Synthesis of Tc-99m labeled glucosamino-Asp-cyclic(Arg-Gly-Asp-D-Phe-Lys) as a potential angiogenesis imaging agent

초록

Angiogenesis imaging agents for single photon emission computed tomography ( SPECT) play a role in diagnosing tumor-induced angiogenesis as well as tumor metastasis. We synthesized and evaluated radiolabeled RGD glycopeptides by incorporation of the [Tc-99m(CO)(3)(H2O)(3)](+) center dot Tc-99m labeled glucosamino-D-c(RGDfK) ([Tc-99m]2) was prepared in 90-93% radiochemical yields (decay corrected). In vitro cell binding assays demonstrated selective binding [Tc-99m]2 to human umbilical vein endothelial ( HUVE) cells, with inhibition of binding to 37.3% of control levels by 10 mu M of cold authentic compounds. In addition, [Tc-99m]2 was shown to have high binding affinity to purified alpha(v)beta(3) integrin (IC50 = 1.5 nM). These results suggest that these radiolabeled RGD glycopeptides may have value for non-invasive assessment of angiogenesis. (c) 2007 Elsevier Ltd. All rights reserved.

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