Chen Haojun, Niu Gang, Wu Hua, Chen Xiaoyuan
1. Department of Nuclear Medicine, Xiamen Cancer Center, the First Affiliated Hospital of Xiamen University, Xiamen, China ; 2. Laboratory of Molecular Imaging and Nanomedicine, National Institute of Biomedical Imaging and Bioengineering, National Institutes of Health, Bethesda, Maryland.
2. Laboratory of Molecular Imaging and Nanomedicine, National Institute of Biomedical Imaging and Bioengineering, National Institutes of Health, Bethesda, Maryland.
Theranostics. 2016 Jan 1;6(1):78-92. doi: 10.7150/thno.13242. eCollection 2016.
Molecular imaging for non-invasive assessment of angiogenesisis is of great interest for clinicians because of the wide-spread application of anti-angiogenic cancer therapeutics. Besides, many other interventions that involve the change of blood vessel/tumor microenvironment would also benefit from such imaging strategies. Of the imaging techniques that target angiogenesis, radiolabeled Arg-Gly-Asp (RGD) peptides have been a major focus because of their high affinity and selectivity for integrin αvβ3--one of the most extensively examined target of angiogenesis. Since the level of integrin αvβ3 expression has been established as a surrogate marker of angiogenic activity, imaging αvβ3 expression can potentially be used as an early indicator of effectiveness of antiangiogenic therapy at the molecular level. In this review, we summarize RGD-based PET tracers that have already been used in clinical trials and intercompared them in terms of radiosynthesis, dosimetry, pharmacokinetics and clinical applications. A perspective of their future use in the clinic is also provided.
由于抗血管生成癌症治疗方法的广泛应用，用于非侵入性评估血管生成的分子成像对临床医生具有极大的吸引力。此外，许多涉及血管/肿瘤微环境变化的其他干预措施也将受益于此类成像策略。在针对血管生成的成像技术中，放射性标记的精氨酸-甘氨酸-天冬氨酸（RGD）肽一直是主要焦点，因为它们对整合素αvβ3具有高亲和力和选择性，整合素αvβ3是血管生成研究最为广泛的靶点之一。由于整合素αvβ3的表达水平已被确立为血管生成活性的替代标志物，成像αvβ3的表达有可能在分子水平上用作抗血管生成治疗有效性的早期指标。在本综述中，我们总结了已用于临床试验的基于RGD的PET示踪剂，并在放射性合成、剂量学、药代动力学和临床应用方面对它们进行了比较。还提供了它们未来在临床应用的前景。
