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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
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
2013-08-01
DOI10.1021/mp400040z
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
WOS记录号WOS:000322863200010
引用统计
被引频次:8[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/57234
专题北京大学医药卫生分析中心
北京大学基础医学院
北京大学医药卫生分析中心_研发办公室
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
推荐引用方式
GB/T 7714
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.
APA Dong, Chengyan.,Zhao, Huiyun.,Yang, Sujuan.,Shi, Jiyun.,Huang, Jinming.,...&Wang, Fan.(2013).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.MOLECULAR PHARMACEUTICS,10(8),2925-2933.
MLA Dong, Chengyan,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".MOLECULAR PHARMACEUTICS 10.8(2013):2925-2933.
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