Receptor tyrosine kinases and cancer: oncogenic mechanisms and therapeutic approaches

Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery

(2020) George M. Burslem et al.   CELL

Discovery and Optimization of Small Molecules Targeting the Protein–Protein Interaction of Heat Shock Protein 90 (Hsp90) and Cell Division Cycle 37 as Orally Active Inhibitors for the Treatment of Colorectal Cancer

(2020) Lei Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identifying drug targets in tissues and whole blood with thermal-shift profiling

(2020) Jessica Perrin et al.   NATURE BIOTECHNOLOGY

A drug discovery platform to identify compounds that inhibit EGFR triple mutants

(2020) Punit Saraon et al.   Nature Chemical Biology

Antitumor activity of crizotinib in lung cancers harboring a MET exon 14 alteration

(2020) Alexander Drilon et al.   NATURE MEDICINE

Targeting FLT3 mutations in AML: review of current knowledge and evidence

(2019) Naval Daver et al.   LEUKEMIA

Bioluminescence resonance energy transfer–based imaging of protein–protein interactions in living cells

(2019) Hiroyuki Kobayashi et al.   Nature Protocols

Selective inhibition of N-linked glycosylation impairs receptor tyrosine kinase processing

(2019) Elsenoor Klaver et al.   Disease Models & Mechanisms

Single and dual targeting of mutant EGFR with an allosteric inhibitor

(2019) Ciric To et al.   Cancer Discovery

Targeting BCR-ABL1 in Chronic Myeloid Leukemia by PROTAC-mediated Targeted Protein Degradation

(2019) George M Burslem et al.   CANCER RESEARCH

Targeted protein degradation: elements of PROTAC design

(2019) Stacey-Lynn Paiva et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Dynamin inhibitors impair platelet-derived growth factor β-receptor dimerization and signaling

(2019) Johan Heldin et al.   EXPERIMENTAL CELL RESEARCH

The Transcriptional Roles of ALK Fusion Proteins in Tumorigenesis

(2019) Stephen P. Ducray et al.   Cancers

HER2-targeted therapies — a role beyond breast cancer

(2019) Do-Youn Oh et al.   Nature Reviews Clinical Oncology

Structural characterization of EGFR exon 19 deletion mutation using molecular dynamics simulation

(2019) Mahlet Z. Tamirat et al.   PLoS One

Targeted protein degradation: expanding the toolbox

(2019) Matthieu Schapira et al.   NATURE REVIEWS DRUG DISCOVERY

Functional recruitment of dynamin requires multimeric interactions for efficient endocytosis

(2019) Morgane Rosendale et al.   Nature Communications

Crystal structure of EGFR T790M/C797S/V948R in complex with EAI045

(2018) Peng Zhao et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Reactivation of mutant-EGFR degradation through clathrin inhibition overcomes resistance to EGFR tyrosine kinase inhibitors.

(2018) Ludovic Ménard et al.   CANCER RESEARCH

Oligosaccharyltransferase Inhibition Overcomes Therapeutic Resistance to EGFR Tyrosine Kinase Inhibitors

(2018) Cecilia Lopez Sambrooks et al.   CANCER RESEARCH

Multiplexed Proteome Dynamics Profiling Reveals Mechanisms Controlling Protein Homeostasis

(2018) Mikhail M. Savitski et al.   CELL

Oligosaccharyltransferase inhibition Reduces Receptor Tyrosine Kinase Activation and Enhances Glioma Radiosensitivity

(2018) Marta Baro et al.   CLINICAL CANCER RESEARCH

Kinase-targeted cancer therapies: progress, challenges and future directions

(2018) Khushwant S. Bhullar et al.   Molecular Cancer

NanoBRET Approaches to Study Ligand Binding to GPCRs and RTKs

(2018) Leigh A. Stoddart et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Homogeneous Assay for Target Engagement Utilizing Bioluminescent Thermal Shift

(2018) Melanie L. Dart et al.   ACS Medicinal Chemistry Letters

Enhancing Antiproliferative Activity and Selectivity of a FLT-3 Inhibitor by Proteolysis Targeting Chimera Conversion

