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Title
PI3K inhibitors are finally coming of age
Authors
Keywords
-
Journal
NATURE REVIEWS DRUG DISCOVERY
Volume -, Issue -, Pages -
Publisher
Springer Science and Business Media LLC
Online
2021-06-14
DOI
10.1038/s41573-021-00209-1
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- Safety and tolerability of idelalisib, lenalidomide, and rituximab in relapsed and refractory lymphoma: the Alliance for Clinical Trials in Oncology A051201 and A051202 phase 1 trials
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- Efficacy and safety of idelalisib in combination with ofatumumab for previously treated chronic lymphocytic leukaemia: an open-label, randomised phase 3 trial
- (2017) Jeffrey A Jones et al. Lancet Haematology
- Quantification of sensitivity and resistance of breast cancer cell lines to anti-cancer drugs using GR metrics
- (2017) Marc Hafner et al. Scientific Data
- Ex vivo Akt inhibition promotes the generation of potent CD19CAR T cells for adoptive immunotherapy
- (2017) Ryan Urak et al. Journal for ImmunoTherapy of Cancer
- PI3Kα inhibition reduces obesity in mice
- (2016) Elena Lopez-Guadamillas et al. Aging-US
- First-in-human phase I study of copanlisib (BAY 80-6946), an intravenous pan-class I phosphatidylinositol 3-kinase inhibitor, in patients with advanced solid tumors and non-Hodgkin's lymphomas
- (2016) A. Patnaik et al. ANNALS OF ONCOLOGY
- Cancer Stem Cells: Basic Concepts and Therapeutic Implications
- (2016) Dany Nassar et al. Annual Review of Pathology-Mechanisms of Disease
- Phase 2 study of idelalisib and entospletinib: pneumonitis limits combination therapy in relapsed refractory CLL and NHL
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- Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kδ and CK1ε in hematological malignancies
- (2016) Changchun Deng et al. BLOOD
- Idelalisib given front-line for treatment of chronic lymphocytic leukemia causes frequent immune-mediated hepatotoxicity
- (2016) B. L. Lampson et al. BLOOD
- PDK1-SGK1 Signaling Sustains AKT-Independent mTORC1 Activation and Confers Resistance to PI3Kα Inhibition
- (2016) Pau Castel et al. CANCER CELL
- Phosphoinositide 3-Kinase Regulates Glycolysis through Mobilization of Aldolase from the Actin Cytoskeleton
- (2016) Hai Hu et al. CELL
- Discovery and SAR of Novel 2,3-Dihydroimidazo[1,2-c]quinazoline PI3K Inhibitors: Identification of Copanlisib (BAY 80-6946)
- (2016) William J. Scott et al. ChemMedChem
- Strategically Timing Inhibition of Phosphatidylinositol 3-Kinase to Maximize Therapeutic Index in Estrogen Receptor Alpha-Positive, PIK3CA-Mutant Breast Cancer
- (2016) W. Yang et al. CLINICAL CANCER RESEARCH
- Combined Inhibition of Both p110α and p110β Isoforms of Phosphatidylinositol 3-Kinase Is Required for Sustained Therapeutic Effect in PTEN-Deficient, ER + Breast Cancer
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- The hVps34‐SGK3 pathway alleviates sustained PI3K/Akt inhibition by stimulating mTORC1 and tumour growth
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- Efficacy and safety of idelalisib in patients with relapsed, rituximab- and alkylating agent-refractory follicular lymphoma: a subgroup analysis of a phase 2 study
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- Randomized phase 1 study of the phosphatidylinositol 3-kinase δ inhibitor idelalisib in patients with allergic rhinitis
- (2016) Friedrich Horak et al. JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY
- Molecular Alterations and Everolimus Efficacy in Human Epidermal Growth Factor Receptor 2–Overexpressing Metastatic Breast Cancers: Combined Exploratory Biomarker Analysis From BOLERO-1 and BOLERO-3
- (2016) Fabrice André et al. JOURNAL OF CLINICAL ONCOLOGY
- Intermittent High-Dose Scheduling of AZD8835, a Novel Selective Inhibitor of PI3K and PI3K , Demonstrates Treatment Strategies for PIK3CA-Dependent Breast Cancers
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- Overexpression of PIK3CA in murine head and neck epithelium drives tumor invasion and metastasis through PDK1 and enhanced TGFβ signaling
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- Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate
- (2016) Catherine A. Evans et al. ACS Medicinal Chemistry Letters
- Targeting PI3K in Cancer: Impact on Tumor Cells, Their Protective Stroma, Angiogenesis, and Immunotherapy
