The dynamic nature of the kinome

The Plasticity of Oncogene Addiction: Implications for Targeted Therapies Directed to Receptor Tyrosine Kinases

(2015) Vinochani Pillay et al.   NEOPLASIA

Dynamic Reprogramming of the Kinome in Response to Targeted MEK Inhibition in Triple-Negative Breast Cancer

(2012) James S. Duncan et al.   CELL

mTOR Signaling in Growth Control and Disease

(2012) Mathieu Laplante et al.   CELL

Defining the expressed breast cancer kinome

(2012) Alicia A Midland et al.   CELL RESEARCH

Treatment options for chronic myeloid leukemia

(2012) Maria Florencia Tanaka et al.   EXPERT OPINION ON PHARMACOTHERAPY

Complexity in the signaling network: insights from the use of targeted inhibitors in cancer therapy

(2012) J. S. Logue et al.   GENES & DEVELOPMENT

Combinations of BRAF, MEK, and PI3K/mTOR Inhibitors Overcome Acquired Resistance to the BRAF Inhibitor GSK2118436 Dabrafenib, Mediated by NRAS or MEK Mutations

(2012) J. G. Greger et al.   MOLECULAR CANCER THERAPEUTICS

Widespread potential for growth-factor-driven resistance to anticancer kinase inhibitors

(2012) Timothy R. Wilson et al.   NATURE

From single cells to deep phenotypes in cancer

(2012) Sean C Bendall et al.   NATURE BIOTECHNOLOGY

Multiplexed mass cytometry profiling of cellular states perturbed by small-molecule regulators

(2012) Bernd Bodenmiller et al.   NATURE BIOTECHNOLOGY

Improved Survival with MEK Inhibition in BRAF-Mutated Melanoma

(2012) Keith T. Flaherty et al.   NEW ENGLAND JOURNAL OF MEDICINE

The Evolution of Protein Kinase Inhibitors from Antagonists to Agonists of Cellular Signaling

(2011) Arvin C. Dar et al.   Annual Review of Biochemistry

AMPK and mTOR in Cellular Energy Homeostasis and Drug Targets

(2011) Ken Inoki et al.   Annual Review of Pharmacology and Toxicology

Acquired resistance to drugs targeting receptor tyrosine kinases

(2011) Steven A. Rosenzweig   BIOCHEMICAL PHARMACOLOGY

The role of targeted chemical proteomics in pharmacology

(2011) Chris W Sutton   BRITISH JOURNAL OF PHARMACOLOGY

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

(2011) Sarat Chandarlapaty et al.   CANCER CELL

Mutant BRAF Melanomas—Dependence and Resistance

(2011) Poulikos I. Poulikakos et al.   CANCER CELL

Nilotinib and MEK Inhibitors Induce Synthetic Lethality through Paradoxical Activation of RAF in Drug-Resistant Chronic Myeloid Leukemia

(2011) Leisl M. Packer et al.   CANCER CELL

Tpl2 kinase signal transduction in inflammation and cancer

(2011) Maria Vougioukalaki et al.   CANCER LETTERS

Signal control through Raf: in sickness and in health

(2011) Jihan K Osborne et al.   CELL RESEARCH

“Going KiNativ”: Probing the Native Kinome

(2011) Lee M. Graves et al.   CHEMISTRY & BIOLOGY

In Situ Kinase Profiling Reveals Functionally Relevant Properties of Native Kinases

(2011) Matthew P. Patricelli et al.   CHEMISTRY & BIOLOGY

Mechanisms of drug resistance in kinases

(2011) Rina Barouch-Bentov et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Induction of Cutaneous Squamous Cell Carcinomas by RAF Inhibitors: Cause for Concern?

(2011) Mario E. Lacouture et al.   JOURNAL OF CLINICAL ONCOLOGY

RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E)

(2011) Poulikos I. Poulikakos et al.   NATURE

Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity

(2011) Theonie Anastassiadis et al.   NATURE BIOTECHNOLOGY

Combating trastuzumab resistance by targeting SRC, a common node downstream of multiple resistance pathways

(2011) Siyuan Zhang et al.   NATURE MEDICINE

Acquired MET expression confers resistance to EGFR inhibition in a mouse model of glioblastoma multiforme

(2011) H J Jun 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

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

Amplification of the Driving Oncogene, KRAS or BRAF, Underpins Acquired Resistance to MEK1/2 Inhibitors in Colorectal Cancer Cells

(2011) A. S. Little et al.   Science Signaling

Resistance to MEK Inhibitors: Should We Co-Target Upstream?

(2011) P. I. Poulikakos et al.   Science Signaling

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

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

Epidermal Growth Factor Receptor cooperates with Src Family Kinases in acquired resistance to cetuximab

(2010) Deric L. Wheeler et al.   CANCER BIOLOGY & THERAPY

Preexistence and Clonal Selection of MET Amplification in EGFR Mutant NSCLC

(2010) Alexa B. Turke et al.   CANCER CELL

Acquired Resistance to BRAF Inhibitors Mediated by a RAF Kinase Switch in Melanoma Can Be Overcome by Cotargeting MEK and IGF-1R/PI3K

(2010) Jessie Villanueva et al.   CANCER CELL

Genetic and Structural Variation in the Gastric Cancer Kinome Revealed through Targeted Deep Sequencing

(2010) Z. J. Zang et al.   CANCER RESEARCH

Kinase-Dead BRAF and Oncogenic RAS Cooperate to Drive Tumor Progression through CRAF

(2010) Sonja J. Heidorn et al.   CELL

Targeting Multiple Kinase Pathways: A Change In Paradigm

(2010) L. Gossage et al.   CLINICAL CANCER RESEARCH

New Opportunities to Treat the T315I-Bcr-Abl Mutant in Chronic Myeloid Leukaemia: Tyrosine Kinase Inhibitors and Molecules that Act by Alternative Mechanisms

(2010) S. Schenone et al.   CURRENT MEDICINAL CHEMISTRY

Quantifying oncogenic phosphotyrosine signaling networks through systems biology

(2010) Amanda M Del Rosario et al.   CURRENT OPINION IN GENETICS & DEVELOPMENT

Epidermal growth factor receptor inhibitors in oncology

(2010) Igor Vivanco et al.   CURRENT OPINION IN ONCOLOGY

RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF

(2010) Poulikos I. Poulikakos et al.   NATURE

RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth

(2010) Georgia Hatzivassiliou et al.   NATURE

Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma

(2010) Gideon Bollag et al.   NATURE

COT drives resistance to RAF inhibition through MAP kinase pathway reactivation

(2010) Cory M. Johannessen et al.   NATURE

Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation

(2010) Ramin Nazarian et al.   NATURE

The (un)targeted cancer kinome

(2010) Oleg Fedorov et al.   Nature Chemical Biology

A chemical and phosphoproteomic characterization of dasatinib action in lung cancer

(2010) Jiannong Li et al.   Nature Chemical Biology

Rapidly Acquired Resistance to EGFR Tyrosine Kinase Inhibitors in NSCLC Cell Lines through De-Repression of FGFR2 and FGFR3 Expression

(2010) Kathryn E. Ware et al.   PLoS One

Analysis of Kinase Gene Expression Patterns across 5681 Human Tissue Samples Reveals Functional Genomic Taxonomy of the Kinome

(2010) Sami Kilpinen et al.   PLoS One

BRAF Gene Amplification Can Promote Acquired Resistance to MEK Inhibitors in Cancer Cells Harboring the BRAF V600E Mutation

(2010) R. B. Corcoran et al.   Science Signaling

Integrating BRAF/MEK inhibitors into combination therapy for melanoma

(2009) K S M Smalley et al.   BRITISH JOURNAL OF CANCER

Kinome signaling through regulated protein–protein interactions in normal and cancer cells

(2009) Tony Pawson et al.   CURRENT OPINION IN CELL BIOLOGY

ErbB receptors and signaling pathways in cancer

(2009) Nancy E Hynes et al.   CURRENT OPINION IN CELL BIOLOGY

A comprehensive target selectivity survey of the BCR-ABL kinase inhibitor INNO-406 by kinase profiling and chemical proteomics in chronic myeloid leukemia cells

(2009) U Rix et al.   LEUKEMIA

Global Effects of Kinase Inhibitors on Signaling Networks Revealed by Quantitative Phosphoproteomics

(2009) Cuiping Pan et al.   MOLECULAR & CELLULAR PROTEOMICS

Large-scale Proteomics Analysis of the Human Kinome

(2009) Felix S. Oppermann et al.   MOLECULAR & CELLULAR PROTEOMICS

Oncogenic B-RAF Negatively Regulates the Tumor Suppressor LKB1 to Promote Melanoma Cell Proliferation

(2009) Bin Zheng et al.   MOLECULAR CELL

Inhibitors paradoxically prime kinases

(2009) Stephen V Frye et al.   Nature Chemical Biology

Target profiling of small molecules by chemical proteomics

(2009) Uwe Rix et al.   Nature Chemical Biology

Uncoupling of the LKB1-AMPKα Energy Sensor Pathway by Growth Factors and Oncogenic BRAFV600E

(2009) Rosaura Esteve-Puig et al.   PLoS One

MEK1 mutations confer resistance to MEK and B-RAF inhibition

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

Kinase-Selective Enrichment Enables Quantitative Phosphoproteomics of the Kinome across the Cell Cycle

(2008) Henrik Daub et al.   MOLECULAR CELL

A quantitative analysis of kinase inhibitor selectivity

(2008) Mazen W Karaman et al.   NATURE BIOTECHNOLOGY

EGFR Antagonists in Cancer Treatment

(2008) Fortunato Ciardiello et al.   NEW ENGLAND JOURNAL OF MEDICINE