(2018) George M. Burslem et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Addressing Kinase-Independent Functions of Fak via PROTAC-Mediated Degradation

(2018) Philipp M. Cromm et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

NTRK fusion-positive cancers and TRK inhibitor therapy

(2018) Emiliano Cocco et al.   Nature Reviews Clinical Oncology

Fibroblast growth factor receptors as treatment targets in clinical oncology

(2018) Masaru Katoh   Nature Reviews Clinical Oncology

Systematic Identification of Oncogenic EGFR Interaction Partners

(2017) Julia Petschnigg et al.   JOURNAL OF MOLECULAR BIOLOGY

Broad-Spectrum Kinase Profiling in Live Cells with Lysine-Targeted Sulfonyl Fluoride Probes

(2017) Qian Zhao et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

A Global Analysis of the Receptor Tyrosine Kinase-Protein Phosphatase Interactome

(2017) Zhong Yao et al.   MOLECULAR CELL

Targeting the Golgi apparatus to overcome acquired resistance of non-small cell lung cancer cells to EGFR tyrosine kinase inhibitors

(2017) Yoshimi Ohashi et al.   Oncotarget

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

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

M-COPA, a Golgi Disruptor, Inhibits Cell Surface Expression of MET Protein and Exhibits Antitumor Activity against MET-Addicted Gastric Cancers

(2016) Yoshimi Ohashi et al.   CANCER RESEARCH

Oncogenic KRAS Regulates Tumor Cell Signaling via Stromal Reciprocation

(2016) Christopher J. Tape et al.   CELL

Signal processing by the endosomal system

(2016) Roberto Villaseñor et al.   CURRENT OPINION IN CELL BIOLOGY

Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases

(2016) Ying-Nan P. Chen et al.   NATURE

Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors

(2016) Yong Jia et al.   NATURE

Oligosaccharyltransferase inhibition induces senescence in RTK-driven tumor cells

(2016) Cecilia Lopez-Sambrooks et al.   Nature Chemical Biology

Recurrent MET fusion genes represent a drug target in pediatric glioblastoma

(2016)   NATURE MEDICINE

The use of cellular thermal shift assay (CETSA) to study Crizotinib resistance in ALK-expressing human cancers

(2016) Abdulraheem Alshareef et al.   Scientific Reports

NanoBRET—A Novel BRET Platform for the Analysis of Protein–Protein Interactions

(2015) Thomas Machleidt et al.   ACS Chemical Biology

Insulin/receptor binding: The last piece of the puzzle?

(2015) Pierre De Meyts   BIOESSAYS

Paracrine Effect of NRG1 and HGF Drives Resistance to MEK Inhibitors in Metastatic Uveal Melanoma

(2015) H. Cheng et al.   CANCER RESEARCH

Insulator dysfunction and oncogene activation in IDH mutant gliomas

(2015) William A. Flavahan et al.   NATURE

Catalytic in vivo protein knockdown by small-molecule PROTACs

(2015) Daniel P Bondeson et al.   Nature Chemical Biology

Acquired EGFR C797S mutation mediates resistance to AZD9291 in non–small cell lung cancer harboring EGFR T790M

(2015) Kenneth S Thress et al.   NATURE MEDICINE

Regulation of EGFR signal transduction by analogue-to-digital conversion in endosomes

(2015) Roberto Villaseñor et al.   eLife

Different Epidermal Growth Factor (EGF) Receptor Ligands Show Distinct Kinetics and Biased or Partial Agonism for Homodimer and Heterodimer Formation

(2014) Jennifer L. Macdonald-Obermann et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The mammalian-membrane two-hybrid assay (MaMTH) for probing membrane-protein interactions in human cells

(2014) Julia Petschnigg et al.   NATURE METHODS

Synthesis of the Pitstop family of clathrin inhibitors

(2014) Mark J Robertson et al.   Nature Protocols

The cellular thermal shift assay for evaluating drug target interactions in cells