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- Systematic Functional Characterization of Resistance to PI3K Inhibition in Breast Cancer
- (2016) X. Le et al. Cancer Discovery
- Efficacy and safety of idelalisib in patients with relapsed, rituximab- and alkylating agent-refractory follicular lymphoma: a subgroup analysis of a phase 2 study
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- PI3K signalling in inflammation
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- Measurement of PIP3 Levels Reveals an Unexpected Role for p110β in Early Adaptive Responses to p110α-Specific Inhibitors in Luminal Breast Cancer
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- Identification of Variant-Specific Functions of PIK3CA by Rapid Phenotyping of Rare Mutations
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- Pharmacological Inhibition of PI3K Reduces Adiposity and Metabolic Syndrome in Obese Mice and Rhesus Monkeys
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- Taselisib (GDC-0032), a Potent -Sparing Small Molecule Inhibitor of PI3K, Radiosensitizes Head and Neck Squamous Carcinomas Containing Activating PIK3CA Alterations
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- Clinical Pharmacokinetic and Pharmacodynamic Profile of Idelalisib
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- PI3K inhibitors in inflammation, autoimmunity and cancer
- (2015) Anne-Katrien Stark et al. CURRENT OPINION IN PHARMACOLOGY
- Metabolic Reprogramming of Immune Cells in Cancer Progression
- (2015) Subhra K. Biswas IMMUNITY
- Optimization of Novel Indazoles as Highly Potent and Selective Inhibitors of Phosphoinositide 3-Kinase δ for the Treatment of Respiratory Disease
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- Discovery of (R)-8-(1-(3,5-Difluorophenylamino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide (AZD8186): A Potent and Selective Inhibitor of PI3Kβ and PI3Kδ for the Treatment of PTEN-Deficient Cancers
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- Management of adverse events associated with idelalisib treatment: expert panel opinion
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- Inhibition of PI3K Pathway Reduces Invasiveness and Epithelial-to-Mesenchymal Transition in Squamous Lung Cancer Cell Lines Harboring PIK3CA Gene Alterations
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- PI3K inhibition results in enhanced estrogen receptor function and dependence in hormone receptor–positive breast cancer
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- Discovery of a Potent Class of PI3Kα Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT)
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- Akt1 and -2 inhibition diminishes terminal differentiation and enhances central memory CD8+T-cell proliferation and survival
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- Allosteric activation of PI3Kα by oncogenic mutations
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- Inhibition of Akt signaling promotes the generation of superior tumor-reactive T cells for adoptive immunotherapy
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- Idelalisib, an inhibitor of phosphatidylinositol 3-kinase p110 , for relapsed/refractory chronic lymphocytic leukemia
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- Idelalisib, a selective inhibitor of phosphatidylinositol 3-kinase- , as therapy for previously treated indolent non-Hodgkin lymphoma
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- CDK 4/6 Inhibitors Sensitize PIK3CA Mutant Breast Cancer to PI3K Inhibitors
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- Akt Inhibition Enhances Expansion of Potent Tumor-Specific Lymphocytes with Memory Cell Characteristics
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- Akt-Dependent Metabolic Reprogramming Regulates Tumor Cell Histone Acetylation
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- The effects of the novel SHIP1 activator AQX-1125 on allergen-induced responses in mild-to-moderate asthma
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- First-in-Human Study of CH5132799, an Oral Class I PI3K Inhibitor, Studying Toxicity, Pharmacokinetics, and Pharmacodynamics, in Patients with Metastatic Cancer
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- Phosphoinositide 3-Kinase Regulates Migration and Invasion of Synoviocytes in Rheumatoid Arthritis
