Nuclear Medicine and Biology
Volume 38, Issue 1 , Pages 113-120 , January 2011

Neurotensin(8–13) analogue: radiolabeling and biological evaluation using different chelators

Received 6 October 2009 ,Revised 1 June 2010 ,Accepted 14 June 2010.

References 

  1. Shuang L. Bifunctional coupling agents for radiolabeling of biomolecules and target-specific delivery of metallic radionuclides. Adv Drug Deliv Rev. 2008;60(12):1347–1370
  2. Vanderheyden J, Liu G, He J, Patel B, Tait JF, Hnatowich DJ. Evaluation of 99mTc-MAG3-annexin V: influence of the chelate on in vitro and in vivo properties in mice. Nucl Med Biol. 2006;33:135–144
  3. Mardirossian G, Wu C, Ruscowski M, Hantowich DJ. The stability of technetium-99m directly labeled to a Fab′ antibody via stannous ion and mercaptoethanol reduction. Nucl Med Commun. 1992;13:503–512
  4. Zhang YM, Liu N, Zhu ZH, Ruscowski M, Hnatowich DJ. Influence of different chelators (HYNIC, MAG3 AND DTPA) on tumor cell accumulation and mouse biodistribution of technetium-99m labeled to antisense DNA. Eur J Nucl Med. 2000;27:1700–1707
  5. Abrams MJ, Juweid M, tenKate CI, Schwartz DA, Hauser MM, Gaul FE, et al. Technetium-99m-human polyclonal IgG radiolabeled via the hydrazino nicotinamide derivative for imaging focal sites of infection in rats. J Nucl Med. 1990;31:2022–2028
  6. Biechlin M, Bonmrtin A, Gilly F, Fraysse M, d'Hardemare AM. Radiolabeling of annexin A5 with 99mTc: comparison of HYNIC-TC vs iminothiolane-Tc-tricarbonyl conjugates. Nucl Med and Biol. 2008;35:679–687
  7. Ono M, Arano Y, Uehara T, Fujioka Y, Ogawa K, Namba S, et al. Intracellular metabolic fate of radioactivity after injection of technetium-99m-labeled hydrazino nicotinamide derivatized proteins. Bioconjug Chem. 1999;10:386–394
  8. Liu S, Edwards DS, Looby RJ, Harris AR, Poirer MJ, Barrett JA, et al. Labeling a hydrazino nicotinamide-modified cyclic IIb/IIa receptor antagonist with 99mTc using aminocarboxylates as coligands. Bioconjug Chem. 1996;7:63–71
  9. Liu S, Edwards DS, Harris AR. A novel ternary ligand system for 99mTc-labeling of hydrazino nicotinamide modified biologically active molecules using imine-N-containing heterocycles as coligands. Bioconjug Chem. 1998;9:583–595
  10. Noll B, Johannsen B, May K, Spies H. Preparation of the renal function imaging agent 99mTc-MAG3 starting from S-unprotected mercaptoacetyltriglycine. Appl Radiat Isot. 1992;43(7):899–901
  11. Duncan RJS, Weston PD, Wrigglesworth R. A new reagent which may be used to introduce sulfhydryl-groups into proteins, and its use in the preparation of conjugates for immunoassay. Anal Biochem. 1983;132:68–73
  12. Winnard P, Chang F, Ruscowski M, Mardirossian G, Hnatowic DJ. Preparation and use of NHS-MAG3 for technetium-99m labeling of DNA. Nucl Med Biol. 1997;24:425–432
  13. Okarvi SM. Peptides-based radiopharmaceuticals and cytotoxic conjugates: potential tools against cancer. Cancer Treat Rev. 2008;34(1):13–26
  14. Fichna J, Janecka A. Synthesis of target-specific radiolabeled peptides for diagnostic imaging. Bioconjug Chem. 2003;14:3–17
  15. Garcia-Garayoa E, Ruegg D, Blauesntein P, Zwimpfer M, Khan IU, Maes V, et al. Chemical and biological characterization of new Re(CO)3/[99mTc](CO)3 bombesin analogues. Nucl Med Biol. 2007;34:17–28
  16. Carraway RE, Leeman SE. The isolation of a new hypotensive peptide, neurotensin, from bovine hypothalami. J Biol Chem. 1973;248:6854–6861
  17. Nock BA, Nikolopoulou A, Reubi J, Maes V, Conrath P, Tourwe D, et al. Toward stable N4-modified neurotensins for NTS1-receptor-targeted tumor imaging with 99mTc. J Med Chem. 2006;49:4767–4776