(2014) Rozbeh Jafari et al.   Nature Protocols

Tracking cancer drugs in living cells by thermal profiling of the proteome

(2014) M. M. Savitski et al.   SCIENCE

The Somatic Genomic Landscape of Glioblastoma

(2013) Cameron W. Brennan et al.   CELL

The epidermal growth factor receptor variant III (EGFRvIII): where wild things are altered

(2013) Hui K. Gan et al.   FEBS Journal

Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay

(2013) D. M. Molina et al.   SCIENCE

Bypass Mechanisms of Resistance to Receptor Tyrosine Kinase Inhibition in Lung Cancer

(2013) M. J. Niederst et al.   Science Signaling

Endocytosis and Cancer

(2013) I. Mellman et al.   Cold Spring Harbor Perspectives in Biology

Tumour micro-environment elicits innate resistance to RAF inhibitors through HGF secretion

(2012) Ravid Straussman et al.   NATURE

Autocrine activation of the MET receptor tyrosine kinase in acute myeloid leukemia

(2012) Alex Kentsis et al.   NATURE MEDICINE

Transforming Fusions of FGFR and TACC Genes in Human Glioblastoma

(2012) D. Singh et al.   SCIENCE

Rescue Screens with Secreted Proteins Reveal Compensatory Potential of Receptor Tyrosine Kinases in Driving Cancer Growth

(2012) Fred Harbinski et al.   Cancer Discovery

Role of the Clathrin Terminal Domain in Regulating Coated Pit Dynamics Revealed by Small Molecule Inhibition

(2011) Lisa von Kleist et al.   CELL

Comprehensive analysis of receptor tyrosine kinase activation in human melanomas reveals autocrine signaling through IGF-1R

(2011) Kerrington R. Molhoek et al.   MELANOMA RESEARCH

A direct role for Met endocytosis in tumorigenesis

(2011) Carine Joffre et al.   NATURE CELL BIOLOGY

A Neutralizing RNA Aptamer against EGFR Causes Selective Apoptotic Cell Death

(2011) Carla Lucia Esposito et al.   PLoS One

COPI-mediated retrograde trafficking from the Golgi to the ER regulates EGFR nuclear transport

(2010) Ying-Nai Wang et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Preexistence and Clonal Selection of MET Amplification in EGFR Mutant NSCLC

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

Cell Signaling by Receptor Tyrosine Kinases

(2010) Mark A. Lemmon et al.   CELL

Molecular Imaging of N-linked Glycosylation Suggests Glycan Biosynthesis Is a Novel Target for Cancer Therapy

(2010) J. N. Contessa et al.   CLINICAL CANCER RESEARCH

Aberrant trafficking of NSCLC-associated EGFR mutants through the endocytic recycling pathway promotes interaction with Src@

(2009) Byung Chung et al.   BMC CELL BIOLOGY

Lung Adenocarcinoma with EGFR Amplification Has Distinct Clinicopathologic and Molecular Features in Never-Smokers

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

Principles of Cancer Therapy: Oncogene and Non-oncogene Addiction

(2009) Ji Luo et al.   CELL

Mislocalized Activation of Oncogenic RTKs Switches Downstream Signaling Outcomes

(2009) Chunaram Choudhary et al.   MOLECULAR CELL

Endocytosis and signalling: intertwining molecular networks

(2009) Alexander Sorkin et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Inhibition of N-Linked Glycosylation Disrupts Receptor Tyrosine Kinase Signaling in Tumor Cells

(2008) J. N. Contessa et al.   CANCER RESEARCH

Hepatocyte Growth Factor Induces Gefitinib Resistance of Lung Adenocarcinoma with Epidermal Growth Factor Receptor-Activating Mutations

(2008) S. Yano et al.   CANCER RESEARCH

Functions of Paracrine PDGF Signaling in the Proangiogenic Tumor Stroma Revealed by Pharmacological Targeting

(2008) Kristian Pietras et al.   PLOS MEDICINE

The molecular functions of Shp2 in the Ras/Mitogen-activated protein kinase (ERK1/2) pathway

(2007) Marie Dance et al.   CELLULAR SIGNALLING