ACS Medicinal Chemistry Letters · 2012 · 39 citations · 12 references
PharmacyMedicinal ChemistryPharmacologyDrug DesignDrug DiscoveryMolecular OncologyLigand-based DesignPharmacodynamics Of Anticancer AgentsPharmacodynamics Of Anticancer DrugsPotency OptimizationCancer Cell Proliferation InhibitionGrowth Inhibition AssaysKinase Inhibitor Library DesignPi3k InhibitorsPten InactivationPten SignalingRational DesignTherapeutic Growth Inhibition
A novel thiazolopyrimidinone series of PI3K-beta selective inhibitors has been identified. This chemotype has provided an excellent tool compound, 18, that showed potent growth inhibition in the PTEN-deficient breast cancer cell line MDA-MB-468 under anchorage-independent conditions, and it also demonstrated pharmacodynamic effects and efficacy in a PTEN-deficient prostate cancer PC-3 xenograft mouse model.
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A Pharmacological Map of the PI3-K Family Defines a Role for p110α in Insulin Signaling
Zachary A. Knight, Beatriz González, Morri E. Feldman et al. · Cell · 2006 · 1.2K citations · Full text
Essential roles of PI(3)K–p110β in cell growth, metabolism and tumorigenesis
Shidong Jia, Zhenning Liu, Sen Zhang et al. · Nature · 2008 · 684 citations · Full text
PTEN-deficient cancers depend on PIK3CB
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Medicine, Oncology, Pharmacology +16
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