Targeting the PI3K pathway for cancer therapy

A phase I study of CAL-101, an isoform-selective inhibitor of phosphatidylinositol 3‐kinase P110δ, in combination with anti-CD20 monoclonal antibody therapy and/or bendamustine in patients with previously treated B-cell malignancies.

(2017) I. W. Flinn et al.   JOURNAL OF CLINICAL ONCOLOGY

Oral PI3 kinase inhibitor BKM120 monotherapy in patients (pts) with advanced solid tumors: An update on safety and efficacy.

(2017) B. Grana et al.   JOURNAL OF CLINICAL ONCOLOGY

A dose-escalation study with the novel formulation of the oral pan-class I PI3K inhibitor BEZ235, solid dispersion system (SDS) sachet, in patients with advanced solid tumors.

(2017) J. D. Peyton et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase I study of CAL-101, an isoform-selective inhibitor of phosphatidylinositol 3‐kinase P110d, in patients with previously treated chronic lymphocytic leukemia.

(2017) S. E. Coutre et al.   JOURNAL OF CLINICAL ONCOLOGY

Results of the phase III, placebo-controlled trial (SUCCEED) evaluating the mTOR inhibitor ridaforolimus (R) as maintenance therapy in advanced sarcoma patients (pts) following clinical benefit from prior standard cytotoxic chemotherapy (CT).

(2017) S. P. Chawla et al.   JOURNAL OF CLINICAL ONCOLOGY

INPP4B: the New Kid on the PI3K Block

(2015) Irina U. Agoulnik et al.   Oncotarget

Crosstalk between NOTCH and AKT signaling during murine megakaryocyte lineage specification

(2011) M. G. Cornejo et al.   BLOOD

PIK3R1 (p85 ) Is Somatically Mutated at High Frequency in Primary Endometrial Cancer

(2011) M. E. Urick et al.   CANCER RESEARCH

mTORC1 and mTORC2 Regulate EMT, Motility, and Metastasis of Colorectal Cancer via RhoA and Rac1 Signaling Pathways

(2011) P. Gulhati et al.   CANCER RESEARCH

A Unique Spectrum of Somatic PIK3CA (p110α) Mutations Within Primary Endometrial Carcinomas

(2011) Meghan L. Rudd et al.   CLINICAL CANCER RESEARCH

Ridaforolimus: a promising drug in the treatment of soft-tissue sarcoma and other malignancies

(2011) Janet E Dancey et al.   Future Oncology

Phosphoinositide-3-Kinase Catalytic Alpha and KRAS Mutations are Important Predictors of Resistance to Therapy with Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Patients with Advanced Non-small Cell Lung Cancer

(2011) Vienna Ludovini et al.   Journal of Thoracic Oncology

Disruption of the AKT pathway inhibits metastasis in an orthotopic model of head and neck squamous cell carcinoma

(2011) Joseph A. Knowles et al.   LARYNGOSCOPE

PIK3CA kinase domain mutation identifies a subgroup of stage III colon cancer patients with poor prognosis

(2011) Arantza Fariña Sarasqueta et al.   CELLULAR ONCOLOGY

PIK3CA amplification associates with resistance to chemotherapy in ovarian cancer patients

(2010) Iwona K. Kolasa et al.   CANCER BIOLOGY & THERAPY

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

Phase I Trial of the Irreversible EGFR and HER2 Kinase Inhibitor BIBW 2992 in Patients With Advanced Solid Tumors

(2010) Timothy A. Yap 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

PI3K/PTEN/AKT/mTOR pathway genetic variation predicts toxicity and distant progression in lung cancer patients receiving platinum-based chemotherapy

(2010) Xia Pu et al.   LUNG CANCER

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

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

The Sex-Determining Region Y-Box 4 and Homeobox C6 Transcriptional Networks in Prostate Cancer Progression

(2009) Carlos S. Moreno   AMERICAN JOURNAL OF PATHOLOGY

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

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

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

(2009) Christina Gewinner et al.   CANCER CELL

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

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

PTEN Loss Contributes to Erlotinib Resistance in EGFR-Mutant Lung Cancer by Activation of Akt and EGFR

(2009) M. L. Sos et al.   CANCER RESEARCH

Involvement of PI3K/PTEN/AKT/mTOR pathway in invasion and metastasis in hepatocellular carcinoma: Association with MMP-9

(2009) Jing-song Chen et al.   HEPATOLOGY RESEARCH

Dysregulated PI3K/Akt/PTEN pathway is a marker of a short disease-free survival in node-negative breast carcinoma

(2009) Alessandra Capodanno et al.   HUMAN PATHOLOGY

Coordination of membrane events during autophagy by multiple class III PI3-kinase complexes

(2009) Anne Simonsen et al.   JOURNAL OF CELL BIOLOGY

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

Methylation of PTEN as a Prognostic Factor in Malignant Melanoma of the Skin

(2009) Christoph Lahtz et al.   JOURNAL OF INVESTIGATIVE DERMATOLOGY

The PI3-K/AKT-Pathway and Radiation Resistance Mechanisms in Non-small Cell Lung Cancer

(2009) Olga C.J. Schuurbiers et al.   Journal of Thoracic Oncology

Oncogenic Ras Signals through Activation of Both Phosphoinositide 3-Kinase and Rac1 to Induce c-Jun NH2-Terminal Kinase-Mediated, Caspase-Independent Cell Death

(2009) J.-Y. Byun et al.   MOLECULAR CANCER RESEARCH

Essential function for the GTPase TC21 in homeostatic antigen receptor signaling

(2009) Pilar Delgado et al.   NATURE IMMUNOLOGY

Ras is an indispensable coregulator of the class IB phosphoinositide 3-kinase p87/p110 

(2009) B. Kurig et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Integrated genomic profiling of endometrial carcinoma associates aggressive tumors with indicators of PI3 kinase activation

(2009) H. B. Salvesen et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Regulation of phosphoinositide 3-kinase expression in health and disease

(2009) Klaartje Kok et al.   TRENDS IN BIOCHEMICAL SCIENCES

The life of a cell: apoptosis regulation by the PI3K/PKB pathway

(2008) Vincent Duronio   BIOCHEMICAL JOURNAL

hVps15, but not Ca2+/CaM, is required for the activity and regulation of hVps34 in mammalian cells

(2008) Ying Yan et al.   BIOCHEMICAL JOURNAL

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

(2008) M S Kim 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

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

Phosphoinositide 3-Kinases p110  and p110  Regulate Cell Cycle Entry, Exhibiting Distinct Activation Kinetics in G1 Phase

(2008) M. Marques et al.   MOLECULAR AND CELLULAR BIOLOGY

Angiogenesis selectively requires the p110α isoform of PI3K to control endothelial cell migration

(2008) Mariona Graupera et al.   NATURE

Comprehensive genomic characterization defines human glioblastoma genes and core pathways

(2008) Roger McLendon et al.   NATURE

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

(2008) A Carracedo et al.   ONCOGENE

Class I PI3K in oncogenic cellular transformation

(2008) L Zhao 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