PI3K and cancer: lessons, challenges and opportunities

Targeting TOR dependence in cancer

(2015)   Oncotarget

mTOR inhibitor efficacy is determined by the eIF4E/4E-BP ratio

(2015) Tommy Alain et al.   Oncotarget

Signaling by the Phosphoinositide 3-Kinase Family in Immune Cells

(2013) Klaus Okkenhaug   Annual Review of Immunology

Immune responses of macrophages and dendritic cells regulated by mTOR signalling

(2013) Karl Katholnig et al.   BIOCHEMICAL SOCIETY TRANSACTIONS

P110 -mediated constitutive PI3K signaling limits the efficacy of p110 -selective inhibition in mantle cell lymphoma, particularly with multiple relapse

(2013) S. Iyengar et al.   BLOOD

Regulation of FANCD2 by the mTOR Pathway Contributes to the Resistance of Cancer Cells to DNA Double-Strand Breaks

(2013) C. Shen et al.   CANCER RESEARCH

Optimal Targeting of HER2–PI3K Signaling in Breast Cancer: Mechanistic Insights and Clinical Implications

(2013) Brent N. Rexer et al.   CANCER RESEARCH

Conditional Loss of ErbB3 Delays Mammary Gland Hyperplasia Induced by Mutant PIK3CA without Affecting Mammary Tumor Latency, Gene Expression, or Signaling

(2013) Christian D. Young et al.   CANCER RESEARCH

Combination of Antibody That Inhibits Ligand-Independent HER3 Dimerization and a p110  Inhibitor Potently Blocks PI3K Signaling and Growth of HER2+ Breast Cancers

(2013) J. T. Garrett et al.   CANCER RESEARCH

eIF4B Phosphorylation by Pim Kinases Plays a Critical Role in Cellular Transformation by Abl Oncogenes

(2013) J. Yang et al.   CANCER RESEARCH

Phosphorylation of Ribosomal Protein S6 Attenuates DNA Damage and Tumor Suppression during Development of Pancreatic Cancer

(2013) A. Khalaileh et al.   CANCER RESEARCH

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

(2013) Ralph Fritsch et al.   CELL

PI3K-δ and PI3K-γ Inhibition by IPI-145 Abrogates Immune Responses and Suppresses Activity in Autoimmune and Inflammatory Disease Models

(2013) David G. Winkler et al.   CHEMISTRY & BIOLOGY

Targeting Activated Akt with GDC-0068, a Novel Selective Akt Inhibitor That Is Efficacious in Multiple Tumor Models

(2013) J. Lin et al.   CLINICAL CANCER RESEARCH

Concomitant BRAF and PI3K/mTOR Blockade Is Required for Effective Treatment of BRAFV600E Colorectal Cancer

(2013) E. M. Coffee et al.   CLINICAL CANCER RESEARCH

mTOR and lymphocyte metabolism

(2013) Hu Zeng et al.   CURRENT OPINION IN IMMUNOLOGY

Adoptive T Cell Transfer for Cancer Immunotherapy in the Era of Synthetic Biology

(2013) Michael Kalos et al.   IMMUNITY

Deciphering and Reversing Tumor Immune Suppression

(2013) Greg T. Motz et al.   IMMUNITY

Mechanism of Action of Conventional and Targeted Anticancer Therapies: Reinstating Immunosurveillance

(2013) Laurence Zitvogel et al.   IMMUNITY

Oncology Meets Immunology: The Cancer-Immunity Cycle

(2013) Daniel S. Chen et al.   IMMUNITY

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

mTOR regulates DNA damage response through NF-κB-mediated FANCD2 pathway in hematopoietic cells

(2013) F Guo et al.   LEUKEMIA

Dual PI3K/AKT/mTOR Inhibitor BEZ235 Synergistically Enhances the Activity of JAK2 Inhibitor against Cultured and Primary Human Myeloproliferative Neoplasm Cells

(2013) W. Fiskus et al.   MOLECULAR CANCER THERAPEUTICS

BAY 80-6946 Is a Highly Selective Intravenous PI3K Inhibitor with Potent p110α and p110δ Activities in Tumor Cell Lines and Xenograft Models

