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Repurposing covalent EGFR/HER2 inhibitors for on-target degradation of human Tribbles 2 (TRIB2) pseudokinase
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Outgoing claims: the papers this work cites, builds on, or argues with.
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A comprehensive review of the preclinical efficacy profile of the ErbB family blocker afatinib in cancer
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Ubiquitin E3 ligase SCFβ-TRCP regulates TRIB2 stability in liver cancer cells
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Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors
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Thienopyrimidine-based dual EGFR/ErbB-2 inhibitors
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Neratinib induces ErbB2 ubiquitylation and endocytic degradation via HSP90 dissociation in breast cancer cells
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Tribbles homolog 2 inactivates C/EBPα and causes acute myelogenous leukemia
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Quantitative Analysis of Hsp90-Client Interactions Reveals Principles of Substrate Recognition
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Activation State-Dependent Binding of Small Molecule Kinase Inhibitors: Structural Insights from Biochemistry
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Discovery of Potent and Selective Covalent Inhibitors of JNK
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Developing Irreversible Inhibitors of the Protein Kinase Cysteinome
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Conformation-Selective ATP-Competitive Inhibitors Control Regulatory Interactions and Noncatalytic Functions of Mitogen-Activated Protein Kinases
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Targeted Protein Degradation: from Chemical Biology to Drug Discovery
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Small-Molecule Kinase Downregulators
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Overcoming Resistance to the THZ Series of Covalent Transcriptional CDK Inhibitors
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SRPKIN-1: A Covalent SRPK1/2 Inhibitor that Potently Converts VEGF from Pro-angiogenic to Anti-angiogenic Isoform
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Targeting non-small cell lung cancer with small-molecule EGFR tyrosine kinase inhibitors
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Live and let die: insights into pseudoenzyme mechanisms from structure
inferredcites →https://doi.org/10.1016/j.str.2015.08.017openalex-snapshot
Molecular Mechanism of CCAAT-Enhancer Binding Protein Recruitment by the TRIB1 Pseudokinase
inferredcites →https://doi.org/10.1016/j.str.2015.10.003openalex-snapshot
TRIBBLES: A Twist in the Pseudokinase Tail
inferredcites →https://doi.org/10.1016/j.str.2015.10.020openalex-snapshot
Structural Basis for the Non-catalytic Functions of Protein Kinases
inferredcites →https://doi.org/10.1016/j.str.2016.12.008openalex-snapshot
STK40 Is a Pseudokinase that Binds the E3 Ubiquitin Ligase COP1
inferredcites →https://doi.org/10.1016/j.tcb.2014.03.008openalex-snapshot
Day of the dead: pseudokinases and pseudophosphatases in physiology and disease
inferredcites →https://doi.org/10.1016/j.tcb.2016.11.002openalex-snapshot
Tribbles in the 21st Century: The Evolving Roles of Tribbles Pseudokinases in Biology and Disease
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Use of a drug‐resistant mutant of stress‐activated protein kinase 2a/p38 to validate the in vivo specificity of SB 203580
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Structure and activity of a unique heparin-derived hexasaccharide.
