Nuclear Medicine and Biology
Volume 33, Issue 8 , Pages 945-952 , November 2006

[99mTc]HYNIC-RGD for imaging integrin αvβ3 expression

  • Clemens Decristoforo

      Affiliations

    • Department of Nuclear Medicine, Medical University of Innsbruck, A-6020 Innsbruck, Austria
    • Corresponding Author InformationCorresponding author. Universitaetsklinik fuer Nuklearmedizin, Anichstrasse 35, A-6020 Innsbruck, Austria. Tel.: +4351250480951; fax: +4351250422659.
    • ,
  • Bluma Faintuch-Linkowski

      Affiliations

    • Radiopharmacy Center Instituto de Pesquisas Energeticas e Nucleares (IPEN), 05508-900 São Paulo, Brazil
    • ,
  • Ana Rey

      Affiliations

    • Cátedra de Radioquímica, Facultad de Química, Universidad de la República, C.P. 11800 Montevideo, Uruguay
    • ,
  • Elisabeth von Guggenberg

      Affiliations

    • Department of Nuclear Medicine, Medical University of Innsbruck, A-6020 Innsbruck, Austria
    • ,
  • Marco Rupprich

      Affiliations

    • Department of Nuclear Medicine, Medical University of Innsbruck, A-6020 Innsbruck, Austria
    • ,
  • Ignacio Hernandez-Gonzales

      Affiliations

    • Centro de Isotopos, Ciudad de la Habana, Cuba
    • ,
  • Teodoro Rodrigo

      Affiliations

    • Radiopharmacy Center Instituto de Pesquisas Energeticas e Nucleares (IPEN), 05508-900 São Paulo, Brazil
    • ,
  • Roland Haubner

      Affiliations

    • Department of Nuclear Medicine, Medical University of Innsbruck, A-6020 Innsbruck, Austria

Received 9 June 2006 ,Revised 4 August 2006 ,Accepted 2 September 2006.

