A Kinase Inhibitor Targeted to mTORC1 Drives Regression in Glioblastoma.

@article{Fan2017AKI,
  title={A Kinase Inhibitor Targeted to mTORC1 Drives Regression in Glioblastoma.},
  author={Qiwen Fan and Ozlem Duran Aksoy and Robyn A Wong and Shirin Ilkhanizadeh and Chris J. Novotny and William Clay Gustafson and Albert Yi-Que Truong and Geraldine Cayanan and Erin F. Simonds and Daphne Adele Haas-Kogan and Joanna J Phillips and Theodore P. Nicolaides and Masanori Okaniwa and Kevan M. Shokat and William S. Weiss},
  journal={Cancer cell},
  year={2017},
  volume={31 3},
  pages={424-435}
}
Although signaling from phosphatidylinositol 3-kinase (PI3K) and AKT to mechanistic target of rapamycin (mTOR) is prominently dysregulated in high-grade glial brain tumors, blockade of PI3K or AKT minimally affects downstream mTOR activity in glioma. Allosteric mTOR inhibitors, such as rapamycin, incompletely block mTORC1 compared with mTOR kinase inhibitors (TORKi). Here, we compared RapaLink-1, a TORKi linked to rapamycin, with earlier-generation mTOR inhibitors. Compared with rapamycin and… CONTINUE READING

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