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- Innate PI3K p110 Regulates Th1/Th17 Development and Microbiota-Dependent Colitis
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- Discovery and in Vivo Evaluation of (S)-N-(1-(7-Fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and Related PI3Kδ Inhibitors for Inflammation and Autoimmune Disease
- (2014) Timothy D. Cushing et al. JOURNAL OF MEDICINAL CHEMISTRY
- Structural Basis for Isoform Selectivity in a Class of Benzothiazole Inhibitors of Phosphoinositide 3-Kinase γ
- (2014) Philip N. Collier et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery and Optimization of Pyrimidone Indoline Amide PI3Kβ Inhibitors for the Treatment of Phosphatase and Tensin Homologue (PTEN)-Deficient Cancers
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- Suppression of Feedback Loops Mediated by PI3K/mTOR Induces Multiple Overactivation of Compensatory Pathways: An Unintended Consequence Leading to Drug Resistance
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- Characterization of the Novel and Specific PI3K Inhibitor NVP-BYL719 and Development of the Patient Stratification Strategy for Clinical Trials
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- Comprehensive molecular characterization of gastric adenocarcinoma
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- Convergent loss of PTEN leads to clinical resistance to a PI(3)Kα inhibitor
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- Inactivation of PI(3)K p110δ breaks regulatory T-cell-mediated immune tolerance to cancer
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- PI3Kδ Inhibition by Idelalisib in Patients with Relapsed Indolent Lymphoma
- (2014) Ajay K. Gopal et al. NEW ENGLAND JOURNAL OF MEDICINE
- Idelalisib and Rituximab in Relapsed Chronic Lymphocytic Leukemia
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- PI3K isoform dependence of PTEN-deficient tumors can be altered by the genetic context
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- Rapid Induction of Apoptosis by PI3K Inhibitors Is Dependent upon Their Transient Inhibition of RAS-ERK Signaling
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- Selective Inhibition of Regulatory T Cells by Targeting the PI3K-Akt Pathway
- (2014) R. Abu-Eid et al. Cancer Immunology Research
- Characterization of Novel PI3Kδ Inhibitors as Potential Therapeutics for SLE and Lupus Nephritis in Pre-Clinical Studies
- (2014) Philipp Haselmayer et al. Frontiers in Immunology
- Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation
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- P110 -mediated constitutive PI3K signaling limits the efficacy of p110 -selective inhibition in mantle cell lymphoma, particularly with multiple relapse
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- PI3K-δ and PI3K-γ Inhibition by IPI-145 Abrogates Immune Responses and Suppresses Activity in Autoimmune and Inflammatory Disease Models
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- Long-term p110α PI3K inactivation exerts a beneficial effect on metabolism
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- Inhibition of the p110α isoform of PI 3-kinase stimulates nonfunctional tumor angiogenesis
- (2013) Adriana Soler et al. JOURNAL OF EXPERIMENTAL MEDICINE
- Discovery of a Potent and Isoform-Selective Targeted Covalent Inhibitor of the Lipid Kinase PI3Kα
- (2013) Mariana Nacht et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of 2-{3-[2-(1-Isopropyl-3-methyl-1H-1,2–4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): A β-Sparing Phosphoinositide 3-Kinase Inhibitor with High Unbound Exposure and Robust in Vivo Antitumor Activity
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- BAY 80-6946 Is a Highly Selective Intravenous PI3K Inhibitor with Potent p110α and p110δ Activities in Tumor Cell Lines and Xenograft Models
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- Dominant-activating germline mutations in the gene encoding the PI(3)K catalytic subunit p110δ result in T cell senescence and human immunodeficiency
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- Genetic heterogeneity of diffuse large B-cell lymphoma
- (2013) Jenny Zhang et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- Phosphoinositide 3-Kinase Gene Mutation Predisposes to Respiratory Infection and Airway Damage
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- mTORC1 Inhibition Is Required for Sensitivity to PI3K p110 Inhibitors in PIK3CA-Mutant Breast Cancer
