RSK3/4 mediate resistance to PI3K pathway inhibitors in breast cancer

Clinical combination of the MEK inhibitor GDC-0973 and the PI3K inhibitor GDC-0941: A first-in-human phase Ib study testing daily and intermittent dosing schedules in patients with advanced solid tumors.

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

Targeting RSK: An Overview of Small Molecule Inhibitors

(2012) Tam Nguyen   Anti-Cancer Agents in Medicinal Chemistry

Abstract CT-01: BYL719, a next generation PI3K alpha specific inhibitor: Preliminary safety, PK, and efficacy results from the first-in-human study

(2012) D. Juric et al.   CANCER RESEARCH

The Clinical Effect of the Dual-Targeting Strategy Involving PI3K/AKT/mTOR and RAS/MEK/ERK Pathways in Patients with Advanced Cancer

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

PI3K/AKT/mTOR Inhibitors in Patients With Breast and Gynecologic Malignancies HarboringPIK3CAMutations

(2012) Filip Janku et al.   JOURNAL OF CLINICAL ONCOLOGY

Molecular Profiling of Patients with Colorectal Cancer and Matched Targeted Therapy in Phase I Clinical Trials

(2012) R. Dienstmann et al.   MOLECULAR CANCER THERAPEUTICS

The Cancer Cell Line Encyclopedia enables predictive modelling of anticancer drug sensitivity

(2012) Jordi Barretina et al.   NATURE

β-catenin confers resistance to PI3K and AKT inhibitors and subverts FOXO3a to promote metastasis in colon cancer

(2012) Stephan P Tenbaum et al.   NATURE MEDICINE

KRASness and PIK3CAness in Patients with Advanced Colorectal Cancer: Outcome after Treatment with Early-Phase Trials with Targeted Pathway Inhibitors

(2012) Ignacio Garrido-Laguna et al.   PLoS One

PI3K Inhibition Impairs BRCA1/2 Expression and Sensitizes BRCA-Proficient Triple-Negative Breast Cancer to PARP Inhibition

(2012) Yasir H. Ibrahim et al.   Cancer Discovery

Regulation and function of the RSK family of protein kinases

(2011) Yves Romeo et al.   BIOCHEMICAL JOURNAL

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

(2011) Sarat Chandarlapaty et al.   CANCER CELL

RSK4 inhibition results in bypass of stress-induced and oncogene-induced senescence

(2011) L. Lopez-Vicente et al.   CARCINOGENESIS

PRKX, TTBK2 and RSK4 expression causes sunitinib resistance in kidney carcinoma- and melanoma-cell lines

(2011) Claus Bender et al.   INTERNATIONAL JOURNAL OF CANCER

Phase I, Dose-Escalation Study of BKM120, an Oral Pan-Class I PI3K Inhibitor, in Patients With Advanced Solid Tumors

(2011) Johanna C. Bendell et al.   JOURNAL OF CLINICAL ONCOLOGY

Targeting cap-dependent translation blocks converging survival signals by AKT and PIM kinases in lymphoma

(2011) Jonathan H. Schatz et al.   JOURNAL OF EXPERIMENTAL MEDICINE

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

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

PIK3CA Mutations in Patients with Advanced Cancers Treated with PI3K/AKT/mTOR Axis Inhibitors

(2011) F. Janku et al.   MOLECULAR CANCER THERAPEUTICS

A chemical-genetic screen reveals a mechanism of resistance to PI3K inhibitors in cancer

(2011) Markus K Muellner et al.   Nature Chemical Biology

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

(2011) Pixu Liu et al.   NATURE MEDICINE

A public genome-scale lentiviral expression library of human ORFs

(2011) Xiaoping Yang et al.   NATURE METHODS

Towards systematic functional characterization of cancer genomes

(2011) Jesse S. Boehm et al.   NATURE REVIEWS GENETICS

Everolimus for Advanced Pancreatic Neuroendocrine Tumors

(2011) James C. Yao et al.   NEW ENGLAND JOURNAL OF MEDICINE

Everolimus in Postmenopausal Hormone-Receptor–Positive Advanced Breast Cancer

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

PIK3CA mutation, but not PTEN loss of function, determines the sensitivity of breast cancer cells to mTOR inhibitory drugs

(2011) B Weigelt et al.   ONCOGENE

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

(2011) V Serra et al.   ONCOGENE

PI3K-targeted therapy can be evaded by gene amplification along the MYC-eukaryotic translation initiation factor 4E (eIF4E) axis

(2011) N. Ilic et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

A genome-wide RNAi screen identifies multiple RSK-dependent regulators of cell migration

(2010) G. A. Smolen et al.   GENES & DEVELOPMENT

Deregulation of the PI3K and KRAS signaling pathways in human cancer cells determines their response to everolimus

(2010) Federica Di Nicolantonio et al.   JOURNAL OF CLINICAL INVESTIGATION

RSK-Mediated Phosphorylation in the C/EBPβ Leucine Zipper Regulates DNA Binding, Dimerization, and Growth Arrest Activity

(2010) Sook Lee et al.   MOLECULAR AND CELLULAR BIOLOGY

Regulation of the mTOR Complex 1 Pathway by Nutrients, Growth Factors, and Stress

(2010) Shomit Sengupta et al.   MOLECULAR CELL

COT drives resistance to RAF inhibition through MAP kinase pathway reactivation

(2010) Cory M. Johannessen et al.   NATURE

Towards a knowledge-based Human Protein Atlas

(2010) Mathias Uhlen et al.   NATURE BIOTECHNOLOGY

Development of a mouse model for sporadic and metastatic colon tumors and its use in assessing drug treatment

(2010) K. E. Hung et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A Technical Assessment of the Utility of Reverse Phase Protein Arrays for the Study of the Functional Proteome in Non-microdissected Human Breast Cancers

(2010) Bryan T. Hennessy et al.   Clinical Proteomics

Regulation of Replicative and Stress-Induced Senescence by RSK4, which is Down-regulated in Human Tumors

(2009) L. Lopez-Vicente et al.   CLINICAL CANCER RESEARCH

In vivo Antitumor Activity of MEK and Phosphatidylinositol 3-Kinase Inhibitors in Basal-Like Breast Cancer Models

(2009) K. P. Hoeflich et al.   CLINICAL CANCER RESEARCH

PI3K and mTOR inhibitors—a new generation of targeted anticancer agents

(2009) Saskia Brachmann et al.   CURRENT OPINION IN CELL BIOLOGY

Targeting the PI3K signaling pathway in cancer

(2009) Kwok-Kin Wong et al.   CURRENT OPINION IN GENETICS & DEVELOPMENT

Targeting the phosphoinositide 3-kinase pathway in cancer

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

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

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

(2009) Morris E Feldman et al.   PLOS BIOLOGY

NVP-BEZ235, a Dual PI3K/mTOR Inhibitor, Prevents PI3K Signaling and Inhibits the Growth of Cancer Cells with Activating PI3K Mutations

(2008) V. Serra et al.   CANCER RESEARCH

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

Anti-invasive and Antimetastatic Activities of Ribosomal Protein S6 Kinase 4 in Breast Cancer Cells

(2008) A. Thakur et al.   CLINICAL CANCER RESEARCH

Efficacy of everolimus in advanced renal cell carcinoma: a double-blind, randomised, placebo-controlled phase III trial

(2008) Robert J Motzer et al.   LANCET

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

The RSK family of kinases: emerging roles in cellular signalling

(2008) Rana Anjum et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY