An inhibitor of mutant IDH1 delays growth and promotes differentiation of glioma cells.

@article{Rohle2013AnIO,
  title={An inhibitor of mutant IDH1 delays growth and promotes differentiation of glioma cells.},
  author={Dan Rohle and Janeta Popovici-Muller and Nicolaos Palaskas and Sevin Turcan and Christian Grommes and Carl Campos and Jennifer Tsoi and Owen Clark and Barbara Oldrini and Evangelia Komisopoulou and Kaiko Kunii and Alicia M. Pedraza and Stefanie Schalm and Lee Silverman and Alexandra A. Miller and Yingjie Wang and Hua 杨华 Yang and Yue Chen and Andrew Kernytsky and Marc K. Rosenblum and Wei Liu and Scott Adams Biller and Shinsan M. Su and C. V. Weiss Brennan and Timothy A. Chan and Thomas G Graeber and Katharine E. Yen and Ingo K. Mellinghoff},
  journal={Science},
  year={2013},
  volume={340 6132},
  pages={
          626-30
        }
}
The recent discovery of mutations in metabolic enzymes has rekindled interest in harnessing the altered metabolism of cancer cells for cancer therapy. One potential drug target is isocitrate dehydrogenase 1 (IDH1), which is mutated in multiple human cancers. Here, we examine the role of mutant IDH1 in fully transformed cells with endogenous IDH1 mutations. A selective R132H-IDH1 inhibitor (AGI-5198) identified through a high-throughput screen blocked, in a dose-dependent manner, the ability of… CONTINUE READING

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