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HER2受体的分子成像:在核医学中靶向HER2进行成像与治疗。

Molecular imaging of HER2 receptor: Targeting HER2 for imaging and therapy in nuclear medicine.

作者信息

Miladinova Daniela

机构信息

Medical School, Saints Cyril and Methodis University, Skopje, North Macedonia.

出版信息

Front Mol Biosci. 2023 Mar 2;10:1144817. doi: 10.3389/fmolb.2023.1144817. eCollection 2023.

Abstract

Targeting HER 2 for imaging and therapy in nuclear medicine has been used with a special emphasis on developing more powerful radiopharmaceuticals. Zirconium-89 plays an essential role in immune PET imaging so was used labeled with anti-HER2 antibody (Trastuzumab and Pertuzumab). Also there were attempts with other PET tracers as Cuprum-64 and Galium-68, as well as SPECT radiopharmaceuticals Indium-111 and Technetium- 99m. Regarding antibody pharmacokinetic that is not quite appropriate for imaging acquisition, several smaller molecules with shorter residence times have been developed. These molecules called nanobody, affibody, minibody do not compromize HER2 receptor affinity and specificity. Excess of Trastuzumab do not block the affinity of labeled affibodies. Silica nanoparticles have been conjugated to anti-HER2 antibodies to enable targeting of HER2 expressing cells with potential of drug delivery carry for antitumor agents and b(beta) or a(alfa) emitting radioisotopes commonly used for radionuclide therapy, as Iodine-131, Lutetium-177, Yttrium-90, Rhenium-188 and Thorium-277.

摘要

在核医学中,针对HER 2进行成像和治疗一直特别强调开发更强大的放射性药物。锆-89在免疫PET成像中起着至关重要的作用,因此被用于标记抗HER2抗体(曲妥珠单抗和帕妥珠单抗)。此外,还尝试使用其他PET示踪剂,如铜-64和镓-68,以及SPECT放射性药物铟-111和锝-99m。鉴于抗体的药代动力学不太适合成像采集,已经开发了几种停留时间较短的小分子。这些分子称为纳米抗体、亲和体、微型抗体,它们不会损害HER2受体的亲和力和特异性。过量的曲妥珠单抗不会阻断标记亲和体的亲和力。二氧化硅纳米颗粒已与抗HER2抗体偶联,以实现对表达HER2的细胞的靶向,具有携带抗肿瘤药物和常用于放射性核素治疗的β或α发射放射性同位素(如碘-131、镥-177、钇-90、铼-188和钍-277)进行药物递送的潜力。

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Targeting HER2 in Nuclear Medicine for Imaging and Therapy.核医学中靶向HER2进行成像与治疗
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