Fibroblast activation protein (FAP) analogues, also known as FAP inhibitors (FAPIs), are compounds that target and inhibit the activity of FAP, a serine protease overexpressed in tumor stroma and other diseases. These analogues have been developed for various applications, including PET imaging and radiotherapy.
Elaboration:
- FAP and its significance:FAP is a type II transmembrane serine protease that plays a role in extracellular matrix remodeling, tumor growth, and metastasis. It is particularly abundant in cancer-associated fibroblasts (CAFs) and is considered a specific marker for these cells.
- FAPI-based PET imaging:FAPIs are used in conjunction with PET imaging to visualize and characterize the presence and activity of CAFs in tumors. This allows for early detection of tumors and assessment of tumor microenvironment characteristics.
- FAPI-based radiotherapy:FAPIs can also be used for targeted radiotherapy, delivering radiation directly to tumor sites where FAP is highly expressed. This can maximize cancer cell destruction while minimizing damage to surrounding healthy tissues.
- Examples of FAPI development:UAMC1110: A potent FAP inhibitor that has been used as a basis for the development of bifunctional chelator-linker conjugates, says SpringerOpen. Welcome to nginx!.FAPi: A compound using the bifunctional chelator DOTA, which can be used to complex with radiometals like lutetium-177, bismuth-213, lead-210, and yttrium-90. FAPI-04, FAPI-46, FAPI-74, NOTA-DD-FAPI, NOTA-FAPI-MB, FAPI-LM3, DOTAGA. (SA. FAPi)2, DOTAGA-FAPI-FUSCC-II, and OncoFAP-DOTAGA: These are examples of quinoline-based FAPI-based radiotracers that have been developed for PET imaging.
- Clinical applications:FAPI-based PET imaging and radiotherapy are being investigated for a variety of diseases, including cancer and other inflammatory conditions. These approaches have shown promising results in improving understanding of FAPI-based imaging and the potential value of FAPI-based tumor radiotherapy.
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