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首页> 外文期刊>Cancer biology & therapy >Radiolabeling and biological evaluation of DOTA-Ph-Al derivative conjugated to anti-EGFR antibody ior egf/r3 for targeted tumor imaging and therapy.
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Radiolabeling and biological evaluation of DOTA-Ph-Al derivative conjugated to anti-EGFR antibody ior egf/r3 for targeted tumor imaging and therapy.

机译：结合抗EGFR抗体或egf / r3的DOTA-Ph-A1衍生物的放射性标记和生物学评估，用于靶向性肿瘤成像和治疗。

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An appropriate bifunctional chelating agent namely DOTA-Ph-Al was developed for the conjugation with biological vectors (anti EGFr antibody). We hereby report the synthesis of p-bromoacetamidobenzyl derivative of DOTA and its conjugation to monoclonal antibody anti-EGFR ior egf/r3. Immunoconjugate was prepared by conjugation of p-bromoacetamidobenzyl derivative of DOTA with ior egf/r3. Modified antibody was purified by size exclusion chromatography. DOTA-Ph-Al-ior egf/r3 exhibited quantitative 99mTc-labeling (>96%) with specific activity 10-20 mCi/mg of protein and 90Y-labeling with specific activity 2-5 mCi/mg. Immunoreactivity was determined by flow cytometry. Receptor ligand assay on murine cell line EAT and human tumor cell line U-87MG showed Kd = 2.87 nM and 4.86 nM respectively. The stability in serum indicated that 99mTc remained bound to antibodies up to 24h and 98% 90Y was associated with the mAb for five days. Biodistribution characteristics of Ab-conjugate radiolabeled to 99mTc and 90Y radionuclide was examined in BALB/c mice grafted with EAT and athymic mice with U-87MG cell line demonstrated high tumor uptake with 5.5 +/- 1.3 and 7.85 +/- 1.2%ID/g at four and 24 h for 99mTc- DOTA-Ph-AI-ior egf/r3 in EAT tumors after post injection respectively. Maximal radiotracer uptake peaked 17.6 +/- 2.5%ID/g in EAT tumor and 12.89 +/- 0.66% ID/g in U-87MG tumor at 48h for 90Y. The drug excreted through renal routes as the activity in the kidneys was 13.42 +/- 0.33%ID/g at 1 h and 4.51 +/- 1.2%ID/g at 4 h for 99mTc- DOTA-Ph-Al-ior egf/r3.
机译：开发了一种合适的双功能螯合剂DOTA-Ph-A1，用于与生物载体（抗EGFr抗体）结合。我们据此报道DOTA的对-溴乙酰氨基苄基衍生物的合成及其与单克隆抗体抗EGFR或egf / r3的缀合。通过将DOTA的对-溴乙酰酰胺基苄基衍生物与egr / r3缀合来制备免疫缀合物。通过尺寸排阻色谱法纯化修饰的抗体。 DOTA-Ph-Al-ior egf / r3表现出定量的99mTc标记（> 96％），比活为10-20 mCi / mg蛋白质，90Y-标记的比活为2-5 mCi / mg。通过流式细胞术确定免疫反应性。在鼠细胞系EAT和人肿瘤细胞U-87MG上的受体配体分析分别显示Kd = 2.87 nM和4.86 nM。血清中的稳定性表明，长达24天，99mTc仍与抗体结合，并且98％的90Y与mAb结合5天。在EAT移植的BALB / c小鼠中检查了放射性标记为99mTc和90Y放射性核素的Ab偶联物的生物分布特征，U-87MG细胞系的无胸腺小鼠表现出较高的肿瘤吸收率，分别为5.5 +/- 1.3和7.85 +/- 1.2％ID /注射后分别在EAT肿瘤中分别在4和24 h分别检测EAT肿瘤中的99mTc-DOTA-Ph-AI-ior egf / r3。 90年内，EAT肿瘤中最大放射性示踪剂摄取达到峰值，为17.6 +/- 2.5％ID / g，U-87MG肿瘤为12.89 +/- 0.66％ID / g。对于99mTc-DOTA-Ph-Al-ior egf /，通过肾脏途径排泄的药物在1小时时的肾脏活性为13.42 +/- 0.33％ID / g，在4小时时为4.51 +/- 1.2％ID / g。 r3。

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