Computer-Aided Targeting of the PI3K/Akt/mTOR Pathway: Toxicity Reduction and Therapeutic Opportunities

Knockdown of cancerous inhibitor of protein phosphatase 2A may sensitize NSCLC cells to cisplatin

(2014) L Wei et al.   CANCER GENE THERAPY

Abstract 3258: Discovery and characterization of SAR260301, a novel PI3Kβ-selective inhibitor in clinical development for the treatment of PTEN-deficient tumors .

(2014) Angela Virone-Oddos et al.   CANCER RESEARCH

Ceramide inhibits insulin-stimulated Akt phosphorylation through activation of Rheb/mTORC1/S6K signaling in skeletal muscle

(2014) Chang-Ting Hsieh et al.   CELLULAR SIGNALLING

Cotargeting of Epidermal Growth Factor Receptor and PI3K Overcomes PI3K-Akt Oncogenic Dependence in Pancreatic Ductal Adenocarcinoma

(2014) M. H. Wong et al.   CLINICAL CANCER RESEARCH

Picking the Point of Inhibition: A Comparative Review of PI3K/AKT/mTOR Pathway Inhibitors

(2014) R. Dienstmann et al.   MOLECULAR CANCER THERAPEUTICS

Endocrinization of FGF1 produces a neomorphic and potent insulin sensitizer

(2014) Jae Myoung Suh et al.   NATURE

PI3K and cancer: lessons, challenges and opportunities

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

Targeting c-MYC by antagonizing PP2A inhibitors in breast cancer

(2014) M. Janghorban et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Zinc oxide nanoparticles induce apoptosis by enhancement of autophagy via PI3K/Akt/mTOR inhibition

(2014) Ruchi Roy et al.   TOXICOLOGY LETTERS

A Diverse Array of Cancer-Associated MTOR Mutations Are Hyperactivating and Can Predict Rapamycin Sensitivity

(2014) B. C. Grabiner et al.   Cancer Discovery

Targeting PI3K/Akt/mTOR Signaling in Cancer

(2014) Camillo Porta et al.   Frontiers in Oncology

Cancerous Inhibitor of Protein Phosphatase 2A, an Emerging Human Oncoprotein and a Potential Cancer Therapy Target

(2013) A. Khanna et al.   CANCER RESEARCH

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

Molecular Pathways: Adipose Inflammation as a Mediator of Obesity-Associated Cancer

(2013) L. R. Howe et al.   CLINICAL CANCER RESEARCH

Roles of EGFR, PI3K, AKT, and mTOR in Heavy Metal-Induced Cancer

(2013) Richard L. Carpenter et al.   CURRENT CANCER DRUG TARGETS

Epidemiology and Molecular Mechanisms Tying Obesity, Diabetes, and the Metabolic Syndrome With Cancer

(2013) E. J. Gallagher et al.   DIABETES CARE

Overcoming resistance to mTOR inhibition for enhanced strategies in clinical trials

(2013) Aung Naing   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Manipulation of Cardiac Phosphatidylinositol 3-Kinase (PI3K)/Akt Signaling by Apoptosis Regulator through Modulating IAP Expression (ARIA) Regulates Cardiomyocyte Death during Doxorubicin-induced Cardiomyopathy

(2013) Youhei Kitamura et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

PI3K Inhibitors as Novel Cancer Therapies: Implications for Cardiovascular Medicine

(2013) Brent A. McLean et al.   JOURNAL OF CARDIAC FAILURE

Binding selectivity studies of PKBα using molecular dynamics simulation and free energy calculations

(2013) Shi-Feng Chen et al.   JOURNAL OF MOLECULAR MODELING

Theoretical studies on beta and delta isoform-specific binding mechanisms of phosphoinositide 3-kinase inhibitors

(2013) Jingyu Zhu et al.   Molecular BioSystems

Development of PI3K inhibitors: lessons learned from early clinical trials

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

A Hydroxylated Metabolite of Flame-Retardant PBDE-47 Decreases the Survival, Proliferation, and Neuronal Differentiation of Primary Cultured Adult Neural Stem Cells and Interferes with Signaling of ERK5 MAP Kinase and Neurotrophin 3

(2013) Tan Li et al.   TOXICOLOGICAL SCIENCES

Make Yourself at Home: Viral Hijacking of the PI3K/Akt Signaling Pathway

(2013) Nora Diehl et al.   Viruses-Basel

Exploring the selectivity of PI3Kα and mTOR inhibitors by 3D-QSAR, molecular dynamics simulations and MM/GBSA binding free energy decomposition

(2013) Feng Wu et al.   MedChemComm

Regulation of AKT gene expression by cisplatin

(2013) JUN ZHANG et al.   Oncology Letters

Senescence Sensitivity of Breast Cancer Cells Is Defined by Positive Feedback Loop between CIP2A and E2F1

(2013) Anni Laine et al.   Cancer Discovery

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

Abstract 3748: NVP-BYL719, a novel PI3Kalpha selective inhibitor with all the characteristics required for clinical development as an anti-cancer agent

