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The Role of PI3K in Growth Regulation

Description: PUBLIC HEALTH RELEVANCE: Defects in insulin-dependent stimulation of Phosphoinositide 3-Kinase (PI3K) result in insulin resistance and type 2 diabetes while activating mutations in PI3K result in cancers. More than twenty investigational drugs that target PI3K are currently in cancer clinical trials. The goal of this grant is to understand how PI3K is activated by insulin an growth factors and to determine how mutations in the gene encoding PI3K cause cancer.
Funding type: research
Funder scheme: R01
Start date: 1990-04-01
End date: 2017-05-31
Investigator: LEWIS C. CANTLEY
Institution: WEILL MEDICAL COLL OF CORNELL UNIV
Funded outputs count: 256
Funder award ID: R01GM041890
OpenAlex ID: G7092873543
Discovery and Structure–Activity Relationship Study of ( Z )‑5-Methylenethiazolidin-4-one Derivatives as Potent and Selective Pan-phosphatidylinositol 5‑Phosphate 4‑Kinase Inhibitors
2020 · Theresa D. Manz, Sindhu Carmen Sivakumaren, et al. · Journal of Medicinal Chemistry · 30
Targeting the PI5P4K Lipid Kinase Family in Cancer Using Covalent Inhibitors
2020 · Sindhu Carmen Sivakumaren, Hyeseok Shim, et al. · Cell chemical biology · 57
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Structure–Activity Relationship Study of Covalent Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors
2019 · Theresa D. Manz, Sindhu C. Sivakumaren, et al. · ACS Medicinal Chemistry Letters · 21
PIK3CA and MAP3K1 alterations imply luminal A status and are associated with clinical benefit from pan-PI3K inhibitor buparlisib and letrozole in ER+ metastatic breast cancer
2019 · Mellissa J. Nixon, Luigi Formisano, et al. · npj Breast Cancer · 43
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Suppression of insulin feedback enhances the efficacy of PI3K inhibitors
2018 · Benjamin D. Hopkins, Chantal Pauli, et al. · Nature · 705
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Phosphatidylinositol-5-Phosphate 4-Kinases Regulate Cellular Lipid Metabolism By Facilitating Autophagy
2018 · Mark R. Lundquist, Marcus D. Goncalves, et al. · Molecular Cell · 106
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PIK3CA C2 Domain Deletions Hyperactivate Phosphoinositide 3-kinase (PI3K), Generate Oncogene Dependence, and Are Exquisitely Sensitive to PI3K α Inhibitors
2017 · Sarah Croessmann, Jonathan H. Sheehan, et al. · Clinical Cancer Research · 38
Identifying and Targeting Sporadic Oncogenic Genetic Aberrations in Mouse Models of Triple-Negative Breast Cancer
2017 · Hui Liu, Charles J. Murphy, et al. · Cancer Discovery · 75
Post-transcriptional Regulation of De Novo Lipogenesis by mTORC1-S6K1-SRPK2 Signaling
2017 · Gina Lee, Yuxiang Zheng, et al. · Cell · 223
The PI3K Pathway in Human Disease
2017 · David A. Fruman, Honyin Chiu, et al. · Cell · 2,750
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Proteomic and Metabolomic Characterization of a Mammalian Cellular Transition from Quiescence to Proliferation
2017 · Ho-Joon Lee, Mark P. Jedrychowski, et al. · Cell Reports · 51
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PI3K-p110α mediates the oncogenic activity induced by loss of the novel tumor suppressor PI3K-p85α
2017 · Lauren M. Thorpe, Jennifer M. Spangle, et al. · Proceedings of the National Academy of Sciences · 102
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Phosphorylation of TXNIP by AKT Mediates Acute Influx of Glucose in Response to Insulin
2017 · Althea N. Waldhart, Holly Dykstra, et al. · Cell Reports · 243
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Personalized In Vitro and In Vivo Cancer Models to Guide Precision Medicine
2017 · Chantal Pauli, Benjamin D. Hopkins, et al. · Cancer Discovery · 943
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Cabozantinib Eradicates Advanced Murine Prostate Cancer by Activating Antitumor Innate Immunity
2017 · Akash Patnaik, Kenneth D. Swanson, et al. · Cancer Discovery · 146
PTEN Regulates Glutamine Flux to Pyrimidine Synthesis and Sensitivity to Dihydroorotate Dehydrogenase Inhibition
2017 · Deepti Mathur, Elias Stratikopoulos, et al. · Cancer Discovery · 139
PARK2 Depletion Connects Energy and Oxidative Stress to PI3K/Akt Activation via PTEN S-Nitrosylation
2017 · Amit Gupta, Sara Anjomani-Virmouni, et al. · Molecular Cell · 136
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Phase I dose escalation study of the PI3kinase pathway inhibitor BKM120 and the oral poly (ADP ribose) polymerase (PARP) inhibitor olaparib for the treatment of high-grade serous ovarian and breast cancer
2016 · U.A. Matulonis, G.M. Wulf, et al. · Annals of Oncology · 219
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Obesity and Cancer Mechanisms: Cancer Metabolism
2016 · Benjamin D. Hopkins, Marcus D. Goncalves, et al. · Journal of Clinical Oncology · 414
Mitotic MELK-eIF4B signaling controls protein synthesis and tumor cell survival
2016 · Yubao Wang, Michael Begley, et al. · Proceedings of the National Academy of Sciences · 67
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Phosphoinositide 3-kinase inhibitors induce DNA damage through nucleoside depletion
2016 · Ashish Juvekar, Hai Hu, et al. · Proceedings of the National Academy of Sciences · 93
Deletion of the gene Pip4k2c , a novel phosphatidylinositol kinase, results in hyperactivation of the immune system
2016 · Hyeseok Shim, Chuan Wu, et al. · Proceedings of the National Academy of Sciences · 61
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A Phase Ib Study of Alpelisib (BYL719), a PI3Kα-Specific Inhibitor, with Letrozole in ER+/HER2− Metastatic Breast Cancer
2016 · Ingrid A. Mayer, Vandana G. Abramson, et al. · Clinical Cancer Research · 320
Glutathione biosynthesis is a metabolic vulnerability in PI(3)K/Akt-driven breast cancer
2016 · Evan C. Lien, Costas A. Lyssiotis, et al. · Nature Cell Biology · 249
A Cross-Species Study of PI3K Protein-Protein Interactions Reveals the Direct Interaction of P85 and SHP2
2016 · Susanne B. Breitkopf, Xuemei Yang, et al. · Scientific Reports · 45
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