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Discovery and Biological Evaluation of Potent Dual ErbB-2/EGFR Tyrosine Kinase Inhibitors: 6-Thiazolylquinazolines
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Lapatinib with trastuzumab for HER2-positive early breast cancer (NeoALTTO): survival outcomes of a randomised, open-label, multicentre, phase 3 trial and their association with pathological complete response
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Determining Cysteines Available for Covalent Inhibition Across the Human Kinome
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Identification and Characterization of JAK2 Pseudokinase Domain Small Molecule Binders
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JAK2 JH2 Fluorescence Polarization Assay and Crystal Structures for Complexes with Three Small Molecules
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Drug-Resistant Aurora A Mutants for Cellular Target Validation of the Small Molecule Kinase Inhibitors MLN8054 and MLN8237
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Electrophilic Fragment-Based Design of Reversible Covalent Kinase Inhibitors
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Loss of Tribbles pseudokinase-3 promotes Akt-driven tumorigenesis via FOXO inactivation
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K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions
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Comprehensive analysis of kinase inhibitor selectivity
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Chaperones as thermodynamic sensors of drug-target interactions reveal kinase inhibitor specificities in living cells
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Comprehensive characterization of the Published Kinase Inhibitor Set
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ATP-competitive inhibitors block protein kinase recruitment to the Hsp90-Cdc37 system
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A unique inhibitor binding site in ERK1/2 is associated with slow binding kinetics
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Pharmacological targeting of the pseudokinase Her3
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Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors
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RETRACTED ARTICLE: TRIB2 confers resistance to anti-cancer therapy by activating the serine/threonine protein kinase AKT
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I-TASSER: a unified platform for automated protein structure and function prediction
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Targeting cancer with small molecule kinase inhibitors
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Induced protein degradation: an emerging drug discovery paradigm
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Kinase inhibitors: the road ahead
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Human TRIB2 is a repressor of FOXO that contributes to the malignant phenotype of melanoma cells
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Overexpression of TRIB2 in human lung cancers contributes to tumorigenesis through downregulation of C/EBPα
inferredcites →https://doi.org/10.1038/onc.2016.66openalex-snapshot
The presence of C/EBPα and its degradation are both required for TRIB2-mediated leukaemia
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KinView: a visual comparative sequence analysis tool for integrated kinome research
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cAMP-dependent protein kinase (PKA) complexes probed by complementary differential scanning fluorimetry and ion mobility–mass spectrometry
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Phosphoregulation of human Mps1 kinase
inferredcites →https://doi.org/10.1042/bj20131174openalex-snapshot
A robust methodology to subclassify pseudokinases based on their nucleotide-binding properties
inferredcites →https://doi.org/10.1042/bj20141441openalex-snapshot
The Tribbles 2 (TRB2) pseudokinase binds to ATP and autophosphorylates in a metal-independent manner
inferredcites →https://doi.org/10.1042/bst20130115openalex-snapshot
Dawn of the dead: protein pseudokinases signal new adventures in cell biology
inferredcites →https://doi.org/10.1042/bst20150103openalex-snapshot
TRIB2 and the ubiquitin proteasome system in cancer
inferredcites →https://doi.org/10.1042/bst20150109openalex-snapshot
Tribbles pseudokinases: novel targets for chemical biology and drug discovery?
inferredcites →https://doi.org/10.1073/pnas.0912101106openalex-snapshot
Structural analysis of the catalytically inactive kinase domain of the human EGF receptor 3
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Covalent EGFR inhibitor analysis reveals importance of reversible interactions to potency and mechanisms of drug resistance