(2012) Christine M. Fritsch et al.   CANCER RESEARCH

The Role and Therapeutic Potential of Ser/Thr Phosphatase PP2A in Apoptotic Signalling Networks in Human Cancer Cells

(2012) V. Janssens et al.   CURRENT MOLECULAR MEDICINE

Ceramide Mediates Vascular Dysfunction in Diet-Induced Obesity by PP2A-Mediated Dephosphorylation of the eNOS-Akt Complex

(2012) Q.-J. Zhang et al.   DIABETES

Targeting the PI3K signaling pathway in cancer therapy

(2012) Chandra Bartholomeusz et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

The biogenesis of active protein phosphatase 2A holoenzymes: a tightly regulated process creating phosphatase specificity

(2012) Ward Sents et al.   FEBS Journal

Microcystin-LR (MCLR) Induces a Compensation of PP2A Activity Mediated by α4 Protein in HEK293 Cells

(2012) Tan Li et al.   International Journal of Biological Sciences

Selective Inhibition of Phosphoinositide 3-Kinase p110α Preserves Lymphocyte Function

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

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

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

Optimal homeostasis necessitates bistable control

(2012) G. Wang   Journal of the Royal Society Interface

Bioinformatics and variability in drug response: a protein structural perspective

(2012) J. L. Lahti et al.   Journal of the Royal Society Interface

Hepatitis C Virus Activates the mTOR/S6K1 Signaling Pathway in Inhibiting IRS-1 Function for Insulin Resistance

(2012) S. K. Bose et al.   JOURNAL OF VIROLOGY

Abstract A171: A potent and selective PI3K inhibitor, INK1117, targets human cancers harboring oncogenic PIK3CA mutations.

(2012) K. Jessen et al.   MOLECULAR CANCER THERAPEUTICS

Microcystin-LR Induces Ceramide to Regulate PP2A and Destabilize Cytoskeleton in HEK293 Cells

(2012) Tan Li et al.   TOXICOLOGICAL SCIENCES

JNK-Dependent Stat3 Phosphorylation Contributes to Akt Activation in Response to Arsenic Exposure

(2012) J. Liu et al.   TOXICOLOGICAL SCIENCES

Cardioprotective effect of salvianolic acid B against arsenic trioxide-induced injury in cardiac H9c2 cells via the PI3K/Akt signal pathway

(2012) Min Wang et al.   TOXICOLOGY LETTERS

Cell Type-Specific Activation of AKT and ERK Signaling Pathways by Small Negatively-Charged Magnetic Nanoparticles

(2012) Jens Rauch et al.   Scientific Reports

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

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

Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799

(2011) Jun Ohwada et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Molecular dynamics simulations and drug discovery

(2011) Jacob D Durrant et al.   BMC BIOLOGY

Understanding the benefit of metformin use in cancer treatment

(2011) Ryan JO Dowling et al.   BMC Medicine

The Selective Class I PI3K Inhibitor CH5132799 Targets Human Cancers Harboring Oncogenic PIK3CA Mutations

(2011) H. Tanaka et al.   CLINICAL CANCER RESEARCH

Physiological cardiac remodelling in response to endurance exercise training: cellular and molecular mechanisms

(2011) Georgina M Ellison et al.   HEART

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

The future of molecular dynamics simulations in drug discovery

(2011) David W. Borhani et al.   JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

Molecular simulation of a series of benzothiazole PI3Kα inhibitors: probing the relationship between structural features, anti-tumor potency and selectivity

(2011) Jinan Wang et al.   JOURNAL OF MOLECULAR MODELING

Characterization of molecular recognition of Phosphoinositide-3-kinase α inhibitor through molecular dynamics simulation

(2011) Yiping Li et al.   JOURNAL OF MOLECULAR MODELING

Isoform-Selective Inhibition of Phosphoinositide 3-Kinase: Identification of a New Region of Nonconserved Amino Acids Critical for p110  Inhibition

(2011) Z. Zheng et al.   MOLECULAR PHARMACOLOGY

α4 is highly expressed in carcinogen-transformed human cells and primary human cancers

(2011) L-P Chen et al.   ONCOGENE

Cadmium Increases HIF-1 and VEGF Expression through ROS, ERK, and AKT Signaling Pathways and Induces Malignant Transformation of Human Bronchial Epithelial Cells

(2011) Yi Jing et al.   TOXICOLOGICAL SCIENCES

miR-190-Mediated Downregulation of PHLPP Contributes to Arsenic-Induced Akt Activation and Carcinogenesis

(2011) Kevin Beezhold et al.   TOXICOLOGICAL SCIENCES

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

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

Metformin and rapamycin have distinct effects on the AKT pathway and proliferation in breast cancer cells

