Genetically engineered mouse models of PI3K signaling in breast cancer

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

Mutation profiling identifies numerous rare drug targets and distinct mutation patterns in different clinical subtypes of breast cancers

(2012) Libero Santarpia et al.   BREAST CANCER RESEARCH AND TREATMENT

Increased signalling of EGFR and IGF1R and deregulation of PTEN/PI3K/Akt pathway are related with trastuzumab resistance in HER2 breast carcinomas

(2012) A Gallardo et al.   BRITISH JOURNAL OF CANCER

Inhibition of PI3K/mTOR Leads to Adaptive Resistance in Matrix-Attached Cancer Cells

(2012) Taru Muranen et al.   CANCER CELL

Life in the Fast Lane: Mammalian Disease Models in the Genomics Era

(2012) Lukas E. Dow et al.   CELL

Combined PI3K/mTOR and MEK Inhibition Provides Broad Antitumor Activity in Faithful Murine Cancer Models

(2012) P. J. Roberts et al.   CLINICAL CANCER RESEARCH

Phosphatidylinositol 3-kinase/AKT/mammalian target of rapamycin pathway inhibition

(2012) Dimitrios Zardavas et al.   CURRENT OPINION IN ONCOLOGY

The p110  and p110  isoforms of PI3K play divergent roles in mammary gland development and tumorigenesis

(2012) T. Utermark et al.   GENES & DEVELOPMENT

Randomized Phase II Trial of Everolimus in Combination With Tamoxifen in Patients With Hormone Receptor–Positive, Human Epidermal Growth Factor Receptor 2–Negative Metastatic Breast Cancer With Prior Exposure to Aromatase Inhibitors: A GINECO Study

(2012) Thomas Bachelot et al.   JOURNAL OF CLINICAL ONCOLOGY

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

Preclinical Pharmacology of AZD5363, an Inhibitor of AKT: Pharmacodynamics, Antitumor Activity, and Correlation of Monotherapy Activity with Genetic Background

(2012) B. R. Davies et al.   MOLECULAR CANCER THERAPEUTICS

The landscape of cancer genes and mutational processes in breast cancer

(2012) Philip J. Stephens et al.   NATURE

The clonal and mutational evolution spectrum of primary triple-negative breast cancers

(2012) Sohrab P. Shah et al.   NATURE

Whole-genome analysis informs breast cancer response to aromatase inhibition

(2012) Matthew J. Ellis et al.   NATURE

A murine lung cancer co-clinical trial identifies genetic modifiers of therapeutic response

(2012) Zhao Chen et al.   NATURE

Comprehensive molecular portraits of human breast tumours

(2012) Daniel C. Koboldt et al.   NATURE

Expression of tumour-specific antigens underlies cancer immunoediting

(2012) Michel DuPage et al.   NATURE

Chemotherapy response of spontaneous mammary tumors is independent of the adaptive immune system

(2012) Metamia Ciampricotti et al.   NATURE MEDICINE

Can predictive biomarkers in breast cancer guide adjuvant endocrine therapy?

(2012) Karin Beelen et al.   Nature Reviews Clinical Oncology

Patient-derived tumour xenografts as models for oncology drug development

(2012) John J. Tentler et al.   Nature Reviews Clinical Oncology

The functions and regulation of the PTEN tumour suppressor

(2012) Min Sup Song et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Conditional activation of Pik3ca H1047R in a knock-in mouse model promotes mammary tumorigenesis and emergence of mutations

(2012) W Yuan et al.   ONCOGENE

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

Antitumor effect of the mTOR inhibitor everolimus in combination with trastuzumab on human breast cancer stem cells in vitro and in vivo

(2012) Yuanxi Zhu et al.   TUMOR BIOLOGY

The mTORC1 Inhibitor Everolimus Prevents and Treats Eμ- Myc Lymphoma by Restoring Oncogene-Induced Senescence

(2012) Meaghan Wall 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

Evolutionary Pathways in BRCA1-Associated Breast Tumors

(2012) Filipe C. Martins et al.   Cancer Discovery

The favorable impact of PIK3CA mutations on survival: an analysis of 2587 patients with breast cancer

(2012) Amaury G. Dumont et al.   Chinese Journal of Cancer

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

Rapid validation of cancer genes in chimeras derived from established genetically engineered mouse models

(2011) Ivo J. Huijbers et al.   BIOESSAYS

Mutational characterization of individual breast tumors: TP53 and PI3K pathway genes are frequently and distinctively mutated in different subtypes

(2011) Sandrine Boyault et al.   BREAST CANCER RESEARCH AND TREATMENT

Evaluation of the association of PIK3CA mutations and PTEN loss with efficacy of trastuzumab therapy in metastatic breast cancer

