Kit formulation for 99mTc-labeling of recombinant Annexin V molecule with a C-terminally engineered cysteine

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• 作者：Chunxiong Lu (1)
  Quanfu Jiang (1)
  Minjin Hu (2)
  Cheng Tan (1)
  Huixin Yu (1)
  Zichun Hua (2) (3)
  
  1. Key Laboratory of Nuclear Medicine ; Ministry of Health ; Jiangsu Key Laboratory of Molecular Nuclear Medicine ; Jiangsu Institute of Nuclear Medicine ; Wuxi ; 214063 ; Jiangsu ; China
  2. Jiangsu Target Pharma Laboratories Inc. ; Changzhou High-Tech Research Institute of Nanjing University ; Changzhou ; 213164 ; Jiangsu ; China
  3. The State Key Laboratory of Pharmaceutical Biotechnology ; Nanjing University ; Nanjing ; 210093 ; China
  
• 关键词：Cys ; Annexin V ; Technetium ; 99m ; Kit ; formulation ; Apoptosis imaging ; Lyophilization
• 刊名：Journal of Radioanalytical and Nuclear Chemistry
• 出版年：2015
• 出版时间：May 2015
• 年：2015
• 卷：304
• 期：2
• 页码：571-578
• 全文大小：1,395 KB
• 参考文献：1. Hofstra, L, Liem, IH, Dumont, EA, Boersma, HH, Heerde, WL, Doevendans, PA, DeMuinck, E, Wellens, HJJ, Kemerink, GJ, Reutelingsperger, CPM, Heidendal, GA (2000) Visualisation of cell death in vivo in patients with acute myocardial infarction. Lancet 356: pp. 209-212 CrossRef
  2. Tait, JF, Gibson, D, Fujikawa, K (1989) Phospholipid binding-properties of human placental anticoagulant protein-I, a member of the lipocortin family. J Biol Chem 264: pp. 7944-7949
  3. Kemerink, GJ, Liu, X, Kieffer, D, Ceyssens, S, Mortelmans, L, Verbruggen, AM, Steinmetz, ND, Vanderheyden, JL, Green, AM, Verbeke, K (2003) Safety, biodistribution, and dosimetry of 99mTc-HYNIC-annexin V, a novel human recombinant annexin V for human application. J Nucl Med 44: pp. 947-952
  4. Toretsky, J, Levenson, A, Weinberg, IN, Tait, JF, Uren, A, Mease, RC (2004) Preparation of F-18 labeled annexin V: a potential PET radiopharmaceutical for imaging cell death. Nucl Med Biol 31: pp. 747-752 CrossRef
  5. Zhu, J-C, Wang, F, Fang, W, Hua, Z-C, Wang, Z-Z (2013) F-18-annexin V apoptosis imaging for detection of myocardium ischemia and reperfusion injury in a rat model. J Radioanal Nucl Chem 298: pp. 1733-1738 CrossRef
  6. Wang, M-W, Zhang, Y-P, Zhang, Y-J, Shen, C (2011) Module-assisted one-pot synthesis of F-18 SFB for radiolabeling proteins. J Radioanal Nucl Chem 289: pp. 191-196 CrossRef
  7. Kurihara, H, Yang, DJ, Cristofanilli, M, Erwin, WD, Yu, DF, Kohanim, S, Mendez, R, Kim, EE (2008) Imaging and dosimetry of 99mTc EC annexin V: preliminary clinical study targeting apoptosis in breast tumors. Appl Radiat Isot 66: pp. 1175-1182 CrossRef
  8. Boersma, HH, Liem, IH, Kemerink, GJ, Thimister, PWL, Hofstra, L, Stolk, LML, Heerde, WL, Pakbiers, MTW, Janssen, D, Beysens, AJ, Reutelingsperger, CPM, Heidendal, GAK (2003) Comparison between human pharmacokinetics and imaging properties of two conjugation methods for Tc-99m-Annexin A5. Br J Radiol. 76: pp. 553-560 CrossRef
  9. Vanderheyden, JL, Liu, G, He, J, Patel, B, Tait, JF, Hnatowich, DJ (2006) Evaluation of 99mTc-MAG3-annexin V: influence of the chelate on in vitro and in vivo properties in mice. Nucl Med Biol 33: pp. 135-144 CrossRef
