For Better or Worse: The Potential for Dose Limiting the On-Target Toxicity of PI 3-Kinase Inhibitors

Targeting PI3K in cancer: mechanisms and advances in clinical trials

(2019) Jing Yang et al.   Molecular Cancer

Infections associated with immunotherapeutic and molecular targeted agents in hematology and oncology. A position paper by the European Conference on Infections in Leukemia (ECIL)

(2019) Georg Maschmeyer et al.   LEUKEMIA

Class II PI3K Functions in Cell Biology and Disease

(2019) Federico Gulluni et al.   TRENDS IN CELL BIOLOGY

p110γ deficiency protects against pancreatic carcinogenesis yet predisposes to diet-induced hepatotoxicity

(2019) Carolina Torres et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Phosphoinositide 3-Kinase Gamma Inhibition Protects from Anthracycline Cardiotoxicity and Reduces Tumor Growth

(2018) Mingchuan Li et al.   CIRCULATION

ESCMID Study Group for Infections in Compromised Hosts (ESGICH) Consensus Document on the safety of targeted and biological therapies: an infectious diseases perspective (Intracellular signaling pathways: tyrosine kinase and mTOR inhibitors)

(2018) M. Reinwald et al.   CLINICAL MICROBIOLOGY AND INFECTION

Activated PI3 Kinase Delta Syndrome: From Genetics to Therapy

(2018) David Michalovich et al.   Frontiers in Immunology

Management of adverse events associated with idelalisib treatment in chronic lymphocytic leukemia and follicular lymphoma: A multidisciplinary position paper

(2018) Antonio Cuneo et al.   HEMATOLOGICAL ONCOLOGY

Suppression of insulin feedback enhances the efficacy of PI3K inhibitors

(2018) Benjamin D. Hopkins et al.   NATURE

Targeted therapy in patients with PIK3CA-related overgrowth syndrome

(2018) Quitterie Venot et al.   NATURE

Mutations in the adaptor-binding domain and associated linker region of p110δ cause Activated PI3K-δ Syndrome 1 (APDS1)

(2017) Lucie Heurtier et al.   HAEMATOLOGICA

Recent advances in the use of PI3K inhibitors for glioblastoma multiforme: current preclinical and clinical development

(2017) Hua-fu Zhao et al.   Molecular Cancer

Mutations in the adaptor-binding domain and associated linker region of p110δ cause Activated PI3K-δ Syndrome 1 (APDS1)

(2017) Lucie Heurtier et al.   HAEMATOLOGICA

A phase I study evaluating GDC-0941, an oral phosphoinositide-3 kinase (PI3K) inhibitor, in patients with advanced solid tumors or multiple myeloma.

(2017) V. Moreno Garcia et al.   JOURNAL OF CLINICAL ONCOLOGY

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

Advances in the Development of Class I Phosphoinositide 3-Kinase (PI3K) Inhibitors

(2016) Dima A. Sabbah et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Risk of mTOR inhibitors induced severe pneumonitis in cancer patients: a meta-analysis of randomized controlled trials

(2016) Xi Zhang et al.   Future Oncology

A Phase Ib Study of BEZ235, a Dual Inhibitor of Phosphatidylinositol 3-Kinase (PI3K) and Mammalian Target of Rapamycin (mTOR), in Patients With Advanced Renal Cell Carcinoma

(2016) Maria I. Carlo et al.   ONCOLOGIST

Differential regulatory functions of three classes of phosphatidylinositol and phosphoinositide 3-kinases in autophagy

(2015) Xinlei Yu et al.   Autophagy

MTOR, PIK3C3, and autophagy: Signaling the beginning from the end

(2015) Michael J Munson et al.   Autophagy

Pharmacological Inhibition of PI3K Reduces Adiposity and Metabolic Syndrome in Obese Mice and Rhesus Monkeys

(2015) Ana Ortega-Molina et al.   Cell Metabolism

FDA Approval: Idelalisib Monotherapy for the Treatment of Patients with Follicular Lymphoma and Small Lymphocytic Lymphoma

(2015) B. W. Miller et al.   CLINICAL CANCER RESEARCH

Drugging PI3K in cancer: refining targets and therapeutic strategies

(2015) Timothy A Yap et al.   CURRENT OPINION IN PHARMACOLOGY

PI3K inhibitors in inflammation, autoimmunity and cancer

(2015) Anne-Katrien Stark et al.   CURRENT OPINION IN PHARMACOLOGY

Management of adverse events associated with idelalisib treatment: expert panel opinion

