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Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349.
- Source :
-
ACS medicinal chemistry letters [ACS Med Chem Lett] 2012 Nov 29; Vol. 4 (1), pp. 103-7. Date of Electronic Publication: 2012 Nov 29 (Print Publication: 2013). - Publication Year :
- 2012
-
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.
Details
- Language :
- English
- ISSN :
- 1948-5875
- Volume :
- 4
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- ACS medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 24900569
- Full Text :
- https://doi.org/10.1021/ml3003132