(2011) E. Razis et al.   BREAST CANCER RESEARCH AND TREATMENT

Poly(ADP-Ribose) polymerase (PARP) inhibitors: Exploiting a synthetic lethal strategy in the clinic

(2011) Timothy A. Yap et al.   CA-A CANCER JOURNAL FOR CLINICIANS

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

(2011) Sarat Chandarlapaty et al.   CANCER CELL

c-Raf, but Not B-Raf, Is Essential for Development of K-Ras Oncogene-Driven Non-Small Cell Lung Carcinoma

(2011) Rafael B. Blasco et al.   CANCER CELL

Cooperation between Pik3ca and p53 Mutations in Mouse Mammary Tumor Formation

(2011) J. R. Adams et al.   CANCER RESEARCH

Luminal Expression of PIK3CA Mutant H1047R in the Mammary Gland Induces Heterogeneous Tumors

(2011) D. S. Meyer et al.   CANCER RESEARCH

Nuclear PTEN Regulates the APC-CDH1 Tumor-Suppressive Complex in a Phosphatase-Independent Manner

(2011) Min Sup Song et al.   CELL

A Rapid and Scalable System for Studying Gene Function in Mice Using Conditional RNA Interference

(2011) Prem K. Premsrirut et al.   CELL

Phase I/II Study of Trastuzumab in Combination With Everolimus (RAD001) in Patients With HER2-Overexpressing Metastatic Breast Cancer Who Progressed on Trastuzumab-Based Therapy

(2011) Phuong K. Morrow et al.   JOURNAL OF CLINICAL ONCOLOGY

Discovery of a Potent, Selective, and Orally Available Class I Phosphatidylinositol 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Kinase Inhibitor (GDC-0980) for the Treatment of Cancer

(2011) Daniel P. Sutherlin et al.   JOURNAL OF MEDICINAL CHEMISTRY

GDC-0980 Is a Novel Class I PI3K/mTOR Kinase Inhibitor with Robust Activity in Cancer Models Driven by the PI3K Pathway

(2011) J. J. Wallin et al.   MOLECULAR CANCER THERAPEUTICS

Identification and Characterization of NVP-BKM120, an Orally Available Pan-Class I PI3-Kinase Inhibitor

(2011) S.-M. Maira et al.   MOLECULAR CANCER THERAPEUTICS

PI3K Pathway Mutations and PTEN Levels in Primary and Metastatic Breast Cancer

(2011) A. M. Gonzalez-Angulo et al.   MOLECULAR CANCER THERAPEUTICS

A continuum model for tumour suppression

(2011) Alice H. Berger et al.   NATURE

Insertional mutagenesis identifies multiple networks of cooperating genes driving intestinal tumorigenesis

(2011) H Nikki March et al.   NATURE GENETICS

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

(2011) Pixu Liu et al.   NATURE MEDICINE

Tumor grafts derived from women with breast cancer authentically reflect tumor pathology, growth, metastasis and disease outcomes

(2011) Yoko S DeRose et al.   NATURE MEDICINE

Everolimus in Postmenopausal Hormone-Receptor–Positive Advanced Breast Cancer

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

The Dual PI3K/mTOR Inhibitor NVP-BEZ235 Induces Tumor Regression in a Genetically Engineered Mouse Model of PIK3CA Wild-Type Colorectal Cancer

(2011) Jatin Roper et al.   PLoS One

Akt1 Is Essential for Postnatal Mammary Gland Development, Function, and the Expression of Btn1a1

(2011) Jessica LaRocca et al.   PLoS One

Feedback upregulation of HER3 (ErbB3) expression and activity attenuates antitumor effect of PI3K inhibitors

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

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

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

Leukocyte Complexity Predicts Breast Cancer Survival and Functionally Regulates Response to Chemotherapy

(2011) David G. DeNardo et al.   Cancer Discovery

PTEN, PIK3CA, p-AKT, and p-p70S6K Status

(2010) Francisco J. Esteva et al.   AMERICAN JOURNAL OF PATHOLOGY

Phase I trial of oral mTOR inhibitor everolimus in combination with trastuzumab and vinorelbine in pre-treated patients with HER2-overexpressing metastatic breast cancer

(2010) Guy Jerusalem et al.   BREAST CANCER RESEARCH AND TREATMENT

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

Hot-spot mutations in p110α of phosphatidylinositol 3-kinase (PI3K): Differential interactions with the regulatory subunit p85 and with RAS

(2010) Li Zhao et al.   CELL CYCLE

PIK3CA Mutations May Be Discordant between Primary and Corresponding Metastatic Disease in Breast Cancer

(2010) J. Dupont Jensen et al.   CLINICAL CANCER RESEARCH

Estimates of worldwide burden of cancer in 2008: GLOBOCAN 2008

(2010) Jacques Ferlay et al.   INTERNATIONAL JOURNAL OF CANCER

Phase I Study of Everolimus Plus Weekly Paclitaxel and Trastuzumab in Patients With Metastatic Breast Cancer Pretreated With Trastuzumab

