Article
Synthesis and evaluation of radiolabeled AGI-5198 analogues as candidate radiotracers for imaging mutant IDH1 expression in tumors.
Bioorganic & medicinal chemistry letters - 15 Feb 2018
Chitneni Satish K, Reitman Zachary J, Spicehandler Rebecca, Gooden David M, Yan Hai, Zalutsky Michael R
Abstract excerpt
Mutations in the metabolic enzyme isocitrate dehydrogenase 1 (IDH1) are commonly found in gliomas. AGI-5198, a potent and selective inhibitor of the mutant IDH1 enzyme, was radiolabeled with radioiodine and fluorine-18. These radiotracers were evaluated as potential probes for imaging mutant IDH1 expression in tumors with positron emission tomography (PET). Radioiodination of AGI-5198 was achieved using a tin...
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