(2013) Ningshu Liu et al.   MOLECULAR CANCER THERAPEUTICS

MEK1 Is Required for PTEN Membrane Recruitment, AKT Regulation, and the Maintenance of Peripheral Tolerance

(2013) Katarina Zmajkovicova et al.   MOLECULAR CELL

K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions

(2013) Jonathan M. Ostrem et al.   NATURE

Small molecule inhibition of the KRAS–PDEδ interaction impairs oncogenic KRAS signalling

(2013) Gunther Zimmermann et al.   NATURE

mTORC1 couples immune signals and metabolic programming to establish Treg-cell function

(2013) Hu Zeng et al.   NATURE

Development of PI3K inhibitors: lessons learned from early clinical trials

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

Everolimus long-term safety and efficacy in subependymal giant cell astrocytoma

(2013) D. A. Krueger et al.   NEUROLOGY

Combination Checkpoint Blockade — Taking Melanoma Immunotherapy to the Next Level

(2013) James L. Riley   NEW ENGLAND JOURNAL OF MEDICINE

Targeting BTK with Ibrutinib in Relapsed Chronic Lymphocytic Leukemia

(2013) John C. Byrd et al.   NEW ENGLAND JOURNAL OF MEDICINE

Characterization of a Tumor-Associated Activating Mutation of the p110β PI 3-Kinase

(2013) Hashem A. Dbouk et al.   PLoS One

Targeting of the MNK-eIF4E axis in blast crisis chronic myeloid leukemia inhibits leukemia stem cell function

(2013) S. Lim et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Myc and mTOR converge on a common node in protein synthesis control that confers synthetic lethality in Myc-driven cancers

(2013) M. Pourdehnad et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Combined targeting of MEK and PI3K/mTOR effector pathways is necessary to effectively inhibit NRAS mutant melanoma in vitro and in vivo

(2013) C. Posch 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

(2013) I. Angulo et al.   SCIENCE

Nuclear PTEN Controls DNA Repair and Sensitivity to Genotoxic Stress

(2013) C. Bassi et al.   SCIENCE

A Tumor Suppressor Complex with GAP Activity for the Rag GTPases That Signal Amino Acid Sufficiency to mTORC1

(2013) L. Bar-Peled et al.   SCIENCE

Amino Acid Deprivation Inhibits TORC1 Through a GTPase-Activating Protein Complex for the Rag Family GTPase Gtr1

(2013) N. Panchaud et al.   Science Signaling

TORC1 Suppression Predicts Responsiveness to RAF and MEK Inhibition in BRAF-Mutant Melanoma

(2013) R. B. Corcoran et al.   Science Translational Medicine

mTORC1 Inhibition Is Required for Sensitivity to PI3K p110  Inhibitors in PIK3CA-Mutant Breast Cancer

(2013) M. Elkabets et al.   Science Translational Medicine

What a Tangled Web We Weave: Emerging Resistance Mechanisms to Inhibition of the Phosphoinositide 3-Kinase Pathway

(2013) S. J. Klempner et al.   Cancer Discovery

Frequent Mutation of the PI3K Pathway in Head and Neck Cancer Defines Predictive Biomarkers

(2013) V. W. Y. Lui et al.   Cancer Discovery

Regulation of Immune Responses by mTOR

(2012) Jonathan D. Powell et al.   Annual Review of Immunology

Decreased mitochondrial apoptotic priming underlies stroma-mediated treatment resistance in chronic lymphocytic leukemia

(2012) M. S. Davids et al.   BLOOD

Acquired resistance mechanisms to tyrosine kinase inhibitors in lung cancer with activating epidermal growth factor receptor mutation—diversity, ductility, and destiny

(2012) Kenichi Suda et al.   CANCER AND METASTASIS REVIEWS

Burkitt Lymphoma: Much More than MYC

(2012) David Dominguez-Sola et al.   CANCER CELL

Synergy between PI3K Signaling and MYC in Burkitt Lymphomagenesis

(2012) Sandrine Sander et al.   CANCER CELL

Targeting Nonclassical Oncogenes for Therapy in T-ALL

(2012) Prem S. Subramaniam et al.   CANCER CELL

Dual Inhibition of Bcl-2 and Bcl-xL Strikingly Enhances PI3K Inhibition-Induced Apoptosis in Human Myeloid Leukemia Cells through a GSK3- and Bim-Dependent Mechanism

