整合素αvβ3与肿瘤的分子显像及靶向治疗

lntegrins alpha v beta 3 in molecular imaging and targeted therapy of neoplasms

整合素αvβ3是由2条多肽链组成的跨膜异二聚体糖蛋白。其在正常细胞表面低表达或不表达而在肿瘤细胞及肿瘤新生血管内皮细胞中高表达，这使得它成为肿瘤分子显像及治疗的靶位点。近年来多种针对整合素αvβ3的显像技术取得了长足进步：包括放射性核素的PET及SPECT显像，MRI显像、超声显像及光学显像；以整合素αvβ3为靶点的靶向治疗包括单克隆抗体治疗、RGD肽类似物治疗及以整合素αvβ3为靶点的药物投放治疗。整合素αvβ3临床研究对开拓肿瘤诊断及治疗有着重要的意义。

Integrins alpha v beta 3 are heterodimerie transmemhrane glycoproteins, consisting of two noncovalently bound transmembrane subunits. Integrins alpha v beta 3 are usually expressed at low or undetectable levels in most adult epithelia but can be highly upregulated in some turaours and vascular endothelial cells, which make them an appealing targets for molecular imaging and therapy. Many different approaches for imaging of integrins alpha v beta 3 expression have been studied in the recent years, including positron emission tomography, single photon emission tomography, magnetic resonance imaging, ultrasound and optical imaging. Integrin antagonists include function-blocking monoclonal antibodies, RGD peptide mimetics, targeted delivery of therapy. Freclinical studies and clinical trials of targeted therapy have great significance for exploring new therapy for tumor.