Article
Catalytic mTOR inhibitors can overcome intrinsic and acquired resistance to allosteric mTOR inhibitors.
Oncotarget - 30 Sept 2014
Hassan Burhan, Akcakanat Argun, Sangai Takafumi, Evans Kurt W, Adkins Farrell, Eterovic Agda Karina, Zhao Hao, Chen Ken, Chen Huiqin, Do Kim-Anh, Xie Shelly M, Holder Ashley M, Naing Aung, Mills Gordon B, Meric-Bernstam Funda
Abstract excerpt
We tested the antitumor efficacy of mTOR catalytic site inhibitor MLN0128 in models with intrinsic or acquired rapamycin-resistance. Cell lines that were intrinsically rapamycin-resistant as well as those that were intrinsically rapamycin-sensitive were sensitive to MLN0128 in vitro. MLN0128 inhibited both mTORC1 and mTORC2 signaling, with more robust inhibition of downstream 4E-BP1 phosphorylation and...
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