(2015) Steven E. Coutré et al.   LEUKEMIA & LYMPHOMA

Role of Phosphoinositide 3-OH Kinase p110β in Skeletal Myogenesis

(2015) Ronald W. Matheny et al.   MOLECULAR AND CELLULAR BIOLOGY

Identifying recurrent mutations in cancer reveals widespread lineage diversity and mutational specificity

(2015) Matthew T Chang et al.   NATURE BIOTECHNOLOGY

Novel Role for p110β PI 3-Kinase in Male Fertility through Regulation of Androgen Receptor Activity in Sertoli Cells

(2015) Julie Guillermet-Guibert et al.   PLoS Genetics

Structure, function and inhibition of the phosphoinositide 3-kinase p110α enzyme

(2014) Jack U. Flanagan et al.   BIOCHEMICAL SOCIETY TRANSACTIONS

Idelalisib, an inhibitor of phosphatidylinositol 3-kinase p110 , for relapsed/refractory chronic lymphocytic leukemia

(2014) J. R. Brown et al.   BLOOD

A phase 1 study of the PI3K  inhibitor idelalisib in patients with relapsed/refractory mantle cell lymphoma (MCL)

(2014) B. S. Kahl et al.   BLOOD

Abstract P2-16-14: Preliminary safety, pharmacokinetics and anti-tumor activity of BYL719, an alpha-specific PI3K inhibitor in combination with fulvestrant: Results from a phase I study

(2014) D Juric et al.   CANCER RESEARCH

Phase I dose-escalation study of buparlisib (BKM120), an oral pan-class I PI3K inhibitor, in Japanese patients with advanced solid tumors

(2014) Yuichi Ando et al.   CANCER SCIENCE

Drug-induced pneumonitis in cancer patients treated with mTOR inhibitors: management and insights into possible mechanisms

(2014) Ignacio Duran et al.   Expert Opinion On Drug Safety

Phase I study of PF-04691502, a small-molecule, oral, dual inhibitor of PI3K and mTOR, in patients with advanced cancer

(2014) Carolyn D. Britten et al.   INVESTIGATIONAL NEW DRUGS

Phase I dose-escalation and -expansion study of buparlisib (BKM120), an oral pan-Class I PI3K inhibitor, in patients with advanced solid tumors

(2014) Jordi Rodon et al.   INVESTIGATIONAL NEW DRUGS

Insulin Secretion Induced by Glucose-dependent Insulinotropic Polypeptide Requires Phosphatidylinositol 3-Kinase γ in Rodent and Human β-Cells

(2014) Jelena Kolic et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Innate PI3K p110  Regulates Th1/Th17 Development and Microbiota-Dependent Colitis

(2014) E. C. Steinbach et al.   JOURNAL OF IMMUNOLOGY

PI3K and cancer: lessons, challenges and opportunities

(2014) David A. Fruman et al.   NATURE REVIEWS DRUG DISCOVERY

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

(2014) Richard R. Furman et al.   NEW ENGLAND JOURNAL OF MEDICINE

PI3Kδ inhibition reduces TNF secretion and neuroinflammation in a mouse cerebral stroke model

(2014) Pei Ching Low et al.   Nature Communications

RAS and RHO Families of GTPases Directly Regulate Distinct Phosphoinositide 3-Kinase Isoforms

(2013) Ralph Fritsch et al.   CELL

Phase I Safety, Pharmacokinetic, and Pharmacodynamic Study of SAR245408 (XL147), an Oral Pan-Class I PI3K Inhibitor, in Patients with Advanced Solid Tumors

(2013) G. I. Shapiro et al.   CLINICAL CANCER RESEARCH

Inhibition of DNA Double-Strand Break Repair by the Dual PI3K/mTOR Inhibitor NVP-BEZ235 as a Strategy for Radiosensitization of Glioblastoma

(2013) Carlos Rodrigo Gil del Alcazar et al.   CLINICAL CANCER RESEARCH

Distinct and opposing roles for the phosphatidylinositol 3-OH kinase catalytic subunits p110α and p110β in the regulation of insulin secretion from rodent and human beta cells

(2013) J. Kolic et al.   DIABETOLOGIA

Long-term p110α PI3K inactivation exerts a beneficial effect on metabolism

(2013) Lazaros C. Foukas et al.   EMBO Molecular Medicine

Extended treatment with selective phosphatidylinositol 3-kinase and mTOR inhibitors has effects on metabolism, growth, behaviour and bone strength

