05 +/- 2.92%ID/g vs 5.87 +/- 1.96%ID/g 4 h p.i.] Although the level of accumulation of (TcHYNIC)-Tc-99m-TOC2 in kidneys was significantly increased (94.40 +/- 6.51%ID/g vs 32.27 +/- 4.51%ID/g 1 h p.i.), this high uptake was inhibited by the injection of 1.-lysine before the administration of Tc-99m-HYNIC-TOC2 (30.99 +/- 5.05%ID/g 1 h p.i.) while tumor uptake decreased only slightly. Consistent with biodistribution data, in vivo planar y imaging showed that the tumors were clearly visualized, while the background signal was much weaker except for that of the kidneys and bladder. The new radiotracer Tc-99m-HYNIC-TOC2 with a higher binding affinity and good stability was designed and evaluated. The higher tumor uptake of Tc-99m-HYNIC-TOC2 suggests that Y-90/Lu-177-labeled TOC2 might have an advantage for the radiotherapy of SSTR2-positive tumors. These data merit the translation of Tc-99m-HYNIC-TOC2 to a clinical setting.

语种: 英语
所属项目编号: 81125011 ; 2011CB707703 ; 2013CB733802 ; 81000625 ; 30930030 ; 81222019 ; 30900373 ; 81201127 ; 81028009 ; 2011YQ030114 ; 2012ZX09102301-018 ; 2012BAK25B03-16 ; 31300 ; BMU20110263 ; 7132123 ; 7132131 ; Z121107002512010
项目资助者: Outstanding Youth Fund ; "973" projects ; National Natural Science Foundation of China (NSFC) ; Ministry of Science and Technology of China ; Ministry of Education of China ; Beijing Natural Science Foundation ; Beijing Nova Program
WOS记录号: WOS:000322863200010
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/57234
Appears in Collections:北京大学医药卫生分析中心_期刊论文

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作者单位: 1.Peking Univ, Med Isotopes Res Ctr, Beijing 100191, Peoples R China
2.Peking Univ, Sch Basic Med Sci, Dept Radiat Med, Beijing 100191, Peoples R China
3.Peking Univ, Med & Hlth Analyt Ctr, Beijing 100191, Peoples R China
4.Beijing Union Med Coll Hosp, Dept Nucl Med, Beijing 100857, Peoples R China

Recommended Citation:
Dong, Chengyan,Zhao, Huiyun,Yang, Sujuan,et al. Tc-99m-Labeled Dimeric Octreotide Peptide: A Radiotracer with High Tumor Uptake for Single-Photon Emission Computed Tomography Imaging of Somatostatin Receptor Subtype 2-Positive Tumors[J]. MOLECULAR PHARMACEUTICS,2013,10(8):2925-2933.
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