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Pharmacologic shifting of a balance between protein refolding and degradation mediated by Hsp90
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Discovery and Exploitation of Inhibitor-resistant Aurora and Polo Kinase Mutants for the Analysis of Mitotic Networks
inferredcites →https://doi.org/10.1074/jbc.m110.206193openalex-snapshot
Structural Analysis of the Mechanism of Inhibition and Allosteric Activation of the Kinase Domain of HER2 Protein
inferredcites →https://doi.org/10.1074/jbc.m701409200openalex-snapshot
TRB2, a Mouse Tribbles Ortholog, Suppresses Adipocyte Differentiation by Inhibiting AKT and C/EBPβ
inferredcites →https://doi.org/10.1089/adt.2011.0380openalex-snapshot
Molecular Interaction Studies Using Microscale Thermophoresis
inferredcites →https://doi.org/10.1093/carcin/bgv002openalex-snapshot
TRIB2 as a biomarker for diagnosis and progression of melanoma
inferredcites →https://doi.org/10.1111/febs.12224openalex-snapshot
Redox regulation of protein kinases
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Kinome‐wide transcriptional profiling of uveal melanoma reveals new vulnerabilities to targeted therapeutics
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Target Binding Properties and Cellular Activity of Afatinib (BIBW 2992), an Irreversible ErbB Family Blocker
inferredcites →https://doi.org/10.1124/pr.113.007450openalex-snapshot
Idiosyncratic Adverse Drug Reactions: Current Concepts
inferredcites →https://doi.org/10.1126/science.1079817openalex-snapshot
TRB3: A tribbles Homolog That Inhibits Akt/PKB Activation by Insulin in Liver
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Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay
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Tracking cancer drugs in living cells by thermal profiling of the proteome
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The target landscape of clinical kinase drugs
inferredcites →https://doi.org/10.1126/science.aan8795openalex-snapshot
Cell cycle heterogeneity directs the timing of neural stem cell activation from quiescence
inferredcites →https://doi.org/10.1158/0008-5472.can-16-3404openalex-snapshot
Response Heterogeneity of EGFR and HER2 Exon 20 Insertions to Covalent EGFR and HER2 Inhibitors
inferredcites →https://doi.org/10.1158/1078-0432.ccr-17-1875openalex-snapshot
Targeting HER2 Aberrations in Non–Small Cell Lung Cancer with Osimertinib
inferredcites →https://doi.org/10.1182/blood-2009-10-247361openalex-snapshot
Transformation by Tribbles homolog 2 (Trib2) requires both the Trib2 kinase domain and COP1 binding
inferredcites →https://doi.org/10.1182/blood-2012-12-471300openalex-snapshot
Tribbles in acute leukemia
inferredcites →https://doi.org/10.1182/blood-2013-07-511683openalex-snapshot
Regulation of Trib2 by an E2F1-C/EBPα feedback loop in AML cell proliferation
inferredcites →https://doi.org/10.1186/1758-2946-4-17openalex-snapshot
Avogadro: an advanced semantic chemical editor, visualization, and analysis platform
inferredcites →https://doi.org/10.1200/jco.2009.26.7278openalex-snapshot
Phase I Trial of the Irreversible EGFR and HER2 Kinase Inhibitor BIBW 2992 in Patients With Advanced Solid Tumors
inferredcites →https://doi.org/10.1200/jco.2009.27.9414openalex-snapshot
Neratinib, an Irreversible Pan-ErbB Receptor Tyrosine Kinase Inhibitor: Results of a Phase II Trial in Patients With Advanced Non–Small-Cell Lung Cancer
inferredcites →https://doi.org/10.1371/journal.pone.0059004openalex-snapshot
A Pareto-Optimal Refinement Method for Protein Design Scaffolds
inferredcites →https://doi.org/10.1371/journal.pone.0098800openalex-snapshot
A Comparison of Protein Kinases Inhibitor Screening Methods Using Both Enzymatic Activity and Binding Affinity Determination
inferredcites →https://doi.org/10.1517/13543780903305428openalex-snapshot
Neratinib: an oral, irreversible dual EGFR/HER2 inhibitor for breast and non-small cell lung cancer
inferredcites →https://doi.org/10.15252/embj.201693929openalex-snapshot
The hVps34‐SGK3 pathway alleviates sustained PI3K/Akt inhibition by stimulating mTORC1 and tumour growth
inferredcites →https://doi.org/10.1634/theoncologist.12-7-756openalex-snapshot
Lapatinib-Associated Toxicity and Practical Management Recommendations
inferredcites →https://doi.org/10.18632/oncotarget.24525openalex-snapshot
Trib2 expression in granulocyte-monocyte progenitors drives a highly drug resistant acute myeloid leukaemia linked to elevated Bcl2
inferredcites →https://doi.org/10.3390/ijms17091378openalex-snapshot
Human TRIB2 Oscillates during the Cell Cycle and Promotes Ubiquitination and Degradation of CDC25C
inferredcites →https://doi.org/10.4155/fmc-2016-0207openalex-snapshot
Pseudokinases: Update on Their Functions and Evaluation as New Drug Targets
inferredcites →https://doi.org/10.4161/23723556.2014.980134openalex-snapshot
TRIB3 suppresses tumorigenesis by controlling mTORC2/AKT/FOXO signaling.
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