Abstract
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.
Footnotes
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The costs of publication of this article were defrayed in part by the payment of page charges. This article must therefore be hereby marked advertisement in accordance with 18 U.S.C. Section 1734 solely to indicate this fact.
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↵1 Supported by Grant 96.017.2 from the Sander-Foundation and in part by the German Reseach Foundation.
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↵2 To whom requests for reprints should be addressed, at Department of Nuclear Medicine, Klinikum rechts der Isar, Technische Universität München, Ismaninger Strasse 22, D-81675 München, Germany. Phone: 49-89-41404554; Fax: 49-89-41404841; E-mail: R.Haubner{at}lrz.tum.de
- Received August 7, 2000.
- Accepted January 12, 2001.
- ©2001 American Association for Cancer Research.
Volume 61, Issue 5
