FAP and FAPI-PET/CT in Malignant and Non-Malignant Diseases: A Perfect Symbiosis?
A fibroblast activation protein (FAP) is an atypical type II transmembrane serine protease with both endopeptidase and post-proline dipeptidyl peptidase activity. FAP is overexpressed in cancer-associated fibroblasts (CAFs), which are found in most epithelial tumors. CAFs have been implicated in pro...
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| Format: | Article |
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MDPI AG
2021-09-01
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| Series: | Cancers |
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| Online Access: | https://www.mdpi.com/2072-6694/13/19/4946 |
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| author | Katharina Dendl Stefan A. Koerber Clemens Kratochwil Jens Cardinale Rebecca Finck Mardjan Dabir Emil Novruzov Tadashi Watabe Vasko Kramer Peter L. Choyke Uwe Haberkorn Frederik L. Giesel |
| author_facet | Katharina Dendl Stefan A. Koerber Clemens Kratochwil Jens Cardinale Rebecca Finck Mardjan Dabir Emil Novruzov Tadashi Watabe Vasko Kramer Peter L. Choyke Uwe Haberkorn Frederik L. Giesel |
| author_sort | Katharina Dendl |
| collection | DOAJ |
| description | A fibroblast activation protein (FAP) is an atypical type II transmembrane serine protease with both endopeptidase and post-proline dipeptidyl peptidase activity. FAP is overexpressed in cancer-associated fibroblasts (CAFs), which are found in most epithelial tumors. CAFs have been implicated in promoting tumor cell invasion, angiogenesis and growth and their presence correlates with a poor prognosis. However, FAP can generally be found during the remodeling of the extracellular matrix and therefore can be detected in wound healing and benign diseases. For instance, chronic inflammation, arthritis, fibrosis and ischemic heart tissue after a myocardial infarction are FAP-positive diseases. Therefore, quinoline-based FAP inhibitors (FAPIs) bind with a high affinity not only to tumors but also to a variety of benign pathologic processes. When these inhibitors are radiolabeled with positron emitting radioisotopes, they provide new diagnostic and prognostic tools as well as insights into the role of the microenvironment in a disease. In this respect, they deliver additional information beyond what is afforded by conventional FDG PET scans that typically report on glucose uptake. Thus, FAP ligands are considered to be highly promising novel tracers that offer a new diagnostic and theranostic potential in a variety of diseases. |
| first_indexed | 2024-03-10T07:04:29Z |
| format | Article |
| id | doaj.art-18665963de2a4a9abdd4c914cab5364c |
| institution | Directory Open Access Journal |
| issn | 2072-6694 |
| language | English |
| last_indexed | 2024-03-10T07:04:29Z |
| publishDate | 2021-09-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Cancers |
| spelling | doaj.art-18665963de2a4a9abdd4c914cab5364c2023-11-22T15:54:46ZengMDPI AGCancers2072-66942021-09-011319494610.3390/cancers13194946FAP and FAPI-PET/CT in Malignant and Non-Malignant Diseases: A Perfect Symbiosis?Katharina Dendl0Stefan A. Koerber1Clemens Kratochwil2Jens Cardinale3Rebecca Finck4Mardjan Dabir5Emil Novruzov6Tadashi Watabe7Vasko Kramer8Peter L. Choyke9Uwe Haberkorn10Frederik L. Giesel11Department of Nuclear Medicine, Heidelberg University Hospital, 69120 Heidelberg, GermanyDepartment of Radiation Oncology, Heidelberg University Hospital, 69120 Heidelberg, GermanyDepartment of Nuclear Medicine, Heidelberg University Hospital, 69120 Heidelberg, GermanyDepartment of Nuclear Medicine, Heidelberg University Hospital, 69120 Heidelberg, GermanyDepartment of Nuclear Medicine, Heidelberg University Hospital, 69120 Heidelberg, GermanyDepartment of Nuclear Medicine, Düsseldorf University Hospital, 40225 Düsseldorf, GermanyDepartment of Nuclear Medicine, Düsseldorf University Hospital, 40225 Düsseldorf, GermanyDepartment of Nuclear Medicine and Tracer Kinetics, Osaka University Graduate School of Medicine, Osaka 565-0871, JapanPositronpharma SA, Santiago 7500921, ChileMolecular Imaging Program, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892-1088, USADepartment of Nuclear Medicine, Heidelberg University Hospital, 69120 Heidelberg, GermanyDepartment of Nuclear Medicine, Heidelberg University Hospital, 69120 Heidelberg, GermanyA fibroblast activation protein (FAP) is an atypical type II transmembrane serine protease with both endopeptidase and post-proline dipeptidyl peptidase activity. FAP is overexpressed in cancer-associated fibroblasts (CAFs), which are found in most epithelial tumors. CAFs have been implicated in promoting tumor cell invasion, angiogenesis and growth and their presence correlates with a poor prognosis. However, FAP can generally be found during the remodeling of the extracellular matrix and therefore can be detected in wound healing and benign diseases. For instance, chronic inflammation, arthritis, fibrosis and ischemic heart tissue after a myocardial infarction are FAP-positive diseases. Therefore, quinoline-based FAP inhibitors (FAPIs) bind with a high affinity not only to tumors but also to a variety of benign pathologic processes. When these inhibitors are radiolabeled with positron emitting radioisotopes, they provide new diagnostic and prognostic tools as well as insights into the role of the microenvironment in a disease. In this respect, they deliver additional information beyond what is afforded by conventional FDG PET scans that typically report on glucose uptake. Thus, FAP ligands are considered to be highly promising novel tracers that offer a new diagnostic and theranostic potential in a variety of diseases.https://www.mdpi.com/2072-6694/13/19/4946FAPI-PET/CTFAPCAFsvarious malignanciesbenign diseasesfibroblast |
| spellingShingle | Katharina Dendl Stefan A. Koerber Clemens Kratochwil Jens Cardinale Rebecca Finck Mardjan Dabir Emil Novruzov Tadashi Watabe Vasko Kramer Peter L. Choyke Uwe Haberkorn Frederik L. Giesel FAP and FAPI-PET/CT in Malignant and Non-Malignant Diseases: A Perfect Symbiosis? Cancers FAPI-PET/CT FAP CAFs various malignancies benign diseases fibroblast |
| title | FAP and FAPI-PET/CT in Malignant and Non-Malignant Diseases: A Perfect Symbiosis? |
| title_full | FAP and FAPI-PET/CT in Malignant and Non-Malignant Diseases: A Perfect Symbiosis? |
| title_fullStr | FAP and FAPI-PET/CT in Malignant and Non-Malignant Diseases: A Perfect Symbiosis? |
| title_full_unstemmed | FAP and FAPI-PET/CT in Malignant and Non-Malignant Diseases: A Perfect Symbiosis? |
| title_short | FAP and FAPI-PET/CT in Malignant and Non-Malignant Diseases: A Perfect Symbiosis? |
| title_sort | fap and fapi pet ct in malignant and non malignant diseases a perfect symbiosis |
| topic | FAPI-PET/CT FAP CAFs various malignancies benign diseases fibroblast |
| url | https://www.mdpi.com/2072-6694/13/19/4946 |
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