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

A phase I dose-escalation study of XL147 (SAR245408), a PI3K inhibitor administered orally to patients (pts) with advanced malignancies.

(2017) G. Edelman et al.   JOURNAL OF CLINICAL ONCOLOGY

Targeting mTOR globally in cancer: Thinking beyond rapamycin

(2011) Boris Shor et al.   CELL CYCLE

The PI3K Pathway As Drug Target in Human Cancer

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

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

(2010) A Chakrabarty et al.   ONCOGENE

Resiliency and Vulnerability in the HER2-HER3 Tumorigenic Driver

(2010) D. N. Amin et al.   Science Translational Medicine

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

Clinical Activity of Gemcitabine Plus Pertuzumab in Platinum-Resistant Ovarian Cancer, Fallopian Tube Cancer, or Primary Peritoneal Cancer

(2009) Sharmila Makhija et al.   JOURNAL OF CLINICAL ONCOLOGY

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

A Central Role for HER3 in HER2-Amplified Breast Cancer: Implications for Targeted Therapy

(2008) S. T. Lee-Hoeflich et al.   CANCER RESEARCH

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

Transforming Growth Factor   Engages TACE and ErbB3 To Activate Phosphatidylinositol-3 Kinase/Akt in ErbB2-Overexpressing Breast Cancer and Desensitizes Cells to Trastuzumab

(2008) S. E. Wang et al.   MOLECULAR AND CELLULAR BIOLOGY

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

The role of PTEN signaling perturbations in cancer and in targeted therapy

(2008) M Keniry et al.   ONCOGENE

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

(2008) A Carracedo et al.   ONCOGENE