14 research outputs found
Quelques aspects de la réaction du phénylisothiocyanate avec les amino-acides et peptides
Doctorat en Sciencesinfo:eu-repo/semantics/nonPublishe
Activité de la déhydrogénase isocitrique dans le liquide céphalo-rachidien normal et pathologique
Enzymes in cancer.III. Triosephosphate isomerase activity of human blood serum in normal individuals and in individuals with various pathological conditions
Phase II trial of a combination of low dose cisplatin (DDP) and bolus 5-fluorouracil (FU) in recurrent and metastatic squamous cell carcinoma of the head and neck
Microbiome metabolic potency towards plant bioactives and consequences for health effects
In vitro and in situ activity-based labeling of fibroblast activation protein with UAMC1110-derived probes
Combination chemotherapy with methotrexate, bleomycin, and vincristine with or without cisplatin in advanced squamous cell carcinoma of the head and neck
Next generation fibroblast activation protein (FAP) targeting PET tracers : the tetrazine ligation allows an easy and convenient way to \ub9\u2078F-labeled (4-quinolinoyl)glycyl-2-cyanopyrrolidines
Abstract: Small-molecular fibroblast activation protein inhibitor (FAPI)-based tracer have been shown to be promising Positron Emission Tomography (PET) 68Ga-labeled radiopharmaceuticals to image a variety of tumors including pancreatic, breast, and colorectal cancers, among others. In this study, we developed a novel 18F-labeled FAPI derivative. [18F]6 was labeled using a synthon approach based on the tetrazine ligation. It showed subnanomolar affinity for the FAP protein and a good selectivity profile against known off-target proteases. Small animal PET studies revealed high tumor uptake and good target-to-background ratios. [18F]6 was excreted via the liver. Overall, [18F]6 showed promising characteristics to be used as a PET tracer and could serve as a lead for further development of halogen-based theranostic FAPI radiopharmaceuticals