Small-molecule inhibitors of the PI3K signaling network

A novel inhibitor of the PI3K/Akt pathway based on the structure of inositol 1,3,4,5,6-pentakisphosphate

(2010) M Falasca et al.   BRITISH JOURNAL OF CANCER

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

(2010) P. Workman et al.   CANCER RESEARCH

The Akt activation inhibitor TCN-P inhibits Akt phosphorylation by binding to the PH domain of Akt and blocking its recruitment to the plasma membrane

(2010) N Berndt et al.   CELL DEATH AND DIFFERENTIATION

PI3K/Akt Signalling Pathway Specific Inhibitors: A Novel Strategy to Sensitize Cancer Cells to Anti-Cancer Drugs

(2010) Marco Falasca   CURRENT PHARMACEUTICAL DESIGN

A Small Molecule Inhibits Akt through Direct Binding to Akt and Preventing Akt Membrane Translocation

(2010) Donghwa Kim et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery of PDK1 Kinase Inhibitors with a Novel Mechanism of Action by Ultrahigh Throughput Screening

(2010) Ekaterina V. Bobkova et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

LL5β Directs the Translocation of Filamin A and SHIP2 to Sites of Phosphatidylinositol 3,4,5-Triphosphate (PtdIns(3,4,5)P3) Accumulation, and PtdIns(3,4,5)P3Localization Is Mutually Modified by Co-recruited SHIP2

(2010) Tetsuji Takabayashi et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Mammalian Target of Rapamycin (mTOR): Conducting the Cellular Signaling Symphony

(2010) Kathryn G. Foster et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

PtdIns(3,4,5)P3 is a regulator of myosin-X localization and filopodia formation

(2010) L. Plantard et al.   JOURNAL OF CELL SCIENCE

Discovery of 1-(4-(4-Propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a Highly Potent, Selective Mammalian Target of Rapamycin (mTOR) Inhibitor for the Treatment of Cancer

(2010) Qingsong Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Bis(morpholino-1,3,5-triazine) Derivatives: Potent Adenosine 5′-Triphosphate Competitive Phosphatidylinositol-3-kinase/Mammalian Target of Rapamycin Inhibitors: Discovery of Compound26(PKI-587), a Highly Efficacious Dual Inhibitor

(2010) Aranapakam M. Venkatesan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Molecular Pharmacology and Antitumor Activity of PHT-427, a Novel Akt/Phosphatidylinositide-Dependent Protein Kinase 1 Pleckstrin Homology Domain Inhibitor

(2010) E. J. Meuillet et al.   MOLECULAR CANCER THERAPEUTICS

MK-2206, an Allosteric Akt Inhibitor, Enhances Antitumor Efficacy by Standard Chemotherapeutic Agents or Molecular Targeted Drugs In vitro and In vivo

(2010) H. Hirai et al.   MOLECULAR CANCER THERAPEUTICS

The Actin-Bundling Protein Palladin Is an Akt1-Specific Substrate that Regulates Breast Cancer Cell Migration

(2010) Y. Rebecca Chin et al.   MOLECULAR CELL

Translation of the phosphoinositide code by PI effectors

(2010) Tatiana G Kutateladze   Nature Chemical Biology

The emerging mechanisms of isoform-specific PI3K signalling

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

Crystal Structure of Human AKT1 with an Allosteric Inhibitor Reveals a New Mode of Kinase Inhibition

(2010) Wen-I Wu et al.   PLoS One

Small molecule inhibition of phosphatidylinositol-3,4,5-triphosphate (PIP3) binding to pleckstrin homology domains

(2010) B. Miao 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

Discovery of the highly potent PI3K/mTOR dual inhibitor PF-04691502 through structure based drug design

(2010) Hengmiao Cheng et al.   MedChemComm

Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin

(2010) Steven D. Knight et al.   ACS Medicinal Chemistry Letters

Development of Phosphoinositide-3 Kinase Pathway Inhibitors for Advanced Cancer

(2010) James M. Cleary et al.   Current Oncology Reports

AKT-Independent Signaling Downstream of Oncogenic PIK3CA Mutations in Human Cancer

(2009) Krishna M. Vasudevan et al.   CANCER CELL

In vitro and In vivo Activity of Novel Small-Molecule Inhibitors Targeting the Pleckstrin Homology Domain of Protein Kinase B/AKT

