RT Journal Article
SR Electronic
T1 Noninvasive Imaging of α<sub>v</sub>β<sub>3</sub> Integrin Expression Using <sup>18</sup>F-labeled RGD-containing Glycopeptide and Positron Emission Tomography
JF Cancer Research
JO Cancer Res
FD American Association for Cancer Research
SP 1781
OP 1785
VO 61
IS 5
A1 Haubner, Roland
A1 Wester, Hans-Jürgen
A1 Weber, Wolfgang A.
A1 Mang, Christian
A1 Ziegler, Sibylle I.
A1 Goodman, Simon L.
A1 Senekowitsch-Schmidtke, Reingard
A1 Kessler, Horst
A1 Schwaiger, Markus
YR 2001
UL http://cancerres.aacrjournals.org/content/61/5/1781.abstract
AB The αvβ3 integrin is an important cell adhesion receptor involved in tumor-induced angiogenesis and tumor metastasis. Here we describe the 18F-labeling of the RGD-containing glycopeptide cyclo(-Arg-Gly-Asp-d-Phe-Lys(sugar amino acid)-) with 4-nitrophenyl 2-[18F]fluoropropionate and the evaluation of this compound in vitro and in tumor mouse models. Binding assays with isolated immobilized αvβ3, αvβ5, and αIIbβ3 as well as in vivo studies using αvβ3-positive and -negative murine and xenotransplanted human tumors demonstrated receptor-specific binding of the radiolabeled glycopeptide yielding high tumor:background ratios (e.g., 120 min postinjection: tumor:blood, 27.5; tumor:muscle, 10.2). First imaging results using a small animal positron emission tomograph suggest that this compound is suitable for noninvasive determination of the αvβ3 integrin status and therapy monitoring. ©2001 American Association for Cancer Research.