(2010) Fabrice Andre et al.   JOURNAL OF CLINICAL ONCOLOGY

Survival Benefit With Proapoptotic Molecular and Pathologic Responses From Dual Targeting of Mammalian Target of Rapamycin and Epidermal Growth Factor Receptor in a Preclinical Model of Pancreatic Neuroendocrine Carcinogenesis

(2010) Christopher W. Chiu et al.   JOURNAL OF CLINICAL ONCOLOGY

The PI3K Pathway As Drug Target in Human Cancer

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

Association of sporadic breast cancer with PTEN/MMAC1/TEP1 promoter hypermethylation

(2010) Vallian Sadeq et al.   MEDICAL ONCOLOGY

Activated Phosphoinositide 3-Kinase/AKT Signaling Confers Resistance to Trastuzumab but not Lapatinib

(2010) N. A. O'Brien 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

Assessing therapeutic responses in Kras mutant cancers using genetically engineered mouse models

(2010) Mallika Singh et al.   NATURE BIOTECHNOLOGY

Subtle variations in Pten dose determine cancer susceptibility

(2010) Andrea Alimonti et al.   NATURE GENETICS

The emerging mechanisms of isoform-specific PI3K signalling

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

Inositol polyphosphate 4-phosphatase II regulates PI3K/Akt signaling and is lost in human basal-like breast cancers

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

PIK3CA mutations associated with gene signature of low mTORC1 signaling and better outcomes in estrogen receptor-positive breast cancer

(2010) S. Loi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

PiggyBac Transposon Mutagenesis: A Tool for Cancer Gene Discovery in Mice

(2010) R. Rad et al.   SCIENCE

Ku-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR)

(2009) Juan M. García-Martínez et al.   BIOCHEMICAL JOURNAL

Phosphatidylinositol-3-kinase and AKT1 mutations occur early in breast carcinoma

(2009) Jennifer Dunlap et al.   BREAST CANCER RESEARCH AND TREATMENT

Evidence that Inositol Polyphosphate 4-Phosphatase Type II Is a Tumor Suppressor that Inhibits PI3K Signaling

(2009) Christina Gewinner et al.   CANCER CELL

Akt1 and Akt2 Play Distinct Roles in the Initiation and Metastatic Phases of Mammary Tumor Progression

(2009) R. L. Dillon et al.   CANCER RESEARCH

Differential Enhancement of Breast Cancer Cell Motility and Metastasis by Helical and Kinase Domain Mutations of Class IA Phosphoinositide 3-Kinase

(2009) H. Pang 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

Biochemical, Cellular, and In vivo Activity of Novel ATP-Competitive and Selective Inhibitors of the Mammalian Target of Rapamycin

(2009) K. Yu et al.   CANCER RESEARCH

Synthetic lethal targeting ofPTENmutant cells with PARP inhibitors

(2009) Ana M. Mendes-Pereira et al.   EMBO Molecular Medicine

PTEN Deficiency in a Luminal ErbB-2 Mouse Model Results in Dramatic Acceleration of Mammary Tumorigenesis and Metastasis

(2009) Babette Schade et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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 II Randomized Study of Neoadjuvant Everolimus Plus Letrozole Compared With Placebo Plus Letrozole in Patients With Estrogen Receptor–Positive Breast Cancer

(2009) José Baselga et al.   JOURNAL OF CLINICAL ONCOLOGY

Response and resistance to MEK inhibition in leukaemias initiated by hyperactive Ras

(2009) Jennifer O. Lauchle et al.   NATURE

A conditional transposon-based insertional mutagenesis screen for genes associated with mouse hepatocellular carcinoma

(2009) Vincent W Keng et al.   NATURE BIOTECHNOLOGY

Phosphorylation by Akt1 promotes cytoplasmic localization of Skp2 and impairs APCCdh1-mediated Skp2 destruction

(2009) Daming Gao et al.   NATURE CELL BIOLOGY

A high-throughput splinkerette-PCR method for the isolation and sequencing of retroviral insertion sites

(2009) Anthony G Uren et al.   Nature Protocols

Differential induction of apoptosis in HER2 and EGFR addicted cancers following PI3K inhibition

(2009) A. C. Faber et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

(2009) Morris E Feldman et al.   PLOS BIOLOGY

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

An Integrative Genomic and Proteomic Analysis of PIK3CA, PTEN, and AKT Mutations in Breast Cancer

(2008) K. Stemke-Hale et al.   CANCER RESEARCH

Distinct roles of the three Akt isoforms in lactogenic differentiation and involution

(2008) Ioanna G. Maroulakou et al.   JOURNAL OF CELLULAR PHYSIOLOGY

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

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

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

PTEN-deficient cancers depend on PIK3CB

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