Haubner R, Wester H J, Weber W A, Mang C, Ziegler S I, Goodman S L, Senekowitsch-Schmidtke R, Kessler H, Schwaiger M
Department of Nuclear Medicine, Technische Universität München, Germany.
Cancer Res. 2001 Mar 1;61(5):1781-5.
The alpha(v)beta3 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 alpha(v)beta3, alpha(v)beta5, and alpha(IIb)beta3 as well as in vivo studies using alpha(v)beta3-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 alpha(v)beta3 integrin status and therapy monitoring.
α(v)β3整合素是一种重要的细胞粘附受体，参与肿瘤诱导的血管生成和肿瘤转移。在此，我们描述了用4-硝基苯基2-[18F]氟丙酸对含RGD的糖肽环(-Arg-Gly-Asp-D-Phe-Lys(糖氨基酸)-)进行18F标记，并在体外和肿瘤小鼠模型中对该化合物进行评估。与分离的固定化α(v)β3、α(v)β5和α(IIb)β3进行结合测定，以及使用α(v)β3阳性和阴性小鼠及异种移植人肿瘤进行体内研究，结果表明放射性标记糖肽具有受体特异性结合，产生高肿瘤：背景比值（例如，注射后120分钟：肿瘤：血液，27.5；肿瘤：肌肉，10.2）。使用小动物正电子发射断层扫描仪的首次成像结果表明，该化合物适用于α(v)β3整合素状态的无创测定和治疗监测。
