Covalent inhibitors of EGFR family protein kinases induce degradation of human Tribbles 2 (TRIB2) pseudokinase in cancer cells

The Cysteinome of Protein Kinases as a Target in Drug Development

(2018) Apirat Chaikuad et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

New tools for evaluating protein tyrosine sulphation: Tyrosyl Protein Sulphotransferases (TPSTs) are novel targets for RAF protein kinase inhibitors

(2018) Dominic P Byrne et al.   BIOCHEMICAL JOURNAL

Targeting non-small cell lung cancer with small-molecule EGFR tyrosine kinase inhibitors

(2018) Mahaveer Singh et al.   DRUG DISCOVERY TODAY

Kinase inhibitors: the road ahead

(2018) Fleur M. Ferguson et al.   NATURE REVIEWS DRUG DISCOVERY

Cell cycle heterogeneity directs the timing of neural stem cell activation from quiescence

(2018) L. Otsuki et al.   SCIENCE

Substrate binding allosterically relieves autoinhibition of the pseudokinase TRIB1

(2018) Sam A. Jamieson et al.   Science Signaling

Pseudokinases: update on their functions and evaluation as new drug targets

(2017) Dominic P Byrne et al.   Future Medicinal Chemistry

Determining Cysteines Available for Covalent Inhibition Across the Human Kinome

(2017) Zheng Zhao et al.   JOURNAL OF MEDICINAL CHEMISTRY

Kinome-wide transcriptional profiling of uveal melanoma reveals new vulnerabilities to targeted therapeutics

(2017) Fiona P. Bailey et al.   Pigment Cell & Melanoma Research

The target landscape of clinical kinase drugs

(2017) Susan Klaeger et al.   SCIENCE

STK40 Is a Pseudokinase that Binds the E3 Ubiquitin Ligase COP1

(2017) Izabela Durzynska et al.   STRUCTURE

Tribbles in the 21st Century: The Evolving Roles of Tribbles Pseudokinases in Biology and Disease

(2017) Patrick A. Eyers et al.   TRENDS IN CELL BIOLOGY

DRP-1 is required for BH3 mimetic-mediated mitochondrial fragmentation and apoptosis

(2017) Mateus Milani et al.   Cell Death & Disease

Identification and Characterization of JAK2 Pