Molecular Imaging Program at Stanford, Department of Radiology, Stanford University, Stanford, California 94305-5344, USA.
Bioconjug Chem. 2010 May 19;21(5):947-54. doi: 10.1021/bc900515p.
Epidermal growth factor receptor (EGFR) has become an attractive target for cancer molecular imaging and therapy. Affibody proteins against EGFR have been reported, and thus, we were interested in evaluating their potential for positron emission tomography (PET) imaging of EGFR positive cancer. An Affibody analogue (Ac-Cys-Z(EGFR:1907)) binding to EGFR was made through conventional solid phase peptide synthesis. The purified protein was site-specifically coupled with the 1,4,7,10-tetraazacyclododecane-1,4,7-tris-aceticacid-10-maleimidethylacetamide (maleimido-mono-amide-DOTA) to produce the bioconjugate, DOTA-Z(EGFR:1907). (64)Cu labeled probe (64)Cu-DOTA-Z(EGFR:1907) displayed a moderate specific activity (5-8 MBq/nmol, 22-35 microCi/microg). Cell uptake assays by pre-incubating without or with 300 times excess unlabeled Ac-Cys-Z(EGFR:1907) showed high EGFR-specific uptake (20% applied activity at 0.5 h) in A431 epidermoid carcinoma cancer cells. The affinity (K(D)) of (64)Cu-DOTA-Z(EGFR:1907) as tested by cell saturation analysis was 20 nM. The serum stability test showed excellent stability of the probe with >95% intact after 4 h of incubation in mouse serum. In vivo small-animal PET imaging showed fast tumor targeting, high tumor accumulation (approximately 10% ID/g at 1 h p.i.), and good tumor-to-normal tissue contrast of (64)Cu-DOTA-Z(EGFR:1907) spiked with a wide dose range of Ac-Cys-Z(EGFR:1907). Bio-distribution studies further demonstrated that the probe had high tumor, blood, liver, and kidney uptakes, while blood radioactivity concentration dropped dramatically at increased spiking doses. Co-injection of the probe with 500 microg of Ac-Cys-Z(EGFR:1907) for blocking significantly reduced the tumor uptake. Thus, (64)Cu-DOTA-Z(EGFR:1907) showed potential as a high tumor contrast EGFR PET imaging reagent. The probe spiked with 50 microg of Ac-Cys-Z(EGFR:1907) improved tumor imaging contrast which may have important clinical applications.
表皮生长因子受体(EGFR)已成为癌症分子成像和治疗的一个有吸引力的靶点。已经报道了针对 EGFR 的亲和体蛋白,因此,我们有兴趣评估它们在 EGFR 阳性癌症的正电子发射断层扫描(PET)成像中的潜力。通过传统的固相肽合成制备了与 EGFR 结合的亲和体类似物(Ac-Cys-Z(EGFR:1907))。将纯化的蛋白质通过定点与 1,4,7,10-四氮杂环十二烷-1,4,7-三乙酸-10-马来酰亚胺基甲基乙酰胺(马来酰亚胺单酰胺-DOTA)偶联,生成生物缀合物 DOTA-Z(EGFR:1907)。(64)Cu 标记探针(64)Cu-DOTA-Z(EGFR:1907)显示出中等的比活度(5-8 MBq/nmol,22-35 microCi/microg)。通过在没有或用 300 倍过量未标记的 Ac-Cys-Z(EGFR:1907)预孵育的细胞摄取实验,在 A431 表皮样癌细胞中显示出高 EGFR 特异性摄取(0.5 h 时应用活性的 20%)。通过细胞饱和分析测试的(64)Cu-DOTA-Z(EGFR:1907)的亲和力(K(D))为 20 nM。血清稳定性试验表明,该探针在小鼠血清中孵育 4 小时后仍具有优异的稳定性,>95%的完整性。体内小动物 PET 成像显示,(64)Cu-DOTA-Z(EGFR:1907)快速靶向肿瘤,高肿瘤积累(注射后 1 小时约为 10%ID/g),并且与用广泛剂量范围的 Ac-Cys-Z(EGFR:1907)标记的探针具有良好的肿瘤与正常组织对比。生物分布研究进一步表明,该探针具有高肿瘤、血液、肝脏和肾脏摄取,而随着标记剂量的增加,血液放射性浓度急剧下降。用 500μg Ac-Cys-Z(EGFR:1907)共注射进行阻断显著降低了肿瘤摄取。因此,(64)Cu-DOTA-Z(EGFR:1907)作为一种高肿瘤对比度 EGFR PET 成像试剂具有潜力。用 50μg Ac-Cys-Z(EGFR:1907)标记探针可提高肿瘤成像对比度,这可能具有重要的临床应用价值。
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