整合素素α_Ⅴβ_3受体显像剂^(18)F标记RGD肽的研究进展

Advance of ^(18)F Labeled RGD Peptide as Integrin α_Ⅴβ_3 Receptor Imaging Agents

血管新生是肿瘤生长、转移过程中不可缺少的生物过程。整合素αⅤβ3受体在新生血管内皮细胞和多种肿瘤细胞表面高表达,在肿瘤血管新生中起着关键作用,目前已成为肿瘤诊断与治疗的一个重要靶点。精氨酸-甘氨酸-天冬氨酸(Arg-Gly-Asp,RGD)肽可特异性地与整合素αⅤβ3受体结合,18 F标记的RGD肽类化合物PET显像可无创、动态地定量监测整合素αⅤβ3受体表达,在肿瘤早期诊断、疗效监测及抗血管新生评价上发挥着重要作用。本文就近年来国内外18F标记RGD肽在肿瘤αⅤβ3受体显像中的研究进展作简要综述。

Angiogenesis is vital for tumor growth and metastasis. Integrin avβ3 receptor has been shown to play a key role in tumor angiogenesis and metastasis. The highly expression of integrin avβ3 receptor in endothelial cells and tumor cells presents an interesting molecular target for diagnosis and treatment of the rapidly growing and metastatic tumors. Arginine-glycine-aspartic acid （Arg-Gly-Asp, RGD） peptide can specifically target to integrin avβ3 receptor. 18F labeled RGD peptides can be used to non-invasively visualize and quantify avβ3 integrin expression levels, and play a key role in early diagnosis of tumor, monitoring and evaluation of anti-angiogenesis. In recent years, there has been a great acceleration in the development of radiolabeled receptor-binding peptides for single photon emission compu- ted tomography （SPECT） and positron emission tomography （PET） imaging in nuclear on-cology. Integrin avβa receptor is expected to become the new target spot of radioactive substance, while the radioactive nuclide labeled RGD peptides will be a potential tumor imaging agent in clinical. This article reviews the recent development of 18F labeled RGD peptide and its application in tumor integrin avβ3 receptor imaging.