(2012) M. Rahmani et al.   CANCER RESEARCH

Trastuzumab-Resistant Cells Rely on a HER2-PI3K-FoxO-Survivin Axis and Are Sensitive to PI3K Inhibitors

(2012) A. Chakrabarty et al.   CANCER RESEARCH

Pten Loss and RAS/MAPK Activation Cooperate to Promote EMT and Metastasis Initiated from Prostate Cancer Stem/Progenitor Cells

(2012) D. J. Mulholland et al.   CANCER RESEARCH

mTOR Signaling in Growth Control and Disease

(2012) Mathieu Laplante et al.   CELL

A Potent Combination of the Novel PI3K Inhibitor, GDC-0941, with Imatinib in Gastrointestinal Stromal Tumor Xenografts: Long-Lasting Responses after Treatment Withdrawal

(2012) G. Floris et al.   CLINICAL CANCER RESEARCH

The Clinical Effect of the Dual-Targeting Strategy Involving PI3K/AKT/mTOR and RAS/MEK/ERK Pathways in Patients with Advanced Cancer

(2012) T. Shimizu et al.   CLINICAL CANCER RESEARCH

Resistance to BRAF Inhibition in BRAF-Mutant Colon Cancer Can Be Overcome with PI3K Inhibition or Demethylating Agents

(2012) M. Mao et al.   CLINICAL CANCER RESEARCH

Dual mTORC1/2 and HER2 Blockade Results in Antitumor Activity in Preclinical Models of Breast Cancer Resistant to Anti-HER2 Therapy

(2012) C. Garcia-Garcia et al.   CLINICAL CANCER RESEARCH

Targeting the microenvironment in chronic lymphocytic leukemia is changing the therapeutic landscape

(2012) Jan A. Burger   CURRENT OPINION IN ONCOLOGY

PIM1 kinase as a target for cancer therapy

(2012) Anna Lena Merkel et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

An overview of the mTOR pathway as a target in cancer therapy

(2012) Ryan D Gentzler et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Selective Inhibition of Phosphoinositide 3-Kinase p110α Preserves Lymphocyte Function

(2012) Lomon So et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

An activating Pik3ca mutation coupled with Pten loss is sufficient to initiate ovarian tumorigenesis in mice

(2012) Kathryn M. Kinross et al.   JOURNAL OF CLINICAL INVESTIGATION

Targeting the B-Cell Lymphoma/Leukemia 2 Family in Cancer

(2012) Matthew S. Davids et al.   JOURNAL OF CLINICAL ONCOLOGY

Bruton Tyrosine Kinase Inhibitor Ibrutinib (PCI-32765) Has Significant Activity in Patients With Relapsed/Refractory B-Cell Malignancies

(2012) Ranjana H. Advani et al.   JOURNAL OF CLINICAL ONCOLOGY

Chemosensitization of Cancer Cells by KU-0060648, a Dual Inhibitor of DNA-PK and PI-3K

(2012) J. M. Munck et al.   MOLECULAR CANCER THERAPEUTICS

Characterization of the Mechanism of Action of the Pan Class I PI3K Inhibitor NVP-BKM120 across a Broad Range of Concentrations

(2012) S. M. Brachmann et al.   MOLECULAR CANCER THERAPEUTICS

TBC1D7 Is a Third Subunit of the TSC1-TSC2 Complex Upstream of mTORC1

(2012) Christian C. Dibble et al.   MOLECULAR CELL

Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR

(2012) Anirudh Prahallad et al.   NATURE

Burkitt lymphoma pathogenesis and therapeutic targets from structural and functional genomics

(2012) Roland Schmitz et al.   NATURE

The translational landscape of mTOR signalling steers cancer initiation and metastasis

(2012) Andrew C. Hsieh et al.   NATURE

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

(2012) Marjorie J Lindhurst et al.   NATURE GENETICS

De novo germline and postzygotic mutations in AKT3, PIK3R2 and PIK3CA cause a spectrum of related megalencephaly syndromes

(2012) Jean-Baptiste Rivière 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

