PT  - JOURNAL ARTICLE
AU  - Haubner, Roland
AU  - Wester, Hans-Jürgen
AU  - Weber, Wolfgang A.
AU  - Mang, Christian
AU  - Ziegler, Sibylle I.
AU  - Goodman, Simon L.
AU  - Senekowitsch-Schmidtke, Reingard
AU  - Kessler, Horst
AU  - Schwaiger, Markus
TI  - 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
DP  - 2001 Mar 03
TA  - Cancer Research
PG  - 1781--1785
VI  - 61
IP  - 5
4099  - http://cancerres.aacrjournals.org/content/61/5/1781.short
4100  - http://cancerres.aacrjournals.org/content/61/5/1781.full
SO  - Cancer Res2001 Mar 03; 61
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.