Targeting AKT1-E17K and the PI3K/AKT Pathway with an Allosteric AKT Inhibitor, ARQ 092

Ras/Raf/MEK/ERK and PI3K/PTEN/Akt/mTOR Cascade Inhibitors: How Mutations Can Result in Therapy Resistance and How to Overcome Resistance

(2015) James Andrew McCubrey et al.   Oncotarget

320 First-in-human study with ARQ 092, a novel pan AKT-inhibitor, in subjects with advanced solid tumors or recurrent malignant lymphoma

(2014) M. Saleh et al.   EUROPEAN JOURNAL OF CANCER

Discovery of Novel AKT Inhibitors with Enhanced Anti-Tumor Effects in Combination with the MEK Inhibitor

(2014) Melissa Dumble et al.   PLoS One

Rapid Induction of Apoptosis by PI3K Inhibitors Is Dependent upon Their Transient Inhibition of RAS-ERK Signaling

(2014) M. Will et al.   Cancer Discovery

AKT1E17K mutations cluster with meningothelial and transitional meningiomas and can be detected by SFRP1 immunohistochemistry

(2013) Felix Sahm et al.   ACTA NEUROPATHOLOGICA

Elevated SGK1 predicts resistance of breast cancer cells to Akt inhibitors

(2013) Eeva M. Sommer et al.   BIOCHEMICAL JOURNAL

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

PI3K Pathway Dependencies in Endometrioid Endometrial Cancer Cell Lines

(2013) B. Weigelt et al.   CLINICAL CANCER RESEARCH

PIK3CA and AKT1 Mutations Have Distinct Effects on Sensitivity to Targeted Pathway Inhibitors in an Isogenic Luminal Breast Cancer Model System

(2013) J. A. Beaver et al.   CLINICAL CANCER RESEARCH

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

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

PIK3CA Mutation H1047R Is Associated with Response to PI3K/AKT/mTOR Signaling Pathway Inhibitors in Early-Phase Clinical Trials

(2012) F. Janku et al.   CANCER RESEARCH

PIK3CA/PTEN Mutations and Akt Activation As Markers of Sensitivity to Allosteric mTOR Inhibitors

(2012) F. Meric-Bernstam et al.   CLINICAL CANCER RESEARCH

Biomarkers of Response to Akt Inhibitor MK-2206 in Breast Cancer

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

Frequent Mutational Activation of the PI3K-AKT Pathway in Trastuzumab-Resistant Breast Cancer

(2012) S. Chandarlapaty et al.   CLINICAL CANCER RESEARCH

Discovery and Optimization of a Series of 3-(3-Phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amines: Orally Bioavailable, Selective, and Potent ATP-Independent Akt Inhibitors

(2012) Mark A. Ashwell et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery and Preclinical Pharmacology of a Selective ATP-Competitive Akt Inhibitor (GDC-0068) for the Treatment of Human Tumors

(2012) James F. Blake et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2012) Jeong Ho Lee et al.   NATURE GENETICS

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

A Mosaic Activating Mutation inAKT1Associated with the Proteus Syndrome

(2011) Marjorie J. Lindhurst et al.   NEW ENGLAND JOURNAL OF MEDICINE

Genomic Complexity and AKT Dependence in Serous Ovarian Cancer

(2011) Aphrothiti J. Hanrahan et al.   Cancer Discovery

E17K substitution in AKT1 in prostate cancer

(2010) J L Boormans et al.   BRITISH JOURNAL OF CANCER

Activating E17K mutation in the gene encoding the protein kinase AKT in a subset of squamous cell carcinoma of the lung

(2010) Donatella Malanga et al.   CELL CYCLE

Rarity ofAKT1andAKT3E17K mutations in squamous cell carcinoma of lung

(2010) Hongdo Do et al.   CELL CYCLE

Akt inhibitors in clinical development for the treatment of cancer

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

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 oncogenic mutation in the pleckstrin homology domain of AKT1 in endometrial carcinomas

(2009) K Shoji et al.   BRITISH JOURNAL OF CANCER

Ligand-Independent HER2/HER3/PI3K Complex Is Disrupted by Trastuzumab and Is Effectively Inhibited by the PI3K Inhibitor GDC-0941

(2009) Teemu T. Junttila et al.   CANCER CELL

AKT1 E17 K pleckstrin homology domain mutation in urothelial carcinoma

(2009) Dorit E. Zilberman et al.   CANCER GENETICS AND CYTOGENETICS

PIK3CA Mutation Associates with Improved Outcome in Breast Cancer

(2009) K. Kalinsky et al.   CLINICAL CANCER RESEARCH

Targeting the phosphoinositide 3-kinase pathway in cancer

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

AKT1 mutations in bladder cancer: identification of a novel oncogenic mutation that can co-operate with E17K

(2009) J M Askham et al.   ONCOGENE

PTEN and the PI3-Kinase Pathway in Cancer

(2008) Nader Chalhoub et al.   Annual Review of Pathology-Mechanisms of Disease

Mutational analysis of oncogenic AKT E17K mutation in common solid cancers and acute leukaemias

(2008) M S Kim et al.   BRITISH JOURNAL OF CANCER

Resistance to chemotherapy: new treatments and novel insights into an old problem

(2008) S Raguz et al.   BRITISH JOURNAL OF CANCER

A novel AKT3 mutation in melanoma tumours and cell lines

(2008) M A Davies et al.   BRITISH JOURNAL OF CANCER

Inhibition of Activated Fibroblast Growth Factor Receptor 2 in Endometrial Cancer Cells Induces Cell Death Despite PTEN Abrogation

(2008) S. A. Byron et al.   CANCER RESEARCH

AKT1 E17K in human solid tumours

(2008) F E Bleeker et al.   ONCOGENE

PI3K pathway alterations in cancer: variations on a theme

(2008) T L Yuan et al.   ONCOGENE

Breast Tumor Cells with PI3K Mutation or HER2 Amplification Are Selectively Addicted to Akt Signaling

(2008) Qing-Bai She et al.   PLoS One