Combined BRAF and MEK Inhibition in Melanoma with BRAF V600 Mutations

(2012) Keith T. Flaherty et al.   NEW ENGLAND JOURNAL OF MEDICINE

Physiological Levels of Pik3caH1047R Mutation in the Mouse Mammary Gland Results in Ductal Hyperplasia and Formation of ERα-Positive Tumors

(2012) Anjali Tikoo et al.   PLoS One

Genome Sequencing Identifies a Basis for Everolimus Sensitivity

(2012) G. Iyer et al.   SCIENCE

G Protein-Coupled Receptor-Mediated Activation of p110  by G   Is Required for Cellular Transformation and Invasiveness

(2012) H. A. Dbouk et al.   Science Signaling

EGFR-Mediated Reactivation of MAPK Signaling Contributes to Insensitivity of BRAF -Mutant Colorectal Cancers to RAF Inhibition with Vemurafenib

(2012) Ryan B. Corcoran et al.   Cancer Discovery

PI3K Inhibition Impairs BRCA1/2 Expression and Sensitizes BRCA-Proficient Triple-Negative Breast Cancer to PARP Inhibition

(2012) Yasir H. Ibrahim et al.   Cancer Discovery

Combining a PI3K Inhibitor with a PARP Inhibitor Provides an Effective Therapy for BRCA1-Related Breast Cancer

(2012) Ashish Juvekar et al.   Cancer Discovery

GS-1101: A Delta-Specific PI3K Inhibitor in Chronic Lymphocytic Leukemia

(2012) Ines M. Macias-Perez et al.   Current Hematologic Malignancy Reports

The PI3K, Metabolic, and Autophagy Networks: Interactive Partners in Cellular Health and Disease

(2011) Naval P. Shanware et al.   Annual Review of Pharmacology and Toxicology

Both p110α and p110β isoforms of PI3K can modulate the impact of loss-of-function of the PTEN tumour suppressor

(2011) Inma M. Berenjeno et al.   BIOCHEMICAL JOURNAL

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

Receptor Tyrosine Kinases and TLR/IL1Rs Unexpectedly Activate Myeloid Cell PI3Kγ, A Single Convergent Point Promoting Tumor Inflammation and Progression

(2011) Michael C. Schmid et al.   CANCER CELL

A Lipid Kinase Cousin Cooperates to Promote Cancer

(2011) Brandon Beagle et al.   CANCER CELL

AKT Inhibition Relieves Feedback Suppression of Receptor Tyrosine Kinase Expression and Activity

(2011) Sarat Chandarlapaty et al.   CANCER CELL

mTOR Kinase Inhibitor AZD8055 Enhances the Immunotherapeutic Activity of an Agonist CD40 Antibody in Cancer Treatment

(2011) Q. Jiang et al.   CANCER RESEARCH

Akt-Dependent Glucose Metabolism Promotes Mcl-1 Synthesis to Maintain Cell Survival and Resistance to Bcl-2 Inhibition

(2011) J. L. Coloff et al.   CANCER RESEARCH

Immunotherapy with PI3K Inhibitor and Toll-Like Receptor Agonist Induces IFN- +IL-17+ Polyfunctional T Cells That Mediate Rejection of Murine Tumors

(2011) N. A. Marshall et al.   CANCER RESEARCH

Pim Kinase Inhibitors Sensitize Prostate Cancer Cells to Apoptosis Triggered by Bcl-2 Family Inhibitor ABT-737

(2011) J. H. Song et al.   CANCER RESEARCH

PTEN Loss Confers BRAF Inhibitor Resistance to Melanoma Cells through the Suppression of BIM Expression

(2011) K. H. T. Paraiso et al.   CANCER RESEARCH

Therapeutic Inhibition of MAP Kinase Interacting Kinase Blocks Eukaryotic Initiation Factor 4E Phosphorylation and Suppresses Outgrowth of Experimental Lung Metastases

(2011) B. W. Konicek et al.   CANCER RESEARCH

Activation of mTORC2 by Association with the Ribosome

(2011) Vittoria Zinzalla et al.   CELL

BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc

(2011) Jake E. Delmore et al.   CELL

Hallmarks of Cancer: The Next Generation

(2011) Douglas Hanahan et al.   CELL

Transient PI3K Inhibition Induces Apoptosis and Overcomes HGF-Mediated Resistance to EGFR-TKIs in EGFR Mutant Lung Cancer