  18. Granier C, van Rietschoten J, Kitabgi P, Poustis C, Freychet P. Synthesis and characterization of neurotensin analogues for structure/activity relationship studies — acetyl-neurotensin-(8–13) is the shortest analogue with full binding and pharmacological activities. Eur J Biochem. 1982;124:117–125
  19. Garcia-Garayoa E, Maes V, Blauestein P, Blanc A, Hohn A, Tourwe D, et al. Double-stabilized neurotensin analogues as potential radiopharmaceuticals for NTR-positive tumors. Nucl Med Biol. 2006;33:495–503
  20. La Bella R, Garcia-Garayoa E, Langer M, Blauenstein P, Beck-Sickinger AG, Schubiger PA. In vitro and in vivo evaluation of a 99mTc(I)-labeled bombesin analogue for imaging of gastrin releasing peptide receptor-positive tumors. Nucl Med Biol. 2002;29:553–560
  21. Faintuch BL, Teodoro R, Duatti A, Muramoto E, Faintuch S, Smith CJ. Radiolabeling bombesin analogs for prostate cancer diagnosis: preclinical studies. Nucl Med Biol. 2008;35(4):401–411
  22. Wang Y, Liu G, Hnatowich DJ. Methods for MAG3 conjugation and 99mTc radiolabeling of biomolecules. Nature Protocols. 2006;1(3):1477–1480
  23. Buchegger F, Bonvin F, Kosinski M, Schaffland AO, Prior J, Reubi JC, et al. Radiolabeled neurotensin analog, 99mTc-NT-XI, evaluated in ductal pancreatic adenocarcinoma patients. J Nucl Med. 2003;44(10):1649–1654
  24. Carraway RE, Plona AM. Involvement of NT in cancer growth evidences, mechanisms and development of diagnostic tolls. Peptides. 2006;27(10):2445–2460
  25. Somai S, Gompel A, Rostene W, Forgez P. Neurotensin counteracts apoptosis in breast cancer cells. Biochem Biophys Res Commun. 2002;295:482–488
  26. Einsiedel J, Hubner H, Hervt M, Harterich S, Koschatzky S, Gmeiner P. Peptide backbone modifications on the C-terminal hexapeptide of neurotensin. Bioorg Med Chem Lett. 2008;18(6):2013–2018
  27. Garcia-Garayoa E, Allemann-Tannahill L, Blauenstein P, Willmann M, Carrel-Remy N, Tourwe D, et al. In vitro and in vivo evaluation of new radiolabeled neurotensin(8–13) analogues with high affinity for NT1 receptors. Nucl Med Biol. 2001;28:75–84
  28. Hultsch C, Pawelke B, Bergmann R, Wuest F. Synthesis and evaluation of novel multimeric neurotensin(8–13) analogs. Bioorg Med Chem. 2006;14:5913–5920
  29. Liu G, Wescott C, Sato A, Wang Y, Liu N, Zhang Y, et al. Nitriles form mixed-coligand complexes with 99mTc-HYNIC-peptide. Nucl Med Biol. 2002;29:107–113
  30. Lei K, Ruscowsky M, Chang F, Qu T, Mardirossian G, Hnatowich DJ. Technetium-99m antibodies labeled with MAG3 and HYNIC — an in vitro and animal in vivo properties. Nucl Med Biol. 1996;23:917–922
  31. Verbke K, Hjeslstuden O, Debrock E, Cleythens B, De Roo M, Verbruggen A. Comparative evaluation of 99mTc-HYNIC-HAS and 99mTc-MAG3-HAS as possible blood poll agents. Nucl Med Comm. 1995;16:942–957
  32. Ono M, Arano Y, Mukai T, Uehara T, Fujioka Y, Ogawa K, et al. Plasma protein binding of 99mTc-labeled hydrazino nicotinamide derivatized polypeptides and peptides. Nucl Med Biol. 2000;28(2):155–164
  33. Decristoforo C, Mather SJ. The influence of chelator on the pharmacokinetics of 99mTc-labelled peptides. Q. J. Nucl. Med. 2002;46:195–205
  34. Decristoforo C, Faintuch BL, Rey A, von Guggenberg E, Rupprich M, Hernandez-Gonzales I, et al. [99mTc]HYNIC-RGD for imaging integrin avb3 expression. Nucl. Med. Biol. 2006;33:945–952

PII: S0969-8051(10)00324-0

doi: 10.1016/j.nucmedbio.2010.06.011

Nuclear Medicine and Biology
Volume 38, Issue 1 , Pages 113-120 , January 2011

Article Tools

* Image Usage & Resolution