(2013) Greg C. Smith et al.   FEBS Journal

Inflammatory Signalings Involved in Airway and Pulmonary Diseases

(2013) I-Ta Lee et al.   MEDIATORS OF INFLAMMATION

CXCL12-Mediated Murine Neural Progenitor Cell Movement Requires PI3Kβ Activation

(2013) Borja L. Holgado et al.   MOLECULAR NEUROBIOLOGY

Development of PI3K inhibitors: lessons learned from early clinical trials

(2013) Jordi Rodon et al.   Nature Reviews Clinical Oncology

PIK3CA Activating Mutations in Facial Infiltrating Lipomatosis

(2013) Reid A. Maclellan et al.   PLASTIC AND RECONSTRUCTIVE SURGERY

Integrative Analysis of Complex Cancer Genomics and Clinical Profiles Using the cBioPortal

(2013) J. Gao et al.   Science Signaling

Somatic Mosaic Activating Mutations in PIK3CA Cause CLOVES Syndrome

(2012) Kyle C. Kurek et al.   AMERICAN JOURNAL OF HUMAN GENETICS

The p110δ subunit of PI3K regulates bone marrow-derived eosinophil trafficking and airway eosinophilia in allergen-challenged mice

(2012) Bit Na Kang et al.   AMERICAN JOURNAL OF PHYSIOLOGY-LUNG CELLULAR AND MOLECULAR PHYSIOLOGY

PI3K signalling in B- and T-lymphocytes: new developments and therapeutic advances

(2012) Lomon So et al.   BIOCHEMICAL JOURNAL

Pten Positively Regulates Brown Adipose Function, Energy Expenditure, and Longevity

(2012) Ana Ortega-Molina et al.   Cell Metabolism

Somatic gain-of-function mutations in PIK3CA in patients with macrodactyly

(2012) Jonathan J. Rios et al.   HUMAN MOLECULAR GENETICS

Inhibition of the PI3 kinase cascade in corticolimbic circuit: temporal and differential effects on contextual fear and extinction

(2012) Milly Kritman et al.   INTERNATIONAL JOURNAL OF NEUROPSYCHOPHARMACOLOGY

Intrapatient Cetuximab Dose Escalation in Metastatic Colorectal Cancer According to the Grade of Early Skin Reactions: The Randomized EVEREST Study

(2012) Eric Van Cutsem et al.   JOURNAL OF CLINICAL ONCOLOGY

Management of Metabolic Effects Associated With Anticancer Agents Targeting the PI3K-Akt-mTOR Pathway

(2012) Naifa L. Busaidy et al.   JOURNAL OF CLINICAL ONCOLOGY

PI3K p110α/Akt Signaling Negatively Regulates Secretion of the Intestinal Peptide Neurotensin Through Interference of Granule Transport

(2012) Jing Li et al.   MOLECULAR ENDOCRINOLOGY

Mosaic overgrowth with fibroadipose hyperplasia is caused by somatic activating mutations in PIK3CA

(2012) Marjorie J Lindhurst et al.   NATURE GENETICS

De novo somatic mutations in components of the PI3K-AKT3-mTOR pathway cause hemimegalencephaly

(2012) Jeong Ho Lee et al.   NATURE GENETICS

PI3Kγ Drives Priming and Survival of Autoreactive CD4+ T Cells during Experimental Autoimmune Encephalomyelitis

(2012) Iain Comerford et al.   PLoS One

Functional Redundancy of Class I Phosphoinositide 3-Kinase (PI3K) Isoforms in Signaling Growth Factor-Mediated Human Neutrophil Survival

(2012) Jatinder K. Juss et al.   PLoS One

The cBio Cancer Genomics Portal: An Open Platform for Exploring Multidimensional Cancer Genomics Data: Figure 1.

