当前位置：
X-MOL 学术
›
Bioconjugate Chem.
›
论文详情
Our official English website, www.x-mol.net, welcomes your
feedback! (Note: you will need to create a separate account there.)
Cucurbituril–Ferrocene: Host–Guest Based Pretargeted Positron Emission Tomography in a Xenograft Model
Bioconjugate Chemistry ( IF 4.0 ) Pub Date : 2021-06-22 , DOI: 10.1021/acs.bioconjchem.1c00280 Vilma I J Jallinoja 1, 2 , Brandon D Carney 1, 2 , Meiying Zhu 1 , Kavita Bhatt 2 , Paul J Yazaki 3 , Jacob L Houghton 1, 2
Bioconjugate Chemistry ( IF 4.0 ) Pub Date : 2021-06-22 , DOI: 10.1021/acs.bioconjchem.1c00280 Vilma I J Jallinoja 1, 2 , Brandon D Carney 1, 2 , Meiying Zhu 1 , Kavita Bhatt 2 , Paul J Yazaki 3 , Jacob L Houghton 1, 2
Affiliation
|
Pretargeted positron emission tomography is a macromolecule-driven nuclear medicine technique that involves targeting a preadministered antigen target-bound macromolecule with a radioligand in vivo, aiming to minimize the overall radiation dose. This study investigates the use of antibody based host–guest chemistry methodology for pretargeted positron emission tomography. We hypothesize that the novel pretargeting approach reported here overcomes the challenges the current pretargeting platforms have with the in vivo stability and modularity of the pretargeting components. A cucurbit[7]uril host molecule modified, anti-carcinoembryonic antigen antibody (M5A; CB7-M5A) and a 68Ga-radiolabeled ferrocene guest radioligand ([68Ga]Ga-NOTA-PEG3-NMe2-Fc) were studied as potential host–guest chemistry pretargeting agents for positron emission tomography in BxPC3 xenografted nude mice. The viability of the platform was studied via in vivo biodistribution and positron emission tomography. Tumor uptake of [68Ga]Ga-NOTA-PEG3-NMe2-Fc was significantly higher in mice which received CB7-M5A prior to the radioligand injection (pretargeted) (3.3 ± 0.7%ID/g) compared to mice which only received the radioligand (nonpretargeted) (0.2 ± 0.1%ID/g).
中文翻译：
葫芦脲-二茂铁：异种移植模型中基于主客体的预靶向正电子发射断层扫描
预靶向正电子发射断层扫描是一种大分子驱动的核医学技术，涉及在体内用放射性配体靶向预先施用的抗原靶结合大分子，旨在最大限度地减少总辐射剂量。本研究研究了基于抗体的主客体化学方法在预靶向正电子发射断层扫描中的应用。我们假设这里报道的新型预靶向方法克服了当前预靶向平台在预靶向成分的体内稳定性和模块化方面所面临的挑战。研究了葫芦[7]尿素宿主分子修饰的抗癌胚抗原抗体（M5A；CB7-M5A）和68 Ga 放射性标记的二茂铁客体放射性配体（[ 68 Ga]Ga-NOTA-PEG 3 -NMe 2 -Fc）作为 BxPC3 异种移植裸鼠正电子发射断层扫描的潜在主客体化学预靶向剂。通过体内生物分布和正电子发射断层扫描研究了该平台的可行性。与仅注射放射性配体的小鼠相比，在注射放射性配体（预先靶向）之前接受CB7-M5A的小鼠的[ 68 Ga]Ga-NOTA-PEG 3 -NMe 2 -Fc的肿瘤摄取显着更高（3.3±0.7%ID/g）接受放射性配体（非预定位）（0.2 ± 0.1%ID/g）。
更新日期：2021-08-19
中文翻译：
葫芦脲-二茂铁：异种移植模型中基于主客体的预靶向正电子发射断层扫描
预靶向正电子发射断层扫描是一种大分子驱动的核医学技术，涉及在体内用放射性配体靶向预先施用的抗原靶结合大分子，旨在最大限度地减少总辐射剂量。本研究研究了基于抗体的主客体化学方法在预靶向正电子发射断层扫描中的应用。我们假设这里报道的新型预靶向方法克服了当前预靶向平台在预靶向成分的体内稳定性和模块化方面所面临的挑战。研究了葫芦[7]尿素宿主分子修饰的抗癌胚抗原抗体（M5A；CB7-M5A）和68 Ga 放射性标记的二茂铁客体放射性配体（[ 68 Ga]Ga-NOTA-PEG 3 -NMe 2 -Fc）作为 BxPC3 异种移植裸鼠正电子发射断层扫描的潜在主客体化学预靶向剂。通过体内生物分布和正电子发射断层扫描研究了该平台的可行性。与仅注射放射性配体的小鼠相比，在注射放射性配体（预先靶向）之前接受CB7-M5A的小鼠的[ 68 Ga]Ga-NOTA-PEG 3 -NMe 2 -Fc的肿瘤摄取显着更高（3.3±0.7%ID/g）接受放射性配体（非预定位）（0.2 ± 0.1%ID/g）。
京公网安备 11010802027423号