Research Progress of Radionuclide-Labeled Small Molecule FAP Inhibitors in Tumor Diagnosis and Treatment
At present, one of the difficulties in the clinical diagnosis and treatment of tumors is to find specific targets and highly selective targeted inhibitors. Fibroblast activation protein (FAP) is a type Ⅱ transmembrane serine protease of the proline oligopeptidase family. A large number of studies ha...
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| Format: | Article |
| Language: | zho |
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Editorial Board of Journal of Isotopes
2022-04-01
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| Series: | Journal of Isotopes |
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| Online Access: | http://www.tws.org.cn/CN/10.7538/tws.2020.youxian.045 |
| _version_ | 1797983634736545792 |
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| author | LIU Jingru;RUI Jiangzhong;ZHU Hong |
| author_facet | LIU Jingru;RUI Jiangzhong;ZHU Hong |
| author_sort | LIU Jingru;RUI Jiangzhong;ZHU Hong |
| collection | DOAJ |
| description | At present, one of the difficulties in the clinical diagnosis and treatment of tumors is to find specific targets and highly selective targeted inhibitors. Fibroblast activation protein (FAP) is a type Ⅱ transmembrane serine protease of the proline oligopeptidase family. A large number of studies have shown that FAP is overexpressed in cancer associated fibroblasts (CAFs) of various tumor entities, and plays important a role in the growth, invasion, metastasis, angiogenesis and immune escape of tumor cells. This suggesting that FAP may become a specific target for tumor diagnosis and treatment. In addition to being highly expressed in inflammation and fibrosis-related diseases, FAP is not normally expressed in normal tissues and organs of adults, so radionuclide-labeled FAP inhibitors have low background activity and can obtain high-contrast images. This article mainly describes the research progress of radionuclide-labeled small molecule FAP inhibitors in terms of affinity, selectivity, structure-activity relationship, in vivo metabolism, and clinical research of FAP inhibitors, in order to benefit clinical diagnosis and treatment. |
| first_indexed | 2024-04-11T06:49:21Z |
| format | Article |
| id | doaj.art-916816f2930b4fa8994e076407276e9b |
| institution | Directory Open Access Journal |
| issn | 1000-7512 |
| language | zho |
| last_indexed | 2024-04-11T06:49:21Z |
| publishDate | 2022-04-01 |
| publisher | Editorial Board of Journal of Isotopes |
| record_format | Article |
| series | Journal of Isotopes |
| spelling | doaj.art-916816f2930b4fa8994e076407276e9b2022-12-22T04:39:15ZzhoEditorial Board of Journal of IsotopesJournal of Isotopes1000-75122022-04-01352135143Research Progress of Radionuclide-Labeled Small Molecule FAP Inhibitors in Tumor Diagnosis and TreatmentLIU Jingru;RUI Jiangzhong;ZHU Hong0Department of nuclear Medicine, Jinling Hospital, Nanjing University School of Medicine；Department of Clinical Pharmacy, Jinling Hospital, Nanjing University School of MedicineAt present, one of the difficulties in the clinical diagnosis and treatment of tumors is to find specific targets and highly selective targeted inhibitors. Fibroblast activation protein (FAP) is a type Ⅱ transmembrane serine protease of the proline oligopeptidase family. A large number of studies have shown that FAP is overexpressed in cancer associated fibroblasts (CAFs) of various tumor entities, and plays important a role in the growth, invasion, metastasis, angiogenesis and immune escape of tumor cells. This suggesting that FAP may become a specific target for tumor diagnosis and treatment. In addition to being highly expressed in inflammation and fibrosis-related diseases, FAP is not normally expressed in normal tissues and organs of adults, so radionuclide-labeled FAP inhibitors have low background activity and can obtain high-contrast images. This article mainly describes the research progress of radionuclide-labeled small molecule FAP inhibitors in terms of affinity, selectivity, structure-activity relationship, in vivo metabolism, and clinical research of FAP inhibitors, in order to benefit clinical diagnosis and treatment.http://www.tws.org.cn/CN/10.7538/tws.2020.youxian.045tumorfapsmall molecule fap inhibitorsradionuclide imaging |
| spellingShingle | LIU Jingru;RUI Jiangzhong;ZHU Hong Research Progress of Radionuclide-Labeled Small Molecule FAP Inhibitors in Tumor Diagnosis and Treatment Journal of Isotopes tumor fap small molecule fap inhibitors radionuclide imaging |
| title | Research Progress of Radionuclide-Labeled Small Molecule FAP Inhibitors in Tumor Diagnosis and Treatment |
| title_full | Research Progress of Radionuclide-Labeled Small Molecule FAP Inhibitors in Tumor Diagnosis and Treatment |
| title_fullStr | Research Progress of Radionuclide-Labeled Small Molecule FAP Inhibitors in Tumor Diagnosis and Treatment |
| title_full_unstemmed | Research Progress of Radionuclide-Labeled Small Molecule FAP Inhibitors in Tumor Diagnosis and Treatment |
| title_short | Research Progress of Radionuclide-Labeled Small Molecule FAP Inhibitors in Tumor Diagnosis and Treatment |
| title_sort | research progress of radionuclide labeled small molecule fap inhibitors in tumor diagnosis and treatment |
| topic | tumor fap small molecule fap inhibitors radionuclide imaging |
| url | http://www.tws.org.cn/CN/10.7538/tws.2020.youxian.045 |
| work_keys_str_mv | AT liujingruruijiangzhongzhuhong researchprogressofradionuclidelabeledsmallmoleculefapinhibitorsintumordiagnosisandtreatment |