References 

  1. Riccabona G, Decristoforo C. Peptide targeted imaging of cancer. Cancer Biother Radiopharm. 2003;18:675–687
  2. Heppeler A, Froidevaux S, Eberle AN, Maecke HR. Receptor targeting for tumour localisation and therapy with radiopeptides. Curr Med Chem. 2000;7:971–994
  3. Reubi JC. Peptide receptors as molecular targets for cancer diagnosis and therapy. Endocr Rev. 2003;24:389–427
  4. Haubner R, Wester HJ. Radiolabeled tracers for imaging of tumour angiogenesis and evaluation of anti-angiogenic therapies. Curr Pharm Des. 2004;10:1439–1455
  5. Haubner R. αíβ3-Integrin imaging: a new approach to characterize angiogenesis?. Eur J Nucl Med Mol Imaging. 2006;33(Suppl 13):54–63
  6. Felding-Habermann B, Mueller BM, Romerdahl CA, Cheresh DA. Involvement of integrin alpha V gene expression in human melanoma tumourigenicity. J Clin Invest. 1992;89:2018–2022
  7. Aumailley M, Gurrath M, Muller G, Calvete J, Timpl R, Kessler H. Arg–Gly–Asp constrained within cyclic pentapeptides. Strong and selective inhibitors of cell adhesion to vitronectin and laminin fragment P1. FEBS Lett. 1991;291:50–54
  8. Haubner R, Wester HJ, Reuning U, Senekowitsch-Schmidtke R, Diefenbach B, Kessler H, et al. Radiolabeled alpha(v)beta3 integrin antagonists: a new class of tracers for tumour targeting. J Nucl Med. 1999;40:1061–1071
  9. Haubner R, Weber WA, Beer AJ, Vabuliene E, Reim D, Sarbia M, et al. Noninvasive visualization of the activated alphavbeta3 integrin in cancer patients by positron emission tomography and [18F]galacto-RGD. PLoS Med. 2005;2:29
  10. Liu S, Edwards DS. 99mTc-labeled small peptides as diagnostic radiopharmaceuticals. Chem Rev. 1999;99:2235–2268
  11. Decristoforo C, Melendez-Alafort L, Sosabowski JK, Mather SJ. 99mTc-HYNIC-[Tyr3]-octreotide for imaging SST-receptor positive tumours, preclinical evaluation and comparison with 111In-octreotide. J Nucl Med. 2000;41:1114–1119
  12. von Guggenberg E, Behe M, Behr TM, Saurer M, Seppi T, Decristoforo C. 99mTc-labeling and in vitro and in vivo evaluation of HYNIC- and (N alpha-His)acetic acid-modified [d-Glu1]-minigastrin. Bioconjug Chem. 2004;15:864–871
  13. van Hagen PM, Breeman WA, Bernard HF, Schaar M, Mooij CM, Srinivasan A, et al. Evaluation of a radiolabelled cyclic DTPA-RGD analogue for tumour imaging and radionuclide therapy. Int J Cancer. 2000;90:186–198
  14. Decristoforo C, Mather SJ. 99m-Technetium labelled peptide–HYNIC conjugates. The effects of lipophilicity and stability on biodistribution. Nucl Med Biol. 1999;26:389–396
  15. Von Guggenberg E, Sarg B, Lindner H, Melendez L, Alafort SJ, Mather R, et al. Preparation via coligand exchange and characterisation of [99mTc-EDDA-HYNIC-d-Phe1, Tyr3]Octreotide (99mTc-EDDA/HYNIC-TOC). J Lab Comp Radiopharm. 2003;46:307–318
  16. Haubner R, Wester HJ, Weber WA, Mang C, Ziegler SI, Goodman SL, et al. Noninvasive imaging of alpha(v)beta3 integrin expression using 18F-labeled RGD-containing glycopeptide and positron emission tomography. Cancer Res. 2001;61:1781–1785
  17. Sivolapenko GB, Skarlos D, Pectasides D, Stathopoulou E, Milonakis A, Sirmalis G, et al. Related imaging of metastatic melanoma utilising a technetium-99m labelled RGD-containing synthetic peptide. Eur J Nucl Med. 1998;25:1383–1389
  18. Noiri E, Goligorsky MS, Wang GJ, Wang J, Cabahug CJ, Sharma S, et al. Biodistribution and clearance of 99mTc-labeled Arg–Gly–Asp (RGD) peptide in rats with ischemic acute renal failure. J Am Soc Nephrol. 1996;7:2682–2688
  19. Haubner R, Bruchertseifer F, Bock M, Kessler H, Schwaiger M, Wester HJ. Synthesis and biological evaluation of a (99m)Tc-labelled cyclic RGD peptide for imaging the alphavbeta3 expression. Nuklearmedizin. 2004;43:26–32
  20. Su ZF, Liu G, Gupta S, Zhu Z, Rusckowski M, Hnatowich DJ. In vitro and in vivo evaluation of a technetium-99m-labeled cyclic RGD peptide as a specific marker of alpha(V)beta(3) integrin for tumour imaging. Bioconjug Chem. 2002;13:561–570
  21. Weber W, Haubner R. Comment on “In vitro and in vivo evaluation of a technetium-99m-labeled cyclic RGD peptide as a specific marker of alphaVbeta3 integrin for tumour imaging”. Bioconjug Chem. 2003;14:274
  22. Su ZF, He J, Rusckowski M, Hnatowich DJ. In vitro cell studies of technetium-99m labeled RGD-HYNIC peptide, a comparison of tricine and EDDA as co-ligands. Nucl Med Biol. 2003;30:141–149
  23. Janssen M, Oyen WJ, Massuger LF, Frielink C, Dijkgraaf I, Edwards DS, et al. Comparison of a monomeric and dimeric radiolabeled RGD-peptide for tumour targeting. Cancer Biother Radiopharm. 2002;17:641–646
  24. Beer AJ, Haubner R, Goebel M, Luderschmidt S, Spilker ME, Wester HJ, et al. Biodistribution and pharmacokinetics of the alphavbeta3-selective tracer 18F-galacto-RGD in cancer patients. J Nucl Med. 2005;46:1333–1341
  25. Villanueva FS. Molecular images of neovascularization: art for art's sake or form with a function?. Circulation. 2005;111:3188–3191
  26. Hua J, Dobrucki LW, Sadeghi MM, Zhang J, Bourke BN, Cavaliere P, et al. Noninvasive imaging of angiogenesis with a 99mTc-labeled peptide targeted at αvβ3 integrin after murine hindlimb ischemia. Circulation. 2005;111:3255–3260
  27. Pichler BJ, Kneilling M, Haubner R, Braumuller H, Schwaiger M, Rocken M, et al. Imaging of delayed-type hypersensitivity reaction by PET and 18F-galacto-RGD. J Nucl Med. 2005;46:184–189

PII: S0969-8051(06)00188-0

doi: 10.1016/j.nucmedbio.2006.09.001

Nuclear Medicine and Biology
Volume 33, Issue 8 , Pages 945-952 , November 2006

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