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用于放射性砹(碘)标记蛋白质的偶联剂SPC的合成及表征 被引量：3

Synthesis and Characterization of SPC as a Linker for Labeling Proteins With Astatine and Iodine Radioisotopes
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摘要 以5-溴烟酸为起始物,通过3步主要反应合成了一种适用于蛋白质放射性砹(碘)标记的偶联剂——5-(三正丁基锡)-3-吡啶甲酸 N-琥珀酰亚胺酯(SPC),并用核磁共振(NMR)、质谱(MS)、高效液相色谱(HPLC)等进行了表征。以该试剂为双功能偶联剂,实现了IgG的^(125)I标记,标记率达30％以上。标记产物在体外具有较高的稳定性。 N-succinimidyl 5-(tributylstannyl)-3-pyridinecarboxylate (SPC), a useful linker for labeling proteins with astatine and iodine radioisotopes, is synthesized in three steps with 5-bromonicotinic acid as a starting material, and is characterized by nuclear magnetic resonance (NMR), mass spectrometer (MS) and high performance liquid chromatography (HPLC). With this bi-functional ester, 125I labeled human IgG is performed in labeling yield of approximately 30%. Also, the in vitro stability of the prepared 125I-IgG is evaluated.
作者 唐军 金建南 刘宁 廖家莉 杨远友
机构地区 四川大学原子核科学技术研究所辐射物理及技术教育部重点实验室
出处 《原子能科学技术》 EI CAS CSCD 2004年第3期261-265,共5页 Atomic Energy Science and Technology
基金 国家自然科学基金(29601104 20171033) 高等学校博士学科点专项科研基金(2003610016)
关键词 偶联剂 放射性砹 合成 表征 蛋白质标记 放射性碘 Astatine High performance liquid chromatography Iodine compounds Mass spectrometers Nuclear magnetic resonance spectroscopy Organic compounds Proteins Radioisotopes
分类号 R817.4 [医药卫生—影像医学与核医学] O625.4 [理学—有机化学]
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参考文献15

  • 1Weinreich R.Molecular Radiotherapy With 211At[M].Amsterdam,Netherlands: Elsevier Science,1997.359～382.
  • 2Zalutsky MR,Bigner DD.Radioimmunotherapy With α-particle-emitting Radioimmunoconjugates[J].Acta Oncol,1996,35:373～379.
  • 3唐军,刘宁,杨远友,金建南.^(211)At标记放射治疗药物进展[J].核技术,2002,25(11):973-979. 被引量：6
  • 4Wilbur DS,Vessella RL,Strany JE,et al.Preparation and Evaluation of para-(211 At) Astatobenzoyl Labeled Antirenal Cell Carcinoma Antibody A6H F(ab')2: In Vivo Distribution Comparison With para-[125 I] Iodobenzaoyl Labeled A6H F(ab')2 [J].Nucl Med Biol,1993,20:917～927.
  • 5Zalutsky MR,Mclendon RE,Garg PK,et al.Radioimmunotherapy of Neoplastic Meningitis in Rats Using an α-particle-emitting Immunoconjugate [J].Cancer Research,1994,54:4 719～4 725.
  • 6Liu Ning,Jin Jiannan,Zhang Shuyuan,et al.Astatine-211 Labeling of a Monoclonal Antibody and Its Fab Fragment: Synthesis,Immunoreactivity and Experimental Therapy[J].J Labeled Compd Radiopharm,1995,36:1 105～1 113.
  • 7Akabani G,McLendon RE,Bigner DD,et al.Microdosimetry of Alpha-particle-emitting 211 At-labeled Monoclonal Antibody(MAb) Using Histological Images of Malignant Brain Tumors [J].J Nucl Med,2000,84.
  • 8Zalutsky MR,Stabin MG,Larsen RH.Tissue Distribution and Radiation Dosimetry of Astatine-211Labeled Chimeric 81C6,an α-particle-emitting Immunoconjugate[J].Nucl Med Biol,1997,24: 255 ～261.
  • 9Vaidyanathan G,Affleck D,Zalutsky MR.Monoclonal Antibody F(ab') 2 Fragment Labeled With Nsuccinimidyl 2,4-dimethoxy-3-halobenzoates: In Vivo Comparison of Iodinated and Astatinated Fragments[J].Nucl Med Biol,1994,21(1) :105～110.
  • 10Yordanov AT,Garmestani K,Zhang M,et al.Preparation and in Vivo Evaluation of Linkers for 211 At Labeling of Humanized Anti-tac [J].Nucl Med Biol,2001,28 :845～856.

二级参考文献2

共引文献5

同被引文献26

  • 1刘振锋,汪勇先,周伟,王丽华,夏姣云,尹端沚.3-正丁基锡-N-琥珀酰亚胺苯甲酸酯的合成及其^(125)I标记[J].同位素,2005,18(3):148-152. 被引量：4
  • 2Pimm M V,Perkin A C,Baldwin R W.Differences in Tumor and Normal Tissue Concentrations of Iodine-and Indium-Labeled Monoclonal Antibody Ⅱ.Biodistribution Studies in Mice With Human Tumor Xenografs[J].Eur J Nucl Med,1985,11:300-304.
  • 3Koizumi M,Endo K,Watanabe Y,et al.Pharmacokinectics of Internally Labeled Monoclonal Antibodies as a Gold Standard:Comparison of Biodistribution of 75 Se-,111 In-,and 125 I-Labeled Monoclonal Antibodies in Osteogenic Sarcoma Xenografts in Nude Mice[J].Cancer Res,1989,49:1 752-1 757.
  • 4Zalusky M R,Narula A S.A Method for the Ra diohalogenation of Proteins Resulting in Decreased Thyroid Uptake of Radioiodine[J].Appl Radiat Isot,1987,38:1 051-1 055.
  • 5Zalusky M R,Narula A S.Radiohalogenation of a Monoclonal Antibody Using a N-Succinimidyl-3-(Tri-n-Butystannyl) Benzoate Intermediate[J].Cancer Res,1988,48:1 446-1 450.
  • 6Wilbur D S,Hadley S W,Hylarides M D,et al.Development of a Stable Radioiodinating Reagent to Label Monoclonal Antibodies for Radiotherapy of Cancer[J].J Nucl Med,1989,30:216-226.
  • 7Khawli L A,Kassis A I.Synthesis of 12I Labeled N-Succinimidyl p-Iodobenzoate for Use in Radiolabeling Antibodies[J].Nucl Med Biol,1989,16:727-733.
  • 8Garg S,Garg P K,Zalusky M R.N-Succinimidyl5-(Trialkylstannyl)-3-Pyridinecarboxlates:a New Class of Reagents for Protein Radioiodination[J].Bioconj Chem,1991,2:50-56.
  • 9Smallridge R C,Burman K D, Ward K E,et al. 3',5'-diiodothyronine to 3'-monoiodothyronine conversion in the fed and fasted rat:enzyme characteristic and evidence for two distinct 5' -deiodinases [J]. Endocrinology, 1981,108 : 2336-2345.
  • 10Koehrle J Aufmkolk M, Rokos H, et al. Rat liver iodothyronine monodeiodinsse: evaluation of the iodothyronine ligand-binding site [J]. J. Biol. Chem., 1986,261:11613-11670.

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原子能科学技术
2004年 第3期

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