Advances in FAP-targeted molecular imaging probes for disease detection

WANG Xiao; XU Xiaoping; SONG Shaoli

doi:10.19732/j.cnki.2096-6210.2024.05.001

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Advances in FAP-targeted molecular imaging probes for disease detection

更新时间：2025-12-15

- Advances in FAP-targeted molecular imaging probes for disease detection
- Vol. 33, Issue 5, Pages: 457-469(2024)
- 作者机构：
  
  复旦大学附属肿瘤医院核医学科，复旦大学上海医学院肿瘤学系,上海,200032
- 作者简介：
- 基金信息：
- DOI：10.19732/j.cnki.2096-6210.2024.05.001
  CLC：
- Published Online：07 November 2024，
  
  Published：07 November 2024
- 稿件说明：
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王潇,许晓平,宋少莉. FAP靶向分子影像探针在疾病检测中的研究进展[J]. 肿瘤影像学, 2024, 33(5): 457-469 https://doi.

org/10.19732/j.cnki.2096-6210.2024.05.001
王潇,许晓平,宋少莉. FAP靶向分子影像探针在疾病检测中的研究进展[J]. 肿瘤影像学, 2024, 33(5): 457-469 https://doi. DOI： 10.19732/j.cnki.2096-6210.2024.05.001.

org/10.19732/j.cnki.2096-6210.2024.05.001 DOI：

摘要

核医学分子影像技术凭借其无创性和高灵敏度的特点被广泛应用于肿瘤、神经系统疾病、心血管疾病等的诊断。成纤维细胞活化蛋白（fibroblast activation protein，FAP）是一种Ⅱ型丝氨酸蛋白酶，其在90%的恶性实体瘤中高表达。目前以FAP为靶点，已经开发了多种FAP抑制剂（FAP inhibitor，FAPI），其中大多数都具有纳摩尔水平的FAP亲和力以及高FAP选择性，应用于肿瘤的正电子发射体层成像（positron emission tomography，PET）/计算机体层成像（computed tomography，CT）。此外，FAP还在活化的成纤维细胞中高表达，有部分学者探究了FAPI PET/CT在非肿瘤疾病中的应用价值。本文将针对于FAP靶向分子影像探针以及在肿瘤疾病和非肿瘤疾病中的研究进展进行述评。

Abstract

The molecular imaging technology of nuclear medicine is widely used in the diagnosis of tumors

neurological diseases

cardiovascular diseases and other diseases due to its non-invasiveness and high sensitivity. Fibroblast Activation Protein (FAP) is a type Ⅱ serine protease that is highly expressed in 90% of malignant solid tumors. A variety of FAP inhibitors (FAPI) have been developed to target FAP

most of which have nanomolar levels of FAP affinity as well as high FAP selectivity for positron emission tomography(PET)/computed tomography(CT) imaging of tumors. In addition to this

FAP is also highly expressed in activated fibroblasts

and some scholars have explored the value of FAPI PET/CT in non-tumor diseases. In this paper

we reviewed the progress of FAP-targeted molecular imaging probes and research in oncologic and non-oncologic diseases.

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