(2012) Ethan Cerami et al.   Cancer Discovery

The phosphoinositide 3-kinase signaling pathway in normal and malignant B cells: activation mechanisms, regulation and impact on cellular functions

(2012) Samantha D. Pauls et al.   Frontiers in Immunology

Effects of acutely inhibiting PI3K isoforms and mTOR on regulation of glucose metabolismin vivo

(2011) Greg C. Smith et al.   BIOCHEMICAL JOURNAL

PIK3R1 (p85 ) Is Somatically Mutated at High Frequency in Primary Endometrial Cancer

(2011) M. E. Urick et al.   CANCER RESEARCH

Present and Future of PI3K Pathway Inhibition in Cancer: Perspectives and Limitations

(2011) E. Ciraolo et al.   CURRENT MEDICINAL CHEMISTRY

Ablation of PI3K p110-  Prevents High-Fat Diet-Induced Liver Steatosis

(2011) M. Chattopadhyay et al.   DIABETES

Local infusion of ghrelin enhanced hippocampal synaptic plasticity and spatial memory through activation of phosphoinositide 3-kinase in the dentate gyrus of adult rats

(2011) Liang Chen et al.   EUROPEAN JOURNAL OF NEUROSCIENCE

PI3K class IB controls the cell cycle checkpoint promoting cell proliferation in hepatocellular carcinoma

(2011) Francesco Dituri et al.   INTERNATIONAL JOURNAL OF CANCER

Phosphoinositide 3-Kinase (PI3K(p110α)) Directly Regulates Key Components of the Z-disc and Cardiac Structure

(2011) Ashley J. Waardenberg et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Phase I, Dose-Escalation Study of BKM120, an Oral Pan-Class I PI3K Inhibitor, in Patients With Advanced Solid Tumors

(2011) Johanna C. Bendell et al.   JOURNAL OF CLINICAL ONCOLOGY

Integrating Cardiac PIP3 and cAMP Signaling through a PKA Anchoring Function of p110γ

(2011) Alessia Perino et al.   MOLECULAR CELL

Differential roles for the p101 and p84 regulatory subunits of PI3Kγ in tumor growth and metastasis

(2011) J A Brazzatti et al.   ONCOGENE

Regulation of lipid binding underlies the activation mechanism of class IA PI3-kinases

(2011) W-C Hon et al.   ONCOGENE

Apolipoprotein E reduces food intake via PI3K/Akt signaling pathway in the hypothalamus

(2011) Ling Shen et al.   PHYSIOLOGY & BEHAVIOR

PI3Ks Maintain the Structural Integrity of T-Tubules in Cardiac Myocytes

(2011) Chia-Yen C. Wu et al.   PLoS One

Blockade of class IB phosphoinositide-3 kinase ameliorates obesity-induced inflammation and insulin resistance

(2011) N. Kobayashi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

PI3K  within a nonhematopoietic cell type negatively regulates diet-induced thermogenesis and promotes obesity and insulin resistance

(2011) B. Becattini et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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(p110α) Protects Against Myocardial Infarction-Induced Heart Failure

(2010) Ruby C.Y. Lin et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

Specific Roles of the p110α Isoform of Phosphatidylinsositol 3-Kinase in Hepatic Insulin Signaling and Metabolic Regulation

(2010) Victoria Rotter Sopasakis et al.   Cell Metabolism

Involvement of Phosphoinositide 3-Kinase γ in Angiogenesis and Healing of Experimental Myocardial Infarction in Mice

(2010) Mauro Siragusa et al.   CIRCULATION RESEARCH

Key Role of Phosphoinositide 3-Kinase Class IB in Pancreatic Cancer

(2010) C. E. Edling et al.   CLINICAL CANCER RESEARCH

Altered Macrophage Function Contributes to Colitis in Mice Defective in the Phosphoinositide-3 Kinase Subunit p110δ

(2010) Jennifer K. Uno et al.   GASTROENTEROLOGY

NVP-BEZ235, a dual pan class I PI3 kinase and mTOR inhibitor, promotes osteogenic differentiation in human mesenchymal stromal cells

(2010) Sally K Martin et al.   JOURNAL OF BONE AND MINERAL RESEARCH

MTORC1 regulates cardiac function and myocyte survival through 4E-BP1 inhibition in mice

(2010) Denghong Zhang et al.   JOURNAL OF CLINICAL INVESTIGATION

Erratum: Corrigendum: The p110δ structure: mechanisms for selectivity and potency of new PI(3)K inhibitors

(2010) Alex Berndt et al.   Nature Chemical Biology

Combining Targeted Therapies: Practical Issues to Consider at the Bench and Bedside

(2010) J. Rodon et al.   ONCOLOGIST

Important roles of PI3K  in osteoclastogenesis and bone homeostasis

(2010) H. Kang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Cancer-derived mutations in the regulatory subunit p85  of phosphoinositide 3-kinase function through the catalytic subunit p110 

