放射性核素标记靶向肿瘤新生血管分子探针研究进展

Diversity of Radioprobes Targeted to Tumor Angiogenesis on Molecular Functional Imaging

分子影像技术能够在细胞及分子水平定性、定量示踪肿瘤新生血管生物学过程。不同的放射性核素标记靶向分子探针在肿瘤新生血管显像过程中发挥着至关重要的作用。系统介绍了目前应用于肿瘤新生血管功能显像的分子探针,包括抗体及其片段、多肽探针、纳米颗粒探针等。纳米颗粒探针因具有不穿透血管内膜的性质,是目前研究较多的肿瘤新生血管靶向探针。肿瘤新生血管显像剂的体内稳定性及生物相容性、靶向结合于肿瘤新生血管的效率及药代动力学性质是目前亟待解决的问题。

Molecular functional imaging could visualize, characterize, and measure the bio logical processes including tumor angiogenesis at the molecular and cellular levels in humans and other living systems. The molecular probes labeled by a variety of radionuclide used in the field of the nuclear medicine play pivotal roles in molecular imaging of tumor angiogene- sis. However, the regulatory role of different probes in tumor angiogenesis has not been systematically illustrated. The current status of tumor angiogenesis imaging with radiola- beled probes of peptide, monoclonal antibody as well as its fragment, especially nanoparti- cle-based probes to gain insights into the robust tumor angiogenesis development were sum- marized. It was recognized that only the probes such as nanoparticle-based probes, whichtruly target the tumor vasculature rather than tumor cells because of poor extravasation, are really tumor angiogenesis imaging agent. The research of molecular probe targeted to angio- genesis would meet its flourish just after the outstanding improvements in the in vivo stabil ity and biocompatibility, tumor-targeting efcacy, and pharmacokinetics of tumor angiogene- sis imaging probes are made. Translation to clinical applications will also be critical for the maximize benets of these novel agents. The future of tumor angiogenesis imaging lies in lia ble imaging probes and multiple imaging modalities, imaging of protein-protein interactions, and quantitative molecular imaging.