以血管生成为分子靶点的放射性核素显像分子探针在肿瘤个体化用药中的应用

血管生成对肿瘤生长至关重要，以肿瘤血管为靶点的抗血管生成治疗日益受到重视，但抗血管生成疗法的机制以及治疗后产生的耐药性尚不明确。无创性放射性核素分子显像可阐明基本的药物机制以及耐药通路，并通过治疗前和治疗期间的靶点量化表达实现个体化的抗血管生成治疗。笔者重点讨论在血管生成过程中4个关键蛋白质，即血管内皮生长因子（VEGF）及其受体、整合素αvβ3、细胞外基质纤连蛋白、基质金属蛋白酶（MMP）的表达在放射性核素标记分子显像探针发展中的作用及其在个体化抗血管生成疗法中的应用。

Targeting angiogenesis of radionuclide imaging molecular probes for tumor individualized medicine

Angiogenesis is essential for tumor growth,and anti-angiogenesis therapy has gained increasing attention in clinical oncology.Nonetheless,the mechanisms underlying anti-angiogenic therapeutics and cancer cell resistance to these drugs remain unclear.Non-invasive nuclide molecular imaging can be used to determine the mechanism of basic drugs and drug-resistant pathways.This tool can also be utilized to personalize anti-angiogenic therapy by enabling target expression quantification prior to and during treatment.This review focuses on the development of radio-labeled probes for imaging the following key proteins expressed during angiogenesis:vascular endothelial growth factor and its receptor integrin αvβ3,the extracellular domain of fibronectin,and matrix metalloproteases.This review also discusses the potential of these probes for individualized anti-angiogenesis therapy.