Overcoming resistance to HER2 inhibitors through state-specific kinase binding

Activation Mechanism of Oncogenic Deletion Mutations in BRAF, EGFR, and HER2

(2016) Scott A. Foster et al.   CANCER CELL

A Structural Perspective on the Regulation of the Epidermal Growth Factor Receptor

(2015) Erika Kovacs et al.   Annual Review of Biochemistry

Growth Factor Identity Is Encoded by Discrete Coiled-Coil Rotamers in the EGFR Juxtamembrane Region

(2015) Amy Doerner et al.   CHEMISTRY & BIOLOGY

The EGFR-HER2 module: a stem cell approach to understanding a prime target and driver of solid tumors

(2015) M R Schneider et al.   ONCOGENE

Identification and Characterization of a Novel Chemotype MEK Inhibitor Able to Alter the Phosphorylation State of MEK1/2

(2015) Takayuki Yoshida et al.   Oncotarget

Structural analysis of the EGFR/HER3 heterodimer reveals the molecular basis for activating HER3 mutations

(2014) P. Littlefield et al.   Science Signaling

The EGFR Family: Not So Prototypical Receptor Tyrosine Kinases

(2014) M. A. Lemmon et al.   Cold Spring Harbor Perspectives in Biology

Oncogenic ERBB3 Mutations in Human Cancers

(2013) Bijay S. Jaiswal et al.   CANCER CELL

Human Breast Cancer Cells Harboring a Gatekeeper T798M Mutation in HER2 Overexpress EGFR Ligands and Are Sensitive to Dual Inhibition of EGFR and HER2

(2013) B. N. Rexer et al.   CLINICAL CANCER RESEARCH

Dual Targeting of HER2-Positive Cancer with Trastuzumab Emtansine and Pertuzumab: Critical Role for Neuregulin Blockade in Antitumor Response to Combination Therapy

(2013) G. D. L. Phillips et al.   CLINICAL CANCER RESEARCH

Mechanism for activation of mutated epidermal growth factor receptors in lung cancer

(2013) M. Red Brewer et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Erlotinib binds both inactive and active conformations of the EGFR tyrosine kinase domain

(2012) Jin H. Park et al.   BIOCHEMICAL JOURNAL

HER3 Is Required for HER2-Induced Preneoplastic Changes to the Breast Epithelium and Tumor Formation

(2012) D. B. Vaught et al.   CANCER RESEARCH

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

(2012) Timothy R. Wilson et al.   NATURE

Trastuzumab Emtansine for HER2-Positive Advanced Breast Cancer

(2012) Sunil Verma et al.   NEW ENGLAND JOURNAL OF MEDICINE

Functional analysis of receptor tyrosine kinase mutations in lung cancer identifies oncogenic extracellular domain mutations of ERBB2

(2012) H. Greulich et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Activating HER2 Mutations in HER2 Gene Amplification Negative Breast Cancer

(2012) Ron Bose et al.   Cancer Discovery

Neuregulin-1-Mediated Autocrine Signaling Underlies Sensitivity to HER2 Kinase Inhibitors in a Subset of Human Cancers

(2011) Timothy R. Wilson et al.   CANCER CELL

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

(2011) Sarat Chandarlapaty et al.   CANCER CELL

Structural Analysis of the Mechanism of Inhibition and Allosteric Activation of the Kinase Domain of HER2 Protein

(2011) Kathleen Aertgeerts et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Mechanistic insights into the activation of oncogenic forms of EGF receptor

(2011) Zhihong Wang et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

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

Quantitation of p95HER2 in Paraffin Sections by Using a p95-Specific Antibody and Correlation with Outcome in a Cohort of Trastuzumab-Treated Breast Cancer Patients

(2010) J. Sperinde et al.   CLINICAL CANCER RESEARCH

Reactivation of epigenetically silenced HER4/ERBB4 results in apoptosis of breast tumor cells

(2010) P M Das et al.   ONCOGENE

ErbB3/HER3 intracellular domain is competent to bind ATP and catalyze autophosphorylation

(2010) Fumin Shi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Resiliency and Vulnerability in the HER2-HER3 Tumorigenic Driver

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

Mechanism for Activation of the EGF Receptor Catalytic Domain by the Juxtamembrane Segment

(2009) Natalia Jura et al.   CELL

The Juxtamembrane Region of the EGF Receptor Functions as an Activation Domain

(2009) Monica Red Brewer et al.   MOLECULAR CELL

Enzymatic assembly of DNA molecules up to several hundred kilobases

(2009) Daniel G Gibson et al.   NATURE METHODS

Inhibitors of HSP90 block p95-HER2 signaling in Trastuzumab-resistant tumors and suppress their growth

(2009) S Chandarlapaty et al.   ONCOGENE

Structural analysis of the catalytically inactive kinase domain of the human EGF receptor 3

(2009) N. Jura 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