Volume 27 Issue 5
Oct.  2003
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Citation:

The reasearch status quo of tumor integrin αvβ3 receptor scintigraphy

  • Received Date: 2002-12-17
  • Integrin αvβ3 receptor is not only expressed on cells surface of many malignant tumors with higher level,but expressed on the neovasculature endothelial cell membrane in malignant tumor tissue with extremely high density and has no expression or cannot be detected in mature vascular endothelial cell and most of the normal organic system.The small molecul cyclic peptides containing RGD motif is an effective antagonist for αvβ3 receptor,which have height selectivity and affinity bind to αvβ3 receptor and is one kind of potential tumor receptor imaging agnet.
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  • [1] Behr TM, Gotthardt M, Barth A, et al. Imaging tumors with peptide-based radioligands[J]. Q J Nucl Med, 2001, 45(2): 189-200.
    [2] Janson ET, Westlin JE, Ohrvall U, et al. Nuclear localization of 111In after intravenous injection of [111In-DTPA-D-Phel]-octreotide in patients with neuroendocrine tumors[J]. J Nucl Med, 2000, 41(9): 1514-1518.
    [3] Folkman J. Addressing tumor blood vessels[J]. Nature Biotechnol, 1997, 15(6): 510.
    [4] Buerkle MA,Pahernik SA, Sutter A, et al. Inhibition of the alpha-nuintegrins with a cyclic RGD peptide impairs angiogenesis, growth and metastasis of solid tumours in vivo[J].Br J Cancer, 2002, 86(5): 788-795.
    [5] Koivunen E, Wang B, Ruoslahti E. Phage libraries displaying cyclic peptides with different ring sizes: ligand specificities of the RGD-directed integrins[J]. Biotechnol N Y, 1995, 13(3): 265-270.
    [6] Brower V. Tumor angiogenesis-new drugs on the block[J].Nat Biotechnol, 1999, 17: 963-968.
    [7] Roland H, Hans JW, Ute R, et al. Radiolabeled αvβ3 integrin antagonists: A new class of tracers for tumor targeting[J]. J Nucl Med, 1999, 40: 1061-1071.
    [8] Su ZF, Liu G, Gupta S, et al. In vitro and in vivo evaluation of a Technetium-99m-labeled cycyclic RGD peptide as a specific marker of alpha (V)beta (3) integrin for tumor imaging[J]. Bioconjug Chem, 2002, 13(3): 561-570.
    [9] Bock M, Bruchertseifer F, Haubner R, et al. 99Tc-m 188Re-and 90Y-labeled αvβ3 antagonists: promising tracer for tumor induced angiogenesis[J]. J Nucl Med, 2000, 41(5, suppl): 41.
    [10] Roland H, Hans JW, Wolfgang A, et al. Noninvasive imaging of αvβ3 integrin expression using 18F-labeled RGD-contining glycopeptide and positron emission tomography[J]. Canner Res, 2001, 61: 1781-1785.
    [11] Sivolapenko GB, skarlos D, Pectasides D, et al. Imaging of metastatic melanoma utilising a technetium-99m-labelled RGD-containing synthetic peptide[J]. Eur J Nucl Med, 1998, 25: 1383-1389.
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The reasearch status quo of tumor integrin αvβ3 receptor scintigraphy

  • Nuclear Medicine Center, Southest Hospital, Third Military Medical University, Chongqing 400038, China

Abstract: Integrin αvβ3 receptor is not only expressed on cells surface of many malignant tumors with higher level,but expressed on the neovasculature endothelial cell membrane in malignant tumor tissue with extremely high density and has no expression or cannot be detected in mature vascular endothelial cell and most of the normal organic system.The small molecul cyclic peptides containing RGD motif is an effective antagonist for αvβ3 receptor,which have height selectivity and affinity bind to αvβ3 receptor and is one kind of potential tumor receptor imaging agnet.

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