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亲和体分子:癌症治疗分子靶点体内成像的潜力。

Affibody molecules: potential for in vivo imaging of molecular targets for cancer therapy.

作者信息

Tolmachev Vladimir, Orlova Anna, Nilsson Fredrik Y, Feldwisch Joachim, Wennborg Anders, Abrahmsén Lars

机构信息

Affibody AB, Box 20137, SE-161 02 Bromma, Swedenn.

出版信息

Expert Opin Biol Ther. 2007 Apr;7(4):555-68. doi: 10.1517/14712598.7.4.555.

Abstract

Targeting radionuclide imaging of tumor-associated antigens may help to select patients who will benefit from a particular biological therapy. Affibody molecules are a novel class of small (approximately 7 kDa) phage display-selected affinity proteins, based on the B-domain scaffold of staphylococcal protein A. A large library (3 x 10(9) variants) has enabled selection of high-affinity (up to 22 pM) binders for a variety of tumor-associated antigens. The small size of Affibody molecules provides rapid tumor localization and fast clearance from nonspecific compartments. Preclinical studies have demonstrated the potential of Affibody molecules for specific and high-contrast radionuclide imaging of HER2 in vivo, and pilot clinical data using indium-111 and gallium-68 labeled anti-HER2 Affibody tracer have confirmed its utility for radionuclide imaging in cancer patients.

摘要

针对肿瘤相关抗原的放射性核素成像可能有助于筛选出能从特定生物疗法中获益的患者。亲和体分子是一类新型的小(约7 kDa)噬菌体展示筛选的亲和蛋白,基于葡萄球菌蛋白A的B结构域支架。一个大型文库(3×10⁹个变体)已能够筛选出针对多种肿瘤相关抗原的高亲和力(高达22 pM)结合剂。亲和体分子的小尺寸使其能够快速在肿瘤中定位,并从非特异性区域快速清除。临床前研究已证明亲和体分子在体内对HER2进行特异性和高对比度放射性核素成像的潜力,使用铟-111和镓-68标记的抗HER2亲和体示踪剂的初步临床数据已证实其在癌症患者放射性核素成像中的效用。

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