(2010) M. Sun et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

B Cell Receptor Signaling: Picky About PI3Ks

(2010) J. J. Limon et al.   Science Signaling

The PI3K Isoforms p110  and p110  Are Essential for Pre-B Cell Receptor Signaling and B Cell Development

(2010) F. Ramadani et al.   Science Signaling

Control of secretory granule access to the plasma membrane by PI3 kinase-γ

(2010) Patrick E MacDonald   Islets

Functional differences between two classes of oncogenic mutation in the PIK3CA gene

(2009) Claire Chaussade et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Evidence for a role for the p110-α isoform of PI3K in skeletal function

(2009) Andrew Grey et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Form and flexibility in phosphoinositide 3-kinases

(2009) Roger Williams et al.   BIOCHEMICAL SOCIETY TRANSACTIONS

The role of Akt1 in terminal stages of endochondral bone formation: Angiogenesis and ossification

(2009) Veronica Ulici et al.   BONE

Somatic Mutations in p85α Promote Tumorigenesis through Class IA PI3K Activation

(2009) Bijay S. Jaiswal et al.   CANCER CELL

Cardiac regulation by phosphoinositide 3-kinases and PTEN

(2009) G. Y. Oudit et al.   CARDIOVASCULAR RESEARCH

PI3K p110α and p110β have differential effects on Akt activation and protection against oxidative stress-induced apoptosis in myoblasts

(2009) R W Matheny et al.   CELL DEATH AND DIFFERENTIATION

Dominant Role of the p110β Isoform of PI3K over p110α in Energy Homeostasis Regulation by POMC and AgRP Neurons

(2009) Hind Al-Qassab et al.   Cell Metabolism

PI 3-kinase and cancer: changing accents

(2009) Peter K Vogt et al.   CURRENT OPINION IN GENETICS & DEVELOPMENT

Insulin Granule Recruitment and Exocytosis Is Dependent on p110  in Insulinoma and Human  -Cells

(2009) G. M. Pigeau et al.   DIABETES

1205 A first-in-human Phase I study to evaluate the pan-PI3K inhibitor GDC-0941 administered QD or BID in patients with advanced solid tumours

(2009) D.D. Von Hoff et al.   EJC SUPPLEMENTS

Effects of PI3K inhibition and low docosahexaenoic acid on cognition and behavior

(2009) Sathyajit S. Bandaru et al.   PHYSIOLOGY & BEHAVIOR

PI3Kγ-deficient mice have reduced levels of allergen-induced eosinophilic inflammation and airway remodeling

(2008) Dae Hyun Lim et al.   AMERICAN JOURNAL OF PHYSIOLOGY-LUNG CELLULAR AND MOLECULAR PHYSIOLOGY

Investigating the role of class-IA PI 3-kinase isoforms in adipocyte differentiation

(2008) Ji Eun Kim et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Phosphoinositide 3-kinase signalling in the vascular system

(2008) F. Morello et al.   CARDIOVASCULAR RESEARCH

Genetic and Pharmacological Targeting of Phosphoinositide 3-Kinase-γ Reduces Atherosclerosis and Favors Plaque Stability by Modulating Inflammatory Processes

(2008) Anne Fougerat et al.   CIRCULATION

Essential role of phosphoinositide 3-kinase gamma in eosinophil chemotaxis within acute pulmonary inflammation

(2008) Matthew Thomas et al.   IMMUNOLOGY

Dual ERK and phosphatidylinositol 3‐kinase pathways control airway smooth muscle proliferation: Differences in asthma

(2008) Janette K. Burgess et al.   JOURNAL OF CELLULAR PHYSIOLOGY

Acute effects of leptin require PI3K signaling in hypothalamic proopiomelanocortin neurons in mice

(2008) Jennifer W. Hill et al.   JOURNAL OF CLINICAL INVESTIGATION

Angiogenesis selectively requires the p110α isoform of PI3K to control endothelial cell migration

(2008) Mariona Graupera et al.   NATURE

Essential roles of PI(3)K–p110β in cell growth, metabolism and tumorigenesis

(2008) Shidong Jia et al.   NATURE

The p110  isoform of phosphoinositide 3-kinase signals downstream of G protein-coupled receptors and is functionally redundant with p110 

(2008) J. Guillermet-Guibert et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Phosphoinositide 3-Kinase p110  Activity: Key Role in Metabolism and Mammary Gland Cancer but Not Development

(2008) E. Ciraolo et al.   Science Signaling