(2011) I. S. Donev et al.   CLINICAL CANCER RESEARCH

A Central Role for mTOR Kinase in Homeostatic Proliferation Induced CD8+ T Cell Memory and Tumor Immunity

(2011) Qingsheng Li et al.   IMMUNITY

Targeting AMPK in the treatment of malignancies

(2011) Eliza Vakana et al.   JOURNAL OF CELLULAR BIOCHEMISTRY

Next-generation mTOR inhibitors in clinical oncology: how pathway complexity informs therapeutic strategy

(2011) Seth A. Wander et al.   JOURNAL OF CLINICAL INVESTIGATION

Phosphatidylinositol 3-Kinase and Antiestrogen Resistance in Breast Cancer

(2011) Todd W. Miller et al.   JOURNAL OF CLINICAL ONCOLOGY

First-in-Man Clinical Trial of the Oral Pan-AKT Inhibitor MK-2206 in Patients With Advanced Solid Tumors

(2011) Timothy A. Yap et al.   JOURNAL OF CLINICAL ONCOLOGY

Phosphoinositide-3-Kinase Catalytic Alpha and KRAS Mutations are Important Predictors of Resistance to Therapy with Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Patients with Advanced Non-small Cell Lung Cancer

(2011) Vienna Ludovini et al.   Journal of Thoracic Oncology

Targeted inhibition of mTORC1 and mTORC2 by active-site mTOR inhibitors has cytotoxic effects in T-cell acute lymphoblastic leukemia

(2011) C Evangelisti et al.   LEUKEMIA

NOTCH and phosphatidylinositide 3-kinase/phosphatase and tensin homolog deleted on chromosome ten/AKT/mammalian target of rapamycin (mTOR) signaling in T-cell development and T-cell acute lymphoblastic leukemia

(2011) Dongmei Guo et al.   LEUKEMIA & LYMPHOMA

Rapamycin Induces Bad Phosphorylation in Association with Its Resistance to Human Lung Cancer Cells

(2011) Y. Liu et al.   MOLECULAR CANCER THERAPEUTICS

Structure of Lipid Kinase p110β/p85β Elucidates an Unusual SH2-Domain-Mediated Inhibitory Mechanism

(2011) Xuxiao Zhang et al.   MOLECULAR CELL

RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia

(2011) Johannes Zuber et al.   NATURE

Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia

(2011) Mark A. Dawson et al.   NATURE

The kinase mTOR regulates the differentiation of helper T cells through the selective activation of signaling by mTORC1 and mTORC2

(2011) Greg M Delgoffe et al.   NATURE IMMUNOLOGY

Oncogenic PIK3CA-driven mammary tumors frequently recur via PI3K pathway–dependent and PI3K pathway–independent mechanisms

(2011) Pixu Liu et al.   NATURE MEDICINE

Rapamycin passes the torch: a new generation of mTOR inhibitors

(2011) Don Benjamin et al.   NATURE REVIEWS DRUG DISCOVERY

Everolimus in Postmenopausal Hormone-Receptor–Positive Advanced Breast Cancer

(2011) José Baselga et al.   NEW ENGLAND JOURNAL OF MEDICINE

Requirement for ribosomal protein S6 kinase 1 to mediate glycolysis and apoptosis resistance induced by Pten deficiency

(2011) P. Tandon et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

PI3K-targeted therapy can be evaded by gene amplification along the MYC-eukaryotic translation initiation factor 4E (eIF4E) axis

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

Targeting MYC dependence in cancer by inhibiting BET bromodomains

(2011) J. A. Mertz et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structural Basis for Activation and Inhibition of Class I Phosphoinositide 3-Kinases

(2011) Oscar Vadas et al.   Science Signaling

PI3K and STAT3: A New Alliance

(2011) P. K. Vogt et al.   Cancer Discovery

PI3K  Inhibitors in Cancer: Rationale and Serendipity Merge in the Clinic

(2011) D. A. Fruman et al.   Cancer Discovery

mTOR Kinase Inhibition Causes Feedback-Dependent Biphasic Regulation of AKT Signaling

