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100 1 _ |a Neumaier, Felix
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245 _ _ |a Mutated Isocitrate Dehydrogenase (mIDH) as Target for PET Imaging in Gliomas
260 _ _ |a Basel
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500 _ _ |a This work was supported by Deutsche Forschungsgemeinschaft (DFG), grant number NE 890/9-1.
520 _ _ |a Gliomas are the most common primary brain tumors in adults. A diffuse infiltrativegrowth pattern and high resistance to therapy make them largely incurable, but there are significantdifferences in the prognosis of patients with different subtypes of glioma. Mutations in isocitratedehydrogenase (IDH) have been recognized as an important biomarker for glioma classification anda potential therapeutic target. However, current clinical methods for detecting mutated IDH (mIDH)require invasive tissue sampling and cannot be used for follow-up examinations or longitudinalstudies. PET imaging could be a promising approach for non-invasive assessment of the IDH statusin gliomas, owing to the availability of various mIDH-selective inhibitors as potential leads for thedevelopment of PET tracers. In the present review, we summarize the rationale for the developmentof mIDH-selective PET probes, describe their potential applications beyond the assessment of theIDH status and highlight potential challenges that may complicate tracer development. In addition,we compile the major chemical classes of mIDH-selective inhibitors that have been described to dateand briefly consider possible strategies for radiolabeling of the most promising candidates. Whereavailable, we also summarize previous studies with radiolabeled analogs of mIDH inhibitors andassess their suitability for PET imaging in gliomas.
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700 1 _ |a Zlatopolskiy, Boris D.
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700 1 _ |a Neumaier, Bernd
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773 _ _ |a 10.3390/molecules28072890
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