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- B-cell receptor signaling as a driver of lymphoma development and evolution
- (2013) Carsten U. Niemann et al. SEMINARS IN CANCER BIOLOGY
- Signaling interplay between transforming growth factor-β receptor and PI3K/AKT pathways in cancer
- (2013) Long Zhang et al. TRENDS IN BIOCHEMICAL SCIENCES
- PI3 Kinase δ Is a Key Regulator of Synoviocyte Function in Rheumatoid Arthritis
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- Isoform-selective induction of human p110δ PI3K expression by TNFα: identification of a new and induciblePIK3CDpromoter
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- Potent and selective inhibitors of PI3Kδ: Obtaining isoform selectivity from the affinity pocket and tryptophan shelf
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- Characterization of AQX-1125, a small-molecule SHIP1 activator
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- Characterization of AQX-1125, a small-molecule SHIP1 activator
- (2012) Grant R Stenton et al. BRITISH JOURNAL OF PHARMACOLOGY
- Oncogenic PI3K Mutations Lead to NF- B-Dependent Cytokine Expression following Growth Factor Deprivation
- (2012) J. E. Hutti et al. CANCER RESEARCH
- Systemic Elevation of PTEN Induces a Tumor-Suppressive Metabolic State
- (2012) Isabel Garcia-Cao et al. CELL
- Pten Positively Regulates Brown Adipose Function, Energy Expenditure, and Longevity
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- Inhibitors Targeting Mitosis: Tales of How Great Drugs against a Promising Target Were Brought Down by a Flawed Rationale
- (2012) E. Komlodi-Pasztor et al. CLINICAL CANCER RESEARCH
- High levels of p110δ PI3K expression in solid tumor cells suppress PTEN activity, generating cellular sensitivity to p110δ inhibitors through PTEN activation
- (2012) Niki Tzenaki et al. FASEB JOURNAL
- Selective Inhibition of Phosphoinositide 3-Kinase p110α Preserves Lymphocyte Function
- (2012) Lomon So et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Agammaglobulinemia and absent B lineage cells in a patient lacking the p85α subunit of PI3K
- (2012) Mary Ellen Conley et al. JOURNAL OF EXPERIMENTAL MEDICINE
- Active PI3K Pathway Causes an Invasive Phenotype Which Can Be Reversed or Promoted by Blocking the Pathway at Divergent Nodes
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- Oncogenic mutations mimic and enhance dynamic events in the natural activation of phosphoinositide 3-kinase p110 (PIK3CA)
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- Neuregulin 1-ErbB4-PI3K signaling in schizophrenia and phosphoinositide 3-kinase-p110δ inhibition as a potential therapeutic strategy
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- PI3K Inhibition Impairs BRCA1/2 Expression and Sensitizes BRCA-Proficient Triple-Negative Breast Cancer to PARP Inhibition
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- Combining a PI3K Inhibitor with a PARP Inhibitor Provides an Effective Therapy for BRCA1-Related Breast Cancer
- (2012) Ashish Juvekar et al. Cancer Discovery
- Genomic Determinants of PI3K Pathway Inhibitor Response in Cancer
- (2012) Britta Weigelt et al. Frontiers in Oncology
- Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799
- (2011) Jun Ohwada et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- PI3K inhibitor, GS-1101 (CAL-101), attenuates pathway signaling, induces apoptosis, and overcomes signals from the microenvironment in cellular models of Hodgkin lymphoma
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- The phosphoinositide 3'-kinase delta inhibitor, CAL-101, inhibits B-cell receptor signaling and chemokine networks in chronic lymphocytic leukemia
- (2011) J. Hoellenriegel et al. BLOOD
- AKT Inhibition Relieves Feedback Suppression of Receptor Tyrosine Kinase Expression and Activity
- (2011) Sarat Chandarlapaty et al. CANCER CELL
- Phosphatidylinositol 3-Kinase and Antiestrogen Resistance in Breast Cancer
- (2011) Todd W. Miller et al. JOURNAL OF CLINICAL ONCOLOGY
- Identification and Characterization of NVP-BKM120, an Orally Available Pan-Class I PI3-Kinase Inhibitor
- (2011) S.-M. Maira et al. MOLECULAR CANCER THERAPEUTICS
- Mitosis is not a key target of microtubule agents in patient tumors
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- Everolimus in Postmenopausal Hormone-Receptor–Positive Advanced Breast Cancer