(2011) V. S. Rodrik-Outmezguine et al.   Cancer Discovery

The APL Paradigm and the “Co-Clinical Trial” Project

(2011) Caterina Nardella et al.   Cancer Discovery

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

Characterization of PF-4708671, a novel and highly specific inhibitor of p70 ribosomal S6 kinase (S6K1)

(2010) Laura R. Pearce et al.   BIOCHEMICAL JOURNAL

4E-BP1 Is a Key Effector of the Oncogenic Activation of the AKT and ERK Signaling Pathways that Integrates Their Function in Tumors

(2010) Qing-Bai She et al.   CANCER CELL

Pim 1 kinase inhibitor ETP-45299 suppresses cellular proliferation and synergizes with PI3K inhibition

(2010) Carmen Blanco-Aparicio et al.   CANCER LETTERS

Beyond Rapalog Therapy: Preclinical Pharmacology and Antitumor Activity of WYE-125132, an ATP-Competitive and Specific Inhibitor of mTORC1 and mTORC2

(2010) K. Yu et al.   CANCER RESEARCH

Drugging the PI3 Kinome: From Chemical Tools to Drugs in the Clinic

(2010) P. Workman et al.   CANCER RESEARCH

Akt inhibitors in clinical development for the treatment of cancer

(2010) Sumanta Kumar Pal et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

An Oscillatory Switch in mTOR Kinase Activity Sets Regulatory T Cell Responsiveness

(2010) Claudio Procaccini et al.   IMMUNITY

B-cell-derived lymphotoxin promotes castration-resistant prostate cancer

(2010) Massimo Ammirante et al.   NATURE

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

(2010) Alex Berndt et al.   Nature Chemical Biology

Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor

(2010) Matthew R Janes et al.   NATURE MEDICINE

The emerging mechanisms of isoform-specific PI3K signalling

(2010) Bart Vanhaesebroeck et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Bifurcation of insulin signaling pathway in rat liver: mTORC1 required for stimulation of lipogenesis, but not inhibition of gluconeogenesis

(2010) Shijie Li 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

Activity of any class IA PI3K isoform can sustain cell proliferation and survival

(2010) L. C. Foukas et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Critical roles for mTORC2- and rapamycin-insensitive mTORC1-complexes in growth and survival of BCR-ABL-expressing leukemic cells

(2010) Nathalie Carayol et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Nuclear phosphoinositide 3-kinase   controls double-strand break DNA repair

(2010) A. Kumar et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Nontoxic Chemical Interdiction of the Epithelial-to-Mesenchymal Transition by Targeting Cap-Dependent Translation

(2009) Brahma Ghosh et al.   ACS Chemical Biology

A small molecule inhibitor of Pim protein kinases blocks the growth of precursor T-cell lymphoblastic leukemia/lymphoma

(2009) Y.-W. Lin et al.   BLOOD

Pim kinase inhibitor, SGI-1776, induces apoptosis in chronic lymphocytic leukemia cells

(2009) L. S. Chen et al.   BLOOD

mTOR Complex 2 Is Required for the Development of Prostate Cancer Induced by Pten Loss in Mice

(2009) David A. Guertin et al.   CANCER CELL

Somatic Mutations in p85α Promote Tumorigenesis through Class IA PI3K Activation

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

PI3K Pathway Activation Mediates Resistance to MEK Inhibitors in KRAS Mutant Cancers

(2009) S. Wee et al.   CANCER RESEARCH

AZD8055 Is a Potent, Selective, and Orally Bioavailable ATP-Competitive Mammalian Target of Rapamycin Kinase Inhibitor with In vitro and In vivo Antitumor Activity

(2009) C. M. Chresta et al.   CANCER RESEARCH

Suppression of HER2/HER3-Mediated Growth of Breast Cancer Cells with Combinations of GDC-0941 PI3K Inhibitor, Trastuzumab, and Pertuzumab

(2009) E. Yao et al.   CLINICAL CANCER RESEARCH

Emerging common themes in regulation of PIKKs and PI3Ks

(2009) Harri Lempiäinen et al.   EMBO JOURNAL

Inhibitors of translation initiation as cancer therapeutics

(2009) Lisa Lindqvist et al.   Future Medicinal Chemistry

The mTOR Kinase Differentially Regulates Effector and Regulatory T Cell Lineage Commitment

