Research graph
References from Discovery of Tetrasubstituted Quinazolin-4(3 <i>H</i> )-ones as Wild-type-sparing, Highly Selective PI3KαH1047R Inhibitors. Local targets link to admitted publications; unresolved targets remain external evidence.
The PI3K/AKT Pathway as a Target for Cancer Treatment
10.1146/annurev-med-062913-051343 · 2016 · External reference
The PI3K Pathway in Human Disease
10.1016/j.cell.2017.07.029 · 2017 · External reference
PI3K signalling: the path to discovery and understanding
10.1038/nrm3290 · 2012 · External reference
Current State and Future Challenges for PI3K Inhibitors in Cancer Therapy
10.3390/cancers15030703 · 2023 · External reference
A Pan-Cancer Proteogenomic Atlas of PI3K/AKT/mTOR Pathway Alterations
10.1016/j.ccell.2017.04.013 · 2017 · External reference
Comprehensive Characterization of Cancer Driver Genes and Mutations
10.1016/j.cell.2018.07.034 · 2018 · External reference
Frequency and spectrum of PIK3CA somatic mutations in breast cancer
10.1186/s13058-020-01284-9 · 2020 · External reference
Integrative analysis of complex cancer genomics and clinical profiles using the cBioPortal
10.1126/scisignal.2004088 · 2013 · External reference
The cBio cancer genomics portal: an open platform for exploring multidimensional cancer genomics data
10.1158/2159-8290.cd-12-0095 · 2012 · External reference
Alpelisib for PIK3CA-Mutated, Hormone Receptor−Positive Advanced Breast Cancer
10.1056/nejmoa1813904 · 2019 · External reference
Correction: Alpelisib and fulvestrant in PIK3CA-mutated hormone receptor-positive HER2-negative advanced breast cancer included in the French early access program
10.1038/s41388-023-02615-8 · 2023 · External reference
Insulin−PI3K Signalling: An Evolutionarily Insulated Metabolic Driver of Cancer
10.1038/s41574-020-0329-9 · 2020 · External reference
Challenges for the Clinical Development of PI3K Inhibitors: Strategies to Improve Their Impact in Solid Tumors
10.1158/2159-8290.cd-18-1175 · 2019 · External reference
Management Strategies for Hyperglycemia Associated with the α-Selective PI3K Inhibitor Alpelisib for the Treatment of Breast Cancer
10.3390/cancers14071598 · 2022 · External reference
Factors leading to alpelisib discontinuation in patients with hormone receptor positive, human epidermal growth factor receptor-2 negative breast cancer
10.1007/s10549-021-06476-1 · 2022 · External reference
Diabetes mellitus and breast cancer outcomes: a systematic review and meta-analysis
10.1200/jco.2009.27.3011 · 2011 · External reference
A Multidisciplinary Approach to Optimizing Care of Patients Treated with Alpelisib
10.1016/j.breast.2021.12.016 · 2022 · External reference
Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα
10.1021/acs.jmedchem.2c01422 · 2022 · External reference
Inavolisib-Based Therapy in PIK3CA -Mutated Advanced Breast Cancer
10.1056/nejmoa2404625 · 2024 · External reference
Discovery and Clinical Proof-of-Concept of RLY-2608, a First-In-Class Mutant-Selective Allosteric PI3Ka Inhibitor That Decouples Anti-Tumor Activity from Hyperinsulinemia
10.1158/2159-8290.cd-23-0944 · 2023 · External reference
STX-478, a Mutant-Selective, Allosteric PI3Kα Inhibitor Spares Metabolic Dysfunction and Improves Therapeutic Response in PI3Kα-Mutant Xenografts
10.1158/2159-8290.cd-23-0396 · 2023 · External reference
Apharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling
10.1016/j.cell.2006.03.035 · 2006 · External reference
Unresolved reference
External reference
Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein
10.1021/acs.jmedchem.4c00078 · 2024 · External reference
A New Functional Assay Reveals That Membrane Binding Is Critical for Overactivation of the Phosphoinositide 3-Kinase H1047R Mutant
10.1016/j.jbc.2026.111207 · 2026 · External reference
Unresolved reference
External reference
Unresolved reference
External reference
Two Methods, One Goal: Structural Differences between Cocrystallization and Crystal Soaking to Discover Ligand Binding Poses
10.1002/cmdc.202000565 · 2020 · External reference
Cryo-EM structures reveal two allosteric inhibition modes of PI3KαH1047R involving a re-shaping of the activation loop
10.1016/j.str.2024.03.007 · 2024 · External reference
Binding of certain acidic drugs to human albumin: Theoretical and practical estimation of fundamental parameters
10.1007/bf00560349 · 1974 · External reference
Phosphatidylinositol 3-Kinase α−Selective Inhibition with Alpelisib (BYL719) in PIK3CA-Altered Solid Tumors: Results from the First-In-Human Study
10.1200/jco.2017.72.7107 · 2018 · External reference
Characterization of the Novel and Specific PI3Kα Inhibitor NVP-BYL719 and Development of the Patient Stratification Strategy for Clinical Trials