  10. Saint-Hubert, M, Wang, H, Devos, E, Vunckx, K, Zhou, L, Reutelingsperger, C, Verbruggen, A, Mortelmans, L, Ni, Y, Mottaghy, FM (2011) Preclinical imaging of therapy response using metabolic and apoptosis molecular imaging. Mol Imaging Biol 13: pp. 995-1002 CrossRef
  11. Tait, JF, Brown, DS, Gibson, DF, Blankenberg, FG, Strauss, HW (2000) Development and characterization of annexin V mutants with endogenous chelation sites for (99m)Tc. Bioconjug Chem 11: pp. 918-925 CrossRef
  12. Ye, F, Fang, W, Wang, F, Hua, Z-C, Wang, Z, Yang, X (2011) Evaluation of adenosine preconditioning with Tc-99m-His(10)-annexin V in a porcine model of myocardium ischemia and reperfusion injury: preliminary study. Nucl Med Biol 38: pp. 567-574 CrossRef
  13. Tait, JF, Smith, C, Levashova, Z, Patel, B, Blankenberg, FG, Vanderheyden, JL (2006) Improved detection of cell death in vivo with annexin V radiolabeled by site-specific methods. J Nucl Med 47: pp. 1546-1553
  14. Saint-Hubert, M, Mottaghy, FM, Vunckx, K, Nuyts, J, Fonge, H, Prinsen, K, Stroobants, S, Mortelmans, L, Deckers, N, Hofstra, L, Reutelingsperger, CP, Verbruggen, A, Rattat, D (2010) Site-specific labeling of 鈥榮econd generation鈥?annexin V with 99mTc(CO)3 for improved imaging of apoptosis in vivo. Bioorg Med Chem. 18: pp. 1356-1363 CrossRef
  15. Greupink R, Sio CF, Ederveen A, Orsel J (2009) Evaluation of a Tc-99m-labeled annexin A5 variant for non-invasive SPECT imaging of cell death in liver spleen and prostate. Pharm Res 26:2647鈥?656
  16. Fonge, H, Saint Hubert, M, Vunckx, K, Rattat, D, Nuyts, J, Bormans, G, Ni, Y, Reutelingsperger, C, Verbruggen, A (2008) Preliminary in vivo evaluation of a novel 99mTc-labeled HYNIC-cys-annexin A5 as an apoptosis imaging agent. Bioorg Med Chem Lett 18: pp. 3794-3798 CrossRef
  17. Hua Z, Hu M (2014) Expression, preparation and application of human annexin V variants. China patent. CN102690345A
  18. Lu, C, Jiang, Q, Hu, M, Tan, C, Ji, Y, Yu, H, Hua, Z (2013) Preliminary biological evaluation of novel 99mTc-Cys-annexin A5 as a apoptosis imaging agent. Molecules 18: pp. 6908-6918 CrossRef
  19. Guggenberg, EV, Mikolajczak, R, Janota, B, Riccabona, G, Decristoforo, C (2004) Radiopharmaceutical development of a freeze-dried kit formulation for the preparation of [99mTc-EDDA-HYNIC-D-Phe1, Tyr3]-octreotide, a somatostatin analog for tumor diagnosis. J Pharm Sci-US. 93: pp. 2497-2506 CrossRef
  
• 刊物类别：Chemistry and Materials Science
• 刊物主题：Chemistry
  Nuclear Chemistry
  Physical Chemistry
  Nuclear Physics, Heavy Ions and Hadrons
  Diagnostic Radiology
  Inorganic Chemistry
  
• 出版者：Akad茅miai Kiad贸, co-published with Springer Science+Business Media B.V., Formerly Kluwer Academic
• ISSN：1588-2780

文摘

A new formulation of a freeze-dried kit for the labeling of a novel recombinant Annexin V molecules (with a single cysteine residue at its C-terminal, Cys-Annexin V) with technetium-99m has been developed. Effects of the amount range of Cys-Annexin V, stannous chloride, glucoheptonate and disodium edetate on the radiolabeling yield were studied in details. The stabilities of 99mTc-Cys-Annexin V and freeze-dried kits were performed, respectively. In vitro cell uptake studies showed the binding of 99mTc-Cys-Annexin V was specific on testing with apoptotic H446 cells. Therefore, 99mTc-Cys-Annexin V is a potential apoptosis imaging agent and further study is needed.