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Radioiodinated bicyclic RGD peptide for imaging integrin αvβ3 in cancers.
Biochemical and Biophysical Research Communications ( IF 2.5 ) Pub Date : 2020-05-22 , DOI: 10.1016/j.bbrc.2020.05.106
Naoya Kondo 1 , Keita Wakamori 1 , Masahiko Hirata 1 , Takashi Temma 1
Affiliation  

Integrin αvβ3 is an effective marker of angiogenesis in cancer, and αvβ3-specific imaging can yield important details about this complex physiological process. We utilized the recently reported and highly αvβ3-specific peptide, bicyclic RGD (bcRGD), as the basic structure of an in vivo αvβ3 imaging probe, and synthesized a radioiodinated form of bcRGD, namely [125I]bcRGD, with high radiochemical purity (>99%) and high molar activity (81 GBq/μmol). As expected, [125I]bcRGD exhibited high selectivity for αvβ3 compared with αvβ5 and α5β1 in vitro. [125I]bcRGD showed significantly higher accumulation in U-87MG cells (1.6% dose/mg) with high expression of αvβ3 compared to A549 cells (0.3% dose/mg) with only moderate expression. Furthermore, 30 min after administration to tumor-bearing mice, [125I]bcRGD showed significantly higher accumulation in U-87MG tumors (3.8% ID/g) than in A549 tumors (2.1% ID/g), and the radioactivity accumulation ratios of U-87MG tumor/blood and U-87MG tumor/muscle were 4.0 and 6.0, respectively. These results highlight the promising properties of [123/125I]bcRGD for use as an in vivo αvβ3 imaging probe, as well as the utility of bcRGD as a basic structure of molecular probes for both imaging and therapeutic applications. bcRGD may exhibit broad use in future theranostics applications targeting integrin αvβ3-related diseases.



中文翻译:

放射性碘双环RGD肽,用于在癌症中成像整合素αvβ3。

整合素α v β 3是在癌症的血管生成的有效标记,α v β 3特异性成像可以产生关于这个复杂的生理过程的重要细节。我们利用最近报道和高度α v β 3特异性肽,双环RGD(bcRGD),作为一个基本结构体内α v β 3成像探头,并合成bcRGD的放射性碘标记的形式,即[ 125 I] bcRGD ,具有高放射化学纯度(> 99%)和高摩尔活性(81 GBq /μmol)。如所预期的,[ 125 I]显示出bcRGD高选择性α v β 3与α相比v β 5和α 5 β 1 在体外。[ 125 I] bcRGD显示以U-87MG细胞与α的高表达显著更高积累(1.6%剂量/毫克)v β 3相比A549细胞(0.3%剂量/毫克)与仅中度表达。此外,在对荷瘤小鼠给药后30分钟,[ 125 I] bcRGD在U-87MG肿瘤(3.8%ID / g)中的蓄积明显高于在A549肿瘤(2.1%ID / g)中的蓄积,并且放射性蓄积率U-87MG肿瘤/血液和U-87MG肿瘤/肌肉的分别为4.0和6.0。这些结果突出了[ 123/125I] bcRGD用作体内α v β 3的成像探头,以及bcRGD作为分子探针的用于成像和治疗应用中的基本结构的实用程序。bcRGD可以表现出在未来治疗诊断学应用靶向整合素α广泛使用v β 3种相关疾病。

更新日期:2020-05-22
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