AZD8055 Is a Potent, Selective, and Orally Bioavailable ATP-Competitive Mammalian Target of Rapamycin Kinase Inhibitor with In vitro and In vivo Antitumor Activity
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...groups have developed small molecules that directly inhibit mTOR kinase activity (Chresta et al., 2010; Feldman et al., 2009; Garcı́a-Martı́nez et al., 2009; Thoreen et al., 2009; Yu et al., 2009)....
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...One study reported an elevation in blood glucose in mice treated with the mTOR kinase inhibitor AZD8055 (Chresta et al., 2010), suggesting that these inhibitors may also impair metabolism....
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...Another more likely reason why rapamycin may have limited efficacy in cancer treatment is the increasing realization that rapamycin only partially inhibits the phosphorylation of 4E-BP1 (Chresta et al., 2010; Feldman et al., 2009; Garcı́a-Martı́nez et al., 2009; Thoreen et al., 2009; Yu et al., 2009)....
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...…A desaturase 1; VEGF, vascular endothelial Cell 149, April 13, 2012 ª2012 Elsevier Inc. 281 groups have developed small molecules that directly inhibit mTOR kinase activity (Chresta et al., 2010; Feldman et al., 2009; Garcı́a-Martı́nez et al., 2009; Thoreen et al., 2009; Yu et al., 2009)....
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...…more likely reason why rapamycin may have limited efficacy in cancer treatment is the increasing realization that rapamycin only partially inhibits the phosphorylation of 4E-BP1 (Chresta et al., 2010; Feldman et al., 2009; Garcı́a-Martı́nez et al., 2009; Thoreen et al., 2009; Yu et al., 2009)....
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Cites background from "AZD8055 Is a Potent, Selective, and..."
...Recently, independent groups generated a series of synthetic small molecules that function as ATP-competitive inhibitors and block all known mTORC1 and mTORC2 action...
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"AZD8055 Is a Potent, Selective, and..." refers background in this paper
...It functions as a sensor of mitogen, energy, and nutrient levels and is a central controller of cell growth and a negative regulator of autophagy (1, 2)....
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"AZD8055 Is a Potent, Selective, and..." refers background in this paper
...prolonged exposure, it decreases mTORC2 function by decreasing mTOR protein levels (7)....
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