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Ref Type | Journal Article | ||||||||||||
PMID | (24900569) | ||||||||||||
Authors | Pei Z, Blackwood E, Liu L, Malek S, Belvin M, Koehler MF, Ortwine DF, Chen H, Cohen F, Kenny JR, Bergeron P, Lau K, Ly C, Zhao X, Estrada AA, Truong T, Epler JA, Nonomiya J, Trinh L, Sideris S, Lesnick J, Bao L, Vijapurkar U, Mukadam S, Tay S, Deshmukh G, Chen YH, Ding X, Friedman LS, Lyssikatos JP | ||||||||||||
Title | Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349. | ||||||||||||
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Abstract Text | Aberrant activation of the PI3K-Akt-mTOR signaling pathway has been observed in human tumors and tumor cell lines, indicating that these protein kinases may be attractive therapeutic targets for treating cancer. Optimization of advanced lead 1 culminated in the discovery of clinical development candidate 8h, GDC-0349, a potent and selective ATP-competitive inhibitor of mTOR. GDC-0349 demonstrates pathway modulation and dose-dependent efficacy in mouse xenograft cancer models. |
Molecular Profile | Treatment Approach |
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Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
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