10.1158/1535-7163.mct-13-0865 · 2014 · External reference
Two Methods, One Goal: Structural Differences between Cocrystallization and Crystal Soaking to Discover Ligand Binding Poses
10.1002/cmdc.202000565 · ExternalCitation · doi-reference
Binding of certain acidic drugs to human albumin: Theoretical and practical estimation of fundamental parameters
10.1007/bf00560349 · ExternalCitation · doi-reference
Factors leading to alpelisib discontinuation in patients with hormone receptor positive, human epidermal growth factor receptor-2 negative breast cancer
10.1007/s10549-021-06476-1 · ExternalCitation · doi-reference
A Multidisciplinary Approach to Optimizing Care of Patients Treated with Alpelisib
10.1016/j.breast.2021.12.016 · ExternalCitation · doi-reference
A Pan-Cancer Proteogenomic Atlas of PI3K/AKT/mTOR Pathway Alterations
10.1016/j.ccell.2017.04.013 · ExternalCitation · doi-reference
Apharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling
10.1016/j.cell.2006.03.035 · ExternalCitation · doi-reference
The PI3K Pathway in Human Disease
10.1016/j.cell.2017.07.029 · ExternalCitation · doi-reference
Comprehensive Characterization of Cancer Driver Genes and Mutations
10.1016/j.cell.2018.07.034 · ExternalCitation · doi-reference
A New Functional Assay Reveals That Membrane Binding Is Critical for Overactivation of the Phosphoinositide 3-Kinase H1047R Mutant
10.1016/j.jbc.2026.111207 · ExternalCitation · doi-reference
Cryo-EM structures reveal two allosteric inhibition modes of PI3KαH1047R involving a re-shaping of the activation loop
10.1016/j.str.2024.03.007 · ExternalCitation · doi-reference
Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα
10.1021/acs.jmedchem.2c01422 · ExternalCitation · doi-reference
Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein
10.1021/acs.jmedchem.4c00078 · ExternalCitation · doi-reference
PI3K signalling: the path to discovery and understanding
10.1038/nrm3290 · ExternalCitation · doi-reference
Correction: Alpelisib and fulvestrant in PIK3CA-mutated hormone receptor-positive HER2-negative advanced breast cancer included in the French early access program
10.1038/s41388-023-02615-8 · ExternalCitation · doi-reference
Insulin−PI3K Signalling: An Evolutionarily Insulated Metabolic Driver of Cancer
10.1038/s41574-020-0329-9 · ExternalCitation · doi-reference
Alpelisib for PIK3CA-Mutated, Hormone Receptor−Positive Advanced Breast Cancer
10.1056/nejmoa1813904 · ExternalCitation · doi-reference
Inavolisib-Based Therapy in PIK3CA -Mutated Advanced Breast Cancer
10.1056/nejmoa2404625 · ExternalCitation · doi-reference
Integrative analysis of complex cancer genomics and clinical profiles using the cBioPortal
10.1126/scisignal.2004088 · ExternalCitation · doi-reference
The PI3K/AKT Pathway as a Target for Cancer Treatment
10.1146/annurev-med-062913-051343 · ExternalCitation · doi-reference
Characterization of the Novel and Specific PI3Kα Inhibitor NVP-BYL719 and Development of the Patient Stratification Strategy for Clinical Trials
10.1158/1535-7163.mct-13-0865 · ExternalCitation · doi-reference
The cBio cancer genomics portal: an open platform for exploring multidimensional cancer genomics data
10.1158/2159-8290.cd-12-0095 · ExternalCitation · doi-reference
Challenges for the Clinical Development of PI3K Inhibitors: Strategies to Improve Their Impact in Solid Tumors
10.1158/2159-8290.cd-18-1175 · ExternalCitation · doi-reference
STX-478, a Mutant-Selective, Allosteric PI3Kα Inhibitor Spares Metabolic Dysfunction and Improves Therapeutic Response in PI3Kα-Mutant Xenografts
10.1158/2159-8290.cd-23-0396 · ExternalCitation · doi-reference
Discovery and Clinical Proof-of-Concept of RLY-2608, a First-In-Class Mutant-Selective Allosteric PI3Ka Inhibitor That Decouples Anti-Tumor Activity from Hyperinsulinemia
10.1158/2159-8290.cd-23-0944 · ExternalCitation · doi-reference
Frequency and spectrum of PIK3CA somatic mutations in breast cancer
10.1186/s13058-020-01284-9 · ExternalCitation · doi-reference
Diabetes mellitus and breast cancer outcomes: a systematic review and meta-analysis
10.1200/jco.2009.27.3011 · ExternalCitation · doi-reference
Phosphatidylinositol 3-Kinase α−Selective Inhibition with Alpelisib (BYL719) in PIK3CA-Altered Solid Tumors: Results from the First-In-Human Study
10.1200/jco.2017.72.7107 · ExternalCitation · doi-reference
Management Strategies for Hyperglycemia Associated with the α-Selective PI3K Inhibitor Alpelisib for the Treatment of Breast Cancer
10.3390/cancers14071598 · ExternalCitation · doi-reference
Current State and Future Challenges for PI3K Inhibitors in Cancer Therapy
10.3390/cancers15030703 · ExternalCitation · doi-reference