(2009) Greg M. Delgoffe et al.   IMMUNITY

Fine tuning the immune response with PI3K

(2009) David A. Fruman et al.   IMMUNOLOGICAL REVIEWS

Targeting tumorigenesis: development and use of mTOR inhibitors in cancer therapy

(2009) RuiRong Yuan et al.   Journal of Hematology & Oncology

Phosphoinositide 3-Kinase p110  Regulates Natural Antibody Production, Marginal Zone and B-1 B Cell Function, and Autoantibody Responses

(2009) C. A. Durand et al.   JOURNAL OF IMMUNOLOGY

mTOR regulates memory CD8 T-cell differentiation

(2009) Koichi Araki et al.   NATURE

Inhibitor hijacking of Akt activation

(2009) Tatsuya Okuzumi et al.   Nature Chemical Biology

Essential function for the GTPase TC21 in homeostatic antigen receptor signaling

(2009) Pilar Delgado et al.   NATURE IMMUNOLOGY

Regulation of Class IA PI 3-kinases: C2 domain-iSH2 domain contacts inhibit p85/p110  and are disrupted in oncogenic p85 mutants

(2009) H. Wu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Differential Requirement of mTOR in Postmitotic Tissues and Tumorigenesis

(2009) C. Nardella et al.   Science Signaling

The emerging safety profile of mTOR inhibitors, a novel class of anticancer agents

(2009) Kamalesh Sankhala et al.   Targeted Oncology

TOR complex 2: a signaling pathway of its own

(2009) Nadine Cybulski et al.   TRENDS IN BIOCHEMICAL SCIENCES

A chemical screen in diverse breast cancer cell lines reveals genetic enhancers and suppressors of sensitivity to PI3K isoform-selective inhibition

(2008) Neil E. Torbett et al.   BIOCHEMICAL JOURNAL

The TSC1–TSC2 complex: a molecular switchboard controlling cell growth

(2008) Jingxiang Huang et al.   BIOCHEMICAL JOURNAL

Characterization of an Akt Kinase Inhibitor with Potent Pharmacodynamic and Antitumor Activity

(2008) N. Rhodes et al.   CANCER RESEARCH

Tenets of PTEN Tumor Suppression

(2008) Leonardo Salmena et al.   CELL

Targeting the PI3K–AKT–mTOR pathway: progress, pitfalls, and promises

(2008) Timothy A Yap et al.   CURRENT OPINION IN PHARMACOLOGY

Ablation of PI3K blocks BCR-ABL leukemogenesis in mice, and a dual PI3K/mTOR inhibitor prevents expansion of human BCR-ABL+ leukemia cells

(2008) Michael G. Kharas et al.   JOURNAL OF CLINICAL INVESTIGATION

Dose- and Schedule-Dependent Inhibition of the Mammalian Target of Rapamycin Pathway With Everolimus: A Phase I Tumor Pharmacodynamic Study in Patients With Advanced Solid Tumors

(2008) Josep Tabernero et al.   JOURNAL OF CLINICAL ONCOLOGY

Effective use of PI3K and MEK inhibitors to treat mutant Kras G12D and PIK3CA H1047R murine lung cancers

(2008) Jeffrey A Engelman et al.   NATURE MEDICINE

Membrane recognition by phospholipid-binding domains

(2008) Mark A. Lemmon   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Sirolimus for Angiomyolipoma in Tuberous Sclerosis Complex or Lymphangioleiomyomatosis

(2008) John J. Bissler et al.   NEW ENGLAND JOURNAL OF MEDICINE

Drug discovery approaches targeting the PI3K/Akt pathway in cancer

(2008) C Garcia-Echeverria et al.   ONCOGENE

PTEN-deficient cancers depend on PIK3CB

(2008) S. Wee et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Sensing and Integration of Erk and PI3K Signals by Myc

(2008) Tae Lee et al.   PLoS Computational Biology

Targeting phosphoinositide 3-kinase—Moving towards therapy

(2007) Romina Marone et al.   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS