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摘要: 整合素是一类跨膜糖蛋白，介导细胞与细胞、细胞与细胞外间质之间的黏附及信号传导，调节细胞的黏附、迁移、增殖和凋亡等功能，在新生血管内皮细胞及多种恶性肿瘤细胞表面高表达。基于精氨酸-甘氨酸-天冬氨酸(arginine-glycine-aspartate，RGD)结构的多肽能够与整合素αVβ3等亚型特异结合，通过单光子发射计算机断层成像或正电子发射断层成像，无创、在体显示肿瘤的浸润转移特性以及评估血管新生情况等，具有较大的临床应用价值。基于国际、国内相关临床研究最新进展，本专家共识旨在建立整合素RGD受体显像临床应用的指导原则。
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关键词:
- 整合素 /
- 受体显像 /
- 精氨酸-甘氨酸-天冬氨酸多肽 /
- 临床应用专家共识
Abstract: Integrin is a group of transmembrane glycoprotein that mediates cell-cell adhesion and signal transduction. It regulates cell adhesion, migration, proliferation, apoptosis and other functions. It is highly expressed on the surface of neovascular endothelial cells and a variety of malignant tumor cells. The peptides witharginine-glycine-aspartate (RGD) motif can specifically bind to multiplesubtypes of integrin including αVβ3. When labeled with radionuclides for single photon emission tomography (SPECT) or positron emission tomography (PET), the RGD-based peptides can non-invasively reveal the tumor characteristics, including invasion and metastasis, as well as evaluate angiogenesis in vivo. These methods have shown strong value in clinical application. Based on the home-and-abroad progress in relevant clinical research, this expert consensus aims to establish principles for clinical application of RGD-based peptides to integrin imaging.作者贡献：朱朝晖负责查阅文献和撰写初稿；李思进、王凡修改完善并审校定稿；其余成员参与修订。利益冲突：共识制订工作组所有参与人员均声明不存在利益冲突共识核心专家组成员 (按姓氏首字母排序)：兰晓莉(华中科技大学附属协和医院核医学科)，李林(四川大学华西医院核医学科)，李思进(山西医科大学第一医院核医学科)，刘建军(上海交通大学仁济医院核医学科)，马庆杰(吉林大学中日联谊医院核医学科)，宋少莉(复旦大学肿瘤医院核医学科)，王凡(北京大学医学同位素研究中心)，王雪梅(内蒙古医科大学附属医院核医学科)，辛军(中国医科大学附属盛京医院核医学科)，杨志(北京大学肿瘤医院核医学科)，张祥松(中山医科大学附属第一医院核医学科)，朱朝晖(中国医学科学院北京协和医院核医学科) -
表 1 已进入临床研究的整合素RGD受体显像剂及其特征
显像剂 靶向受体 显像方式 形态 结构 PEG链 99mTc-3PRGD2[6] αVβ3 SPECT 环化 二聚体 有 99mTc-Galacto-RGD2[7] αVβ3 SPECT 环化 二聚体 有 99mTc-NC100692[8] αVβ3 SPECT 环化 单体 有 18F-AlfatideⅡ[9] αVβ3 PET 环化 二聚体 有 18F-Alfatide[10] αVβ3 PET 环化 二聚体 有 68Ga-PRGD2[11] αVβ3 PET 环化 二聚体 有 68Ga-RGD[12] αVβ3 PET 环化 单体 无 18F-FPPRGD2[13] αVβ3 PET 环化 二聚体 有 18F-RGD-K5[14] αVβ3 PET 环化 单体 无 18F-Galacto-RGD[15] αVβ3 PET 环化 单体 无 68Ga-DOTA-SFLAP3[16] αVβ6 PET 环化 单体 无 68Ga-SFITGv6[16] αVβ6 PET 环化 单体 无 68Ga-cycratide[17] αVβ6 PET 环化 单体 无 68Ga-Trivehexin[18] αVβ6 PET 环化 三体 无 68Ga-NODAGA-R01-MG[19] αVβ6 PET 结状 单体 无 18F-FP-R01-MG-F2[19] αVβ6 PET 结状 单体 无 18F-αVβ6-BP[20] αVβ6 PET 线性 单体 有 18F-fluciclatide[21] αVβ5和αVβ3 PET 环化 单体 有 68Ga-NOTA-TATE-RGD[22] αVβ3和SSTR2 PET 环化 异二聚体 有 68Ga-NOTA-BBN-RGD[23] αVβ3和GRPR PET 环化 异二聚体 无 PEG：聚乙二醇；SPECT：单光子发射计算机断层成像；PET：正电子发射断层显像；RGD: 同图 1 
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