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- AKT induces senescence in human cells via mTORC1 and p53 in the absence of DNA damage: implications for targeting mTOR during malignancy
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- PI3K-targeted therapy can be evaded by gene amplification along the MYC-eukaryotic translation initiation factor 4E (eIF4E) axis
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- Structural Basis for Activation and Inhibition of Class I Phosphoinositide 3-Kinases
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- PI3K Plays a Critical Role in Neutrophil Activation by Immune Complexes
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- Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer
- (2011) Matthew T. Burger et al. ACS Medicinal Chemistry Letters
- High Frequency of PIK3R1 and PIK3R2 Mutations in Endometrial Cancer Elucidates a Novel Mechanism for Regulation of PTEN Protein Stability
- (2011) Lydia W.T. Cheung et al. Cancer Discovery
- PI3K/p110 is a novel therapeutic target in multiple myeloma
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- CAL-101, a p110 selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability
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- Phosphatidylinositol 3-kinase- inhibitor CAL-101 shows promising preclinical activity in chronic lymphocytic leukemia by antagonizing intrinsic and extrinsic cellular survival signals
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- Discovery of Dual Inhibitors of the Immune Cell PI3Ks p110δ and p110γ: a Prototype for New Anti-inflammatory Drugs
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- Altered Macrophage Function Contributes to Colitis in Mice Defective in the Phosphoinositide-3 Kinase Subunit p110δ
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- Hyperactivation of phosphatidylinositol-3 kinase promotes escape from hormone dependence in estrogen receptor–positive human breast cancer
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- Erratum: Corrigendum: The p110δ structure: mechanisms for selectivity and potency of new PI(3)K inhibitors
- (2010) Alex Berndt et al. Nature Chemical Biology
- The emerging mechanisms of isoform-specific PI3K signalling
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- Activity of any class IA PI3K isoform can sustain cell proliferation and survival
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- The PI3K Isoforms p110 and p110 Are Essential for Pre-B Cell Receptor Signaling and B Cell Development
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- PI3K Regulatory Subunits Lose Control in Cancer
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- Somatic Mutations in p85α Promote Tumorigenesis through Class IA PI3K Activation
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- Inhibition of Class I Phosphoinositide 3-Kinase Activity Impairs Proliferation and Triggers Apoptosis in Acute Promyelocytic Leukemia without Affecting Atra-Induced Differentiation
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- Phosphoinositide 3-Kinase p110 Regulates Natural Antibody Production, Marginal Zone and B-1 B Cell Function, and Autoantibody Responses
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- A chemical screen in diverse breast cancer cell lines reveals genetic enhancers and suppressors of sensitivity to PI3K isoform-selective inhibition
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- An Integrative Genomic and Proteomic Analysis of PIK3CA, PTEN, and AKT Mutations in Breast Cancer
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- PIK3CA Cooperates with Other Phosphatidylinositol 3'-Kinase Pathway Mutations to Effect Oncogenic Transformation
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- Moving towards a Better Understanding of Chemotaxis
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- The Identification of 2-(1H-Indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a Potent, Selective, Orally Bioavailable Inhibitor of Class I PI3 Kinase for the Treatment of Cancer†
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- Angiogenesis selectively requires the p110α isoform of PI3K to control endothelial cell migration
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- Comprehensive genomic characterization defines human glioblastoma genes and core pathways
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- PTEN-deficient cancers depend on PIK3CB
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