(2009) S. A. Moses 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

Cardiac regulation by phosphoinositide 3-kinases and PTEN

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

Mdm2-mediated ubiquitylation: p53 and beyond

(2009) J-C Marine et al.   CELL DEATH AND DIFFERENTIATION

Identification of Allosteric PIF-Pocket Ligands for PDK1 using NMR-Based Fragment Screening and1H-15N TROSY Experiments

(2009) Brian J. Stockman et al.   Chemical Biology & Drug Design

Current Perspectives on Akt Akt-ivation and Akt-ions

(2009) Ronald W. Matheny et al.   EXPERIMENTAL BIOLOGY AND MEDICINE

An ATP-competitive Mammalian Target of Rapamycin Inhibitor Reveals Rapamycin-resistant Functions of mTORC1

(2009) Carson C. Thoreen et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Phase I Trial of Oral Irinotecan and Temozolomide for Children With Relapsed High-Risk Neuroblastoma: A New Approach to Neuroblastoma Therapy Consortium Study

(2009) Lars M. Wagner et al.   JOURNAL OF CLINICAL ONCOLOGY

Targeting the phosphoinositide 3-kinase pathway in cancer

(2009) Pixu Liu et al.   NATURE REVIEWS DRUG DISCOVERY

A frequent kinase domain mutation that changes the interaction between PI3K  and the membrane

(2009) D. Mandelker et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

MicroRNAs Differentially Regulated by Akt Isoforms Control EMT and Stem Cell Renewal in Cancer Cells

(2009) D. Iliopoulos et al.   Science Signaling

Perifosine: Update on a novel Akt inhibitor

(2009) Joell J. Gills et al.   Current Oncology Reports

Active-Site Inhibitors of mTOR Target Rapamycin-Resistant Outputs of mTORC1 and mTORC2

(2009) Morris E Feldman et al.   PLOS BIOLOGY

A Vascular Targeted Pan Phosphoinositide 3-Kinase Inhibitor Prodrug, SF1126, with Antitumor and Antiangiogenic Activity

(2008) J. R. Garlich et al.   CANCER RESEARCH

NVP-BEZ235, a Dual PI3K/mTOR Inhibitor, Prevents PI3K Signaling and Inhibits the Growth of Cancer Cells with Activating PI3K Mutations

(2008) V. Serra et al.   CANCER RESEARCH

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

(2008) N. Rhodes et al.   CANCER RESEARCH

Phosphatidylinositol 3-Kinase Hyperactivation Results in Lapatinib Resistance that Is Reversed by the mTOR/Phosphatidylinositol 3-Kinase Inhibitor NVP-BEZ235

(2008) P. J.A. Eichhorn et al.   CANCER RESEARCH

Small-Molecule Inhibitors of PDK1

(2008) Christian Peifer et al.   ChemMedChem

218 POSTER A phase I dose-escalation study of the safety, pharmacokinetics and pharmacodynamics of XL147, a novel PI3K inhibitor administered orally to patients with advanced solid tumors

(2008) E. Calvo et al.   EJC SUPPLEMENTS

Differential Modulation of Akt/Glycogen Synthase Kinase-3β Pathway Regulates Apoptotic and Cytoprotective Signaling Responses

(2008) Venugopalan D. Nair et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The regulation of cell motility and chemotaxis by phospholipid signaling

(2008) V. Kolsch et al.   JOURNAL OF CELL SCIENCE

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†

(2008) Adrian J. Folkes et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a novel class of AKT pleckstrin homology domain inhibitors

(2008) D. Mahadevan et al.   MOLECULAR CANCER THERAPEUTICS

Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity

(2008) S.-M. Maira et al.   MOLECULAR CANCER THERAPEUTICS

Comprehensive Identification of PIP3-Regulated PH Domains from C. elegans to H. sapiens by Model Prediction and Live Imaging

(2008) Wei Sun Park et al.   MOLECULAR CELL

Dual role of proapoptotic BAD in insulin secretion and beta cell survival

(2008) Nika N Danial et al.   NATURE MEDICINE

Drug discovery approaches targeting the PI3K/Akt pathway in cancer

(2008) C Garcia-Echeverria et al.   ONCOGENE

Taming the PI3K team to hold inflammation and cancer at bay

(2008) Emilio Hirsch et al.   PHARMACOLOGY & THERAPEUTICS

PHLiPPing the switch on Akt and protein kinase C signaling

(2008) John Brognard et al.   TRENDS IN ENDOCRINOLOGY AND METABOLISM

Targeting phosphoinositide 3-kinase—Moving towards therapy

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