Targeting the PI3K/Akt/mTOR Pathway for Breast Cancer Therapy

Ras/Raf/MEK/ERK and PI3K/PTEN/Akt/mTOR Inhibitors: Rationale and Importance to Inhibiting These Pathways in Human Health

(2015) William H. Chappell et al.   Oncotarget

Phase I safety, pharmacokinetic, and pharmacodynamic study of the oral phosphatidylinositol-3-kinase and mTOR inhibitor BGT226 in patients with advanced solid tumors

(2012) B. Markman et al.   ANNALS OF ONCOLOGY

Synthesis and structure–activity relationships of imidazo[1,2-a]pyrimidin-5(1H)-ones as a novel series of beta isoform selective phosphatidylinositol 3-kinase inhibitors

(2012) Hong Lin et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

(2012) Anirudh Prahallad et al.   NATURE

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

PIK3CAmutations and EGFR overexpression predict for lithium sensitivity in human breast epithelial cells

(2011) Michaela J. Higgins et al.   CANCER BIOLOGY & THERAPY

Antitumor Efficacy of PKI-587, a Highly Potent Dual PI3K/mTOR Kinase Inhibitor

(2011) R. Mallon et al.   CLINICAL CANCER RESEARCH

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

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

CAL-101: a phosphatidylinositol-3-kinase p110-delta inhibitor for the treatment of lymphoid malignancies

(2011) Jorge J Castillo et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

mTOR inhibition in breast cancer: unraveling the complex mechanisms of mTOR signal transduction and its clinical implications in therapy

(2011) Ruth O'Regan et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

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

Loss of Human Epidermal Growth Factor Receptor 2 (HER2) Expression in Metastatic Sites of HER2-Overexpressing Primary Breast Tumors

(2011) Naoki Niikura et al.   JOURNAL OF CLINICAL ONCOLOGY

Prospective Study Evaluating the Impact of Tissue Confirmation of Metastatic Disease in Patients With Breast Cancer

(2011) Eitan Amir et al.   JOURNAL OF CLINICAL ONCOLOGY

Autophagy suppression promotes apoptotic cell death in response to inhibition of the PI3K—mTOR pathway in pancreatic adenocarcinoma

(2011) Olga K. Mirzoeva et al.   JOURNAL OF MOLECULAR MEDICINE-JMM

A Sensitized RNA Interference Screen Identifies a Novel Role for the PI3K p110  Isoform in Medulloblastoma Cell Proliferation and Chemoresistance

(2011) A. S. Guerreiro et al.   MOLECULAR CANCER RESEARCH

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

Rapamycin passes the torch: a new generation of mTOR inhibitors

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

Improved Survival with Vemurafenib in Melanoma with BRAF V600E Mutation

(2011) Paul B. Chapman et al.   NEW ENGLAND JOURNAL OF MEDICINE

PI3K inhibition results in enhanced HER signaling and acquired ERK dependency in HER2-overexpressing breast cancer

(2011) V Serra et al.   ONCOGENE

Targeting the Phosphatidylinositol 3-Kinase Signaling Pathway in Breast Cancer

(2011) L. F. Hernandez-Aya et al.   ONCOLOGIST

Targeting the Phosphoinositide-3 (PI3) Kinase Pathway in Breast Cancer

(2011) J. Baselga   ONCOLOGIST

Resistance of Akt kinases to dephosphorylation through ATP-dependent conformational plasticity

(2011) T. O. Chan et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

PIKing the Right Patient

(2010) A. B. Turke et al.   CLINICAL CANCER RESEARCH

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

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

Predictive Biomarkers of Sensitivity to the Phosphatidylinositol 3' Kinase Inhibitor GDC-0941 in Breast Cancer Preclinical Models

(2010) C. O'Brien et al.   CLINICAL CANCER RESEARCH

The PI3K Pathway As Drug Target in Human Cancer

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

Randomized Study of Lapatinib Alone or in Combination With Trastuzumab in Women With ErbB2-Positive, Trastuzumab-Refractory Metastatic Breast Cancer

