Fibroblast activation protein-α (FAP) has emerged as a promising target in the field of radiopharmaceuticals due to its selective expression in cancer-associated fibroblasts (CAFs) and other pathological conditions involving fibrosis and inflammation. Recent advancements have focused on developing FAP-specific radioligands for diagnostic imaging and targeted radionuclide therapy. This perspective summarized the latest progress in FAP radiopharmaceutical development, highlighting novel radioligands, preclinical evaluations, and potential clinical applications. Additionally, we analyzed the advantages and existing problems of targeted FAP radiopharmaceuticals, and discussed the key breakthrough directions of this target, so as to improve the development and conversion of FAP-targeted radiopharmaceuticals.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.ejmech.2024.116787 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
An investigation of antiproliferative and antioxidant properties of crude extracts from Sedum nicaeense All. (Crassulaceae).
Pak J Pharm Sci
January 2025
Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman, Jordan.
This study evaluated the antioxidant and antiproliferative effects of aqueous, ethanolic and methanolic extracts of Sedum nicaeense flowers and leaves. The MTT assay assessed cytotoxicity against colorectal cancer cells (Caco-2, HCT-116), breast cancer cells (T47D, MCF-7) and normal fibroblasts (MRC-5), while the ferric-reducing antioxidant power (FRAP) assay measured antioxidant capacity. Essential oils from flowers and leaves were analyzed using gas chromatography-mass spectrometry (GC-MS).
View Article and Find Full Text PDFAutophagy related 7 (ATG7) regulates food intake and liver health during asparaginase exposure.
J Biol Chem
January 2025
Nutritional Sciences Graduate Program, Rutgers University, New Brunswick, New Jersey, United States; Rutgers Cancer Institute of New Jersey, New Brunswick, New Jersey, United States; Department of Nutritional Sciences, Rutgers University, New Brunswick, New Jersey, United States; Endocrinology and Animal Biosciences Graduate Program, Rutgers University, New Brunswick, New Jersey, United States; New Jersey Institute for Food, Nutrition and Health, Rutgers University, New Brunswick, New Jersey, United States. Electronic address:
Amino acid starvation by the chemotherapy agent asparaginase is a potent activator of the integrated stress response (ISR) in liver and can upregulate autophagy in some cell types. We hypothesized that autophagy related 7 (ATG7), a protein that is essential for autophagy and an ISR target gene, was necessary during exposure to asparaginase to maintain liver health. We knocked down Atg7 systemically (Atg7) or in hepatocytes only (ls-Atg7KO) in mice before exposure to pegylated asparaginase for 5 d.
View Article and Find Full Text PDFSLC7A11 suppresses pyroptosis to alleviate rheumatoid arthritis development by modulating the IL-17 pathway.
Int Immunopharmacol
January 2025
Background: Rheumatoid arthritis (RA) is an autoimmune disease of unknown etiology. This study aims to explore the potential mechanisms by which solute carrier family 7 member 11 (SLC7A11) influences RA development.
Methods: Collagen-induced arthritis (CIA) mice were constructed to observe disease onset and pathological scores.
pH-sensitive phthalocyanine-loaded polymeric nanoparticles as a novel treatment strategy for breast cancer.
Bioorg Chem
January 2025
Department of Systems Biology and Engineering, Silesian University of Technology, Akademicka 2A, 44-100 Gliwice, Poland; A. Chełkowski Institute of Physics, University of Silesia in Katowice, 75 Pułku Piechoty 1a, 41-500 Chorzów, Poland. Electronic address:
Novel pH-sensitive polymeric photosensitizer carriers from the phthalocyanine (Pc) group were investigated as potential photodynamic therapy drugs for the treatment of breast cancer. Their high antiproliferative activity was confirmed by photocytotoxicity studies, which indicated their high efficacy and specificity toward the SK-BR-3 cell line. Importantly, the Pcs encapsulated in the polymeric nanoparticle (NP) carrier exhibited a much better penetration into the acidic environment of tumor cells than their free form.
View Article and Find Full Text PDFThe molar dose of FAPI administered impacts on the FAP-targeted PET imaging and therapy in mouse syngeneic tumor models.
Eur J Nucl Med Mol Imaging
January 2025
Department of Nuclear Medicine, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, 1095 Jiefang Ave, Wuhan, 430030, China.
Purpose: Since fibroblast activation protein (FAP), one predominant biomarker of cancer associated fibroblasts (CAFs), is highly expressed in the tumor stroma of various epidermal-derived cancers, targeting FAP for tumor diagnosis and treatment has shown substantial potentials in both preclinical and clinical studies. However, in preclinical settings, tumor-bearing mice exhibit relatively low absolute FAP expression levels, leading to challenges in acquiring high-quality PET images using radiolabeled FAP ligands (FAPIs) with low molar activity, because of which a saturation effect in imaging is prone to happen. Moreover, how exactly the molar dose of FAPI administered to a mouse influences the targeted PET imaging and radiotherapy remains unclear now.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!