Article
Pan-mutant IDH1 inhibitor BAY 1436032 for effective treatment of IDH1 mutant astrocytoma in vivo.
Acta neuropathologica - 1 Apr 2017
Pusch Stefan, Krausert Sonja, Fischer Viktoria, Balss Jörg, Ott Martina, Schrimpf Daniel, Capper David, Sahm Felix, Eisel Jessica, Beck Ann-Christin, Jugold Manfred, Eichwald Viktoria, Kaulfuss Stefan, Panknin Olaf, Rehwinkel Hartmut, Zimmermann Katja, Hillig Roman C, Guenther Judith, Toschi Luisella, Neuhaus Roland, Haegebart Andrea, Hess-Stumpp Holger, Bauser Markus, Wick Wolfgang, Unterberg Andreas, Herold-Mende Christel, Platten Michael, von Deimling Andreas
Abstract excerpt
Mutations in codon 132 of isocitrate dehydrogenase (IDH) 1 are frequent in diffuse glioma, acute myeloid leukemia, chondrosarcoma and intrahepatic cholangiocarcinoma. These mutations result in a neomorphic enzyme specificity which leads to a dramatic increase of intracellular D-2-hydroxyglutarate (2-HG) in tumor cells. Therefore, mutant IDH1 protein is a highly attractive target for inhibitory drugs. Here, we...
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