(2010) Kimberly L. Blackwell et al.   JOURNAL OF CLINICAL ONCOLOGY

Loss of Phosphatase and Tensin Homolog or Phosphoinositol-3 Kinase Activation and Response to Trastuzumab or Lapatinib in Human Epidermal Growth Factor Receptor 2–Overexpressing Locally Advanced Breast Cancers

(2010) Bhuvanesh Dave et al.   JOURNAL OF CLINICAL ONCOLOGY

Antitumor Efficacy Profile of PKI-402, a Dual Phosphatidylinositol 3-Kinase/Mammalian Target of Rapamycin Inhibitor

(2010) Robert Mallon et al.   MOLECULAR CANCER THERAPEUTICS

A coding-independent function of gene and pseudogene mRNAs regulates tumour biology

(2010) Laura Poliseno et al.   NATURE

The emerging mechanisms of isoform-specific PI3K signalling

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

Knock in of the AKT1 E17K mutation in human breast epithelial cells does not recapitulate oncogenic PIK3CA mutations

(2010) J Lauring et al.   ONCOGENE

H1047R phosphatidylinositol 3-kinase mutant enhances HER2-mediated transformation by heregulin production and activation of HER3

(2010) A Chakrabarty et al.   ONCOGENE

Initial testing (stage 1) of the Akt inhibitor GSK690693 by the pediatric preclinical testing program

(2010) Hernan Carol et al.   PEDIATRIC BLOOD & CANCER

PIKing the right isoform: the emergent role of the p110β subunit in breast cancer

(2010) Silvia Carvalho et al.   VIRCHOWS ARCHIV

Prediction of adjuvant chemotherapy benefit in endocrine responsive, early breast cancer using multigene assays

(2009) Kathy S. Albain et al.   BREAST

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

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

In vitro evaluation of pan-PI3-kinase inhibitor SF1126 in trastuzumab-sensitive and trastuzumab-resistant HER2-over-expressing breast cancer cells

(2009) Tuba Ozbay et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

PIK3CA and PIK3CB Inhibition Produce Synthetic Lethality when Combined with Estrogen Deprivation in Estrogen Receptor-Positive Breast Cancer

(2009) R. J. Crowder et al.   CANCER RESEARCH

Synthetic lethal targeting ofPTENmutant cells with PARP inhibitors

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

Guidelines for Human Epidermal Growth Factor Receptor 2 Testing: Biologic and Methodologic Considerations

(2009) Guido Sauter et al.   JOURNAL OF CLINICAL ONCOLOGY

Inhibition of Poly(ADP-Ribose) Polymerase in Tumors fromBRCAMutation Carriers

(2009) Peter C. Fong et al.   NEW ENGLAND JOURNAL OF MEDICINE

Knockin of mutant PIK3CA activates multiple oncogenic pathways

(2009) John P. Gustin et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Specific apoptosis induction by the dual PI3K/mTor inhibitor NVP-BEZ235 in HER2 amplified and PIK3CA mutant breast cancer cells

(2009) Saskia M. Brachmann et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Inhibitors of the PI3K/Akt/mTOR Pathway: New Hope for Breast Cancer Patients

(2009) Sandra Ghayad et al.   Recent Patents on Anti-Cancer Drug Discovery

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

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

PIK3CA Cooperates with Other Phosphatidylinositol 3'-Kinase Pathway Mutations to Effect Oncogenic Transformation

(2008) K. Oda et al.   CANCER RESEARCH

The PIK3CA Gene as a Mutated Target for Cancer Therapy

(2008) John Gustin et al.   CURRENT CANCER DRUG TARGETS

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

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

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

(2008) J LOPICCOLO et al.   DRUG RESISTANCE UPDATES

Circulating mutant DNA to assess tumor dynamics

(2008) Frank Diehl et al.   NATURE MEDICINE

Drug discovery approaches targeting the PI3K/Akt pathway in cancer

(2008) C Garcia-Echeverria et al.   ONCOGENE

PI3K pathway alterations in cancer: variations on a theme

(2008) T L Yuan et al.   ONCOGENE

The p110  isoform of phosphoinositide 3-kinase signals downstream of G protein-coupled receptors and is functionally redundant with p110 

(2008) J. Guillermet-Guibert et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

PTEN-deficient cancers depend on PIK3CB

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