Masłowska Katarzyna, Halik Paweł Krzysztof, Tymecka Dagmara, Misicka Aleksandra, Gniazdowska Ewa
Centre of Radiochemistry and Nuclear Chemistry, Institute of Nuclear Chemistry and Technology, Dorodna 16, 03-195 Warsaw, Poland.
Faculty of Chemistry, University of Warsaw, Pasteura 1, 02-093 Warsaw, Poland.
Cancers (Basel). 2021 Mar 3;13(5):1072. doi: 10.3390/cancers13051072.
One approach to anticancer treatment is targeted anti-angiogenic therapy (AAT) based on prevention of blood vessel formation around the developing cancer cells. It is known that vascular endothelial growth factor (VEGF) and vascular endothelial growth factor receptors (VEGFRs) play a pivotal role in angiogenesis process; hence, application of angiogenesis inhibitors can be an effective approach in anticancer combination therapeutic strategies. Currently, several types of molecules have been utilised in targeted VEGF/VEGFR anticancer therapy, including human VEGF ligands themselves and their derivatives, anti-VEGF or anti-VEGFR monoclonal antibodies, VEGF binding peptides and small molecular inhibitors of VEGFR tyrosine kinases. These molecules labelled with diagnostic or therapeutic radionuclides can become, respectively, diagnostic or therapeutic receptor radiopharmaceuticals. In targeted anti-angiogenic therapy, diagnostic radioagents play a unique role, allowing the determination of the emerging tumour, to monitor the course of treatment, to predict the treatment outcomes and, first of all, to refer patients for AAT. This review provides an overview of design, synthesis and study of radiolabelled VEGF/VEGFR targeting and imaging agents to date. Additionally, we will briefly discuss their physicochemical properties and possible application in combination targeted radionuclide tumour therapy.
一种抗癌治疗方法是基于阻止癌细胞周围血管形成的靶向抗血管生成疗法（AAT）。众所周知，血管内皮生长因子（VEGF）和血管内皮生长因子受体（VEGFRs）在血管生成过程中起关键作用；因此，应用血管生成抑制剂可能是抗癌联合治疗策略中的一种有效方法。目前，几种类型的分子已被用于靶向VEGF/VEGFR抗癌治疗，包括人VEGF配体本身及其衍生物、抗VEGF或抗VEGFR单克隆抗体、VEGF结合肽以及VEGFR酪氨酸激酶的小分子抑制剂。这些用诊断或治疗性放射性核素标记的分子可分别成为诊断或治疗性受体放射性药物。在靶向抗血管生成治疗中，诊断性放射性药物发挥着独特作用，可用于确定新出现的肿瘤、监测治疗过程、预测治疗结果，首先是为患者推荐AAT治疗。本文综述了迄今为止放射性标记的VEGF/VEGFR靶向和显像剂的设计、合成及研究概况。此外，我们还将简要讨论它们的物理化学性质以及在联合靶向放射性核素肿瘤治疗中的可能应用。
