| 摘要: |
| 成纤维细胞活化蛋白（FAP）在90%以上的上皮性癌间质中高表达，可以作为肿瘤成像和治疗的靶点.而一些已开发的成纤维细胞活化蛋白抑制剂（FAPI），由于对肿瘤的高亲和力和高肿瘤积聚，对肿瘤的诊断和治疗具有重大意义.文章综述了近年来FAPI在肿瘤诊疗方面的研究进展，重点阐述了新型FAPI在核医学上的诊疗应用，并且从构效关系上讨论了FAPI的靶向弹头结构，增强FAPI选择性及延长肿瘤保留时间的策略，进一步推动了FAPI向临床诊疗试剂转化. |
| 关键词: 成纤维细胞活化蛋白抑制剂(FAPI) 核医学影像 放射性治疗 构效关系 |
| DOI：10.3969/J.ISSN.1000-5137.2022.04.007 |
| 分类号:R817.9 |
| 基金项目:国家自然科学基金重大研究计划培育项目（91959105） |
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| Progress in fibroblast activation protein inhibitors for cancer diagnosis and treatment |
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YE Yumeng1, ZHOU Xuesu1, TIAN Qiwei1,2, XUE Fengfeng2, YANG Shiping1
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1.College of Chemistry and Materials Science, Shanghai Normal University, Shanghai 200234, China;2.Shanghai Key Laboratory of Molecular Imaging, Shanghai University of Medicine and Health Sciences, Shanghai 201318, China
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| Abstract: |
| Fibroblast activation protein(FAP) is highly expressed in more than 90% of epithelial carcinoma stroma and can be used as a target for tumor imaging and therapy. Some developed FAP inhibitors(FAPI) are of great significance in the diagnosis and treatment of tumors due to their high affinity for tumors and high tumor accumulation. Herein,the research progress of FAPI in tumor diagnosis and treatment in recent years was reviewed,with an emphasis on the clinical application of novel FAPI in nuclear medicine. In addition,FAPI targeting warhead structure and the strategies of enhancing FAPI selectivity and prolonging tumor retention time were discussed from the perspective of structure-activity relationship,which further promoted the transformation of FAPI into clinical diagnosis and treatment reagents. |
| Key words: fibroblast activating protein inhibitors(FAPI) nuclear medical imaging radiation therapy structure-activity relationship |
