Feedback Suppression of PI3Kα Signaling in PTEN-Mutated Tumors Is Relieved by Selective Inhibition of PI3Kβ

Sarit Schwartz, John Wongvipat, Cath Trigwell, +12

Cancer Cell

Signal TransductionSignaling PathwayCell RegulationPten-mutated TumorsFeedback Suppression +10

Inhibition of PI3Kβ Signaling with AZD8186 Inhibits Growth of PTEN-Deficient Breast and Prostate Tumors Alone and in Combination with Docetaxel

Urs J. Hancox, Sabina Cosulich, Lyndsey Hanson, +21

Molecular Cancer Therapeutics

Discovery of (<i>R</i>)-8-(1-(3,5-Difluorophenylamino)ethyl)-<i>N</i>,<i>N</i>-dimethyl-2-morpholino-4-oxo-4<i>H</i>-chromene-6-carboxamide (AZD8186): A Potent and Selective Inhibitor of PI3Kβ and PI3Kδ for the Treatment of PTEN-Deficient Cancers

Bernard Barlaam, Sabina Cosulich, Sébastien L. Degorce, +15

Journal of Medicinal Chemistry

Pten Deficient TumorsPharmacotherapyPharmaceutical ChemistryTumor BiologyPre-clinical Pharmacology +18

Small-molecule androgen receptor downregulators as an approach to treatment of advanced prostate cancer

Robert H. Bradbury, Neil J. Hales, Alfred A. Rabow, +12

Bioorganic & Medicinal Chemistry Letters

UrologyGenitourinary CancerMedicineHormonal ReceptorAdvanced Prostate Cancer +5

Intermittent High-Dose Scheduling of AZD8835, a Novel Selective Inhibitor of PI3Kα and PI3Kδ, Demonstrates Treatment Strategies for <i>PIK3CA</i> -Dependent Breast Cancers

Kevin Hudson, Urs J. Hancox, Cath Trigwell, +15

Molecular Cancer Therapeutics

Discovery of 1-(4-(5-(5-amino-6-(5-tert-butyl-1,3,4-oxadiazol-2-yl)pyrazin-2-yl)-1-ethyl-1,2,4-triazol-3-yl)piperidin-1-yl)-3-hydroxypropan-1-one (AZD8835): A potent and selective inhibitor of PI3Kα and PI3Kδ for the treatment of cancers

Bernard Barlaam, Sabina Cosulich, Bénédicte Delouvrié, +21

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryMedicineSelective InhibitorPharmacotherapyAnti-cancer Agent +7

Inhibiting PI3Kβ with AZD8186 Regulates Key Metabolic Pathways in PTEN-Null Tumors

James T. Lynch, Urszula M. Polanska, Oona Delpuech, +15

Clinical Cancer Research

Discovery of 9-(1-anilinoethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours

Bernard Barlaam, Sabina Cosulich, Sébastien L. Degorce, +12

Bioorganic & Medicinal Chemistry Letters

Molecular PharmacologyMedicinal ChemistryMedicinePten-deficient TumoursPi3kβ/δ Inhibitors +11

The use of 18F-fluorodeoxyglucose positron emission tomography (18F-FDG PET) as a pathway-specific biomarker with AZD8186, a PI3Kβ/δ inhibitor

Juliana Maynard, Sally-Ann Emmas, François-Xavier Blé, +6

EJNMMI Research

Synthesis and structure–activity relationships of thieno[2,3-b]pyrroles as antagonists of the GnRH receptor

J. C. ARNOULD, Bénédicte Delouvrié, Pascal Boutron, +8

Bioorganic & Medicinal Chemistry Letters

Molecular PharmacologyBiochemistryMedicineNatural SciencesGnrh Receptor +7