Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349.

ABSTRACT: 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.

SUBMITTER: Pei Z 

PROVIDER: S-EPMC4027466 | biostudies-literature | 2013 Jan

REPOSITORIES: biostudies-literature