(2010) Mahvash Zakikhani et al.   BREAST CANCER RESEARCH AND TREATMENT

Molecular Mechanisms of Cardiovascular Toxicity of Targeted Cancer Therapeutics

(2010) Hui Cheng et al.   CIRCULATION RESEARCH

New Strategies in Kidney Cancer: Therapeutic Advances through Understanding the Molecular Basis of Response and Resistance

(2010) B. I. Rini   CLINICAL CANCER RESEARCH

Rapid targeted mutational analysis of human tumours: a clinical platform to guide personalized cancer medicine

(2010) Dora Dias-Santagata et al.   EMBO Molecular Medicine

p53 Plays an Important Role in Cell Fate Determination after Exposure to Microcystin-LR

(2010) Shota Takumi et al.   ENVIRONMENTAL HEALTH PERSPECTIVES

Docking Studies on Isoform-Specific Inhibition of Phosphoinositide-3-Kinases

(2010) Dima A. Sabbah et al.   Journal of Chemical Information and Modeling

Molecular Dynamics Simulations and Elastic Network Analysis of Protein Kinase B (Akt/PKB) Inactivation

(2010) Shu Cheng et al.   Journal of Chemical Information and Modeling

The PI3K Pathway As Drug Target in Human Cancer

(2010) Kevin D. Courtney et al.   JOURNAL OF CLINICAL ONCOLOGY

HPV-associated head and neck cancer: a virus-related cancer epidemic

(2010) Shanthi Marur et al.   LANCET ONCOLOGY

mTOR: from growth signal integration to cancer, diabetes and ageing

(2010) Roberto Zoncu et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

CIP2A mediates effects of bortezomib on phospho-Akt and apoptosis in hepatocellular carcinoma cells

(2010) K-F Chen et al.   ONCOGENE

Molecular distinction between physiological and pathological cardiac hypertrophy: Experimental findings and therapeutic strategies

(2010) Bianca C. Bernardo et al.   PHARMACOLOGY & THERAPEUTICS

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

Pathway-Based Identification of Biomarkers for Targeted Therapeutics: Personalized Oncology with PI3K Pathway Inhibitors

(2010) J. N. Andersen et al.   Science Translational Medicine

Cardiac regulation by phosphoinositide 3-kinases and PTEN

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

Single-Molecule Detection of Epidermal Growth Factor Receptor Mutations in Plasma by Microfluidics Digital PCR in Non-Small Cell Lung Cancer Patients

(2009) T. K.F. Yung et al.   CLINICAL CANCER RESEARCH

The Role of the Akt/mTOR Pathway in Tobacco Carcinogen-Induced Lung Tumorigenesis

(2009) R. M. Memmott et al.   CLINICAL CANCER RESEARCH

Role of a Novel PH-Kinase Domain Interface in PKB/Akt Regulation: Structural Mechanism for Allosteric Inhibition

(2009) Véronique Calleja et al.   PLOS BIOLOGY

Phosphorylation of IRS proteins, insulin action, and insulin resistance

(2008) Sigalit Boura-Halfon et al.   AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM

p38 MAP kinase mediates arsenite-induced apoptosis through FOXO3a activation and induction of Bim transcription

(2008) Beibei Cai et al.   APOPTOSIS

Mechanism and Management of AKT Inhibitor-Induced Hyperglycemia

(2008) M.-C. Crouthamel et al.   CLINICAL CANCER RESEARCH

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

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

Dual Role of Interleukin-6 in Regulating Insulin Sensitivity in Murine Skeletal Muscle

(2008) I. Nieto-Vazquez et al.   DIABETES

Targeting the PI3K/Akt/mTOR pathway: Effective combinations and clinical considerations

(2008) J LOPICCOLO et al.   DRUG RESISTANCE UPDATES

Raw Single-Wall Carbon Nanotubes Induce Oxidative Stress and Activate MAPKs, AP-1, NF-κB, and Akt in Normal and Malignant Human Mesothelial Cells

(2008) Maricica Pacurari et al.   ENVIRONMENTAL HEALTH PERSPECTIVES

S6K Directly Phosphorylates IRS-1 on Ser-270 to Promote Insulin Resistance in Response to TNF-α Signaling through IKK2

(2008) Jin Zhang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The TORrid affairs of viruses: effects of mammalian DNA viruses on the PI3K–Akt–mTOR signalling pathway

(2008) Nicholas J. Buchkovich et al.   NATURE REVIEWS MICROBIOLOGY

PTEN: a new guardian of the genome

(2008) Y Yin et al.   ONCOGENE

The PTEN–PI3K pathway: of feedbacks and cross-talks

(2008) A Carracedo et al.   ONCOGENE

Methylmercury Toxicity and Nrf2-dependent Detoxification in Astrocytes

(2008) Ling Wang et al.   TOXICOLOGICAL SCIENCES

Multiple pathways regulated by the tumor suppressor PP2A in transformation

(2008) Jukka Westermarck et al.   TRENDS IN MOLECULAR MEDICINE

Cancer as robust intrinsic state of endogenous molecular-cellular network shaped by evolution

(2007) Ping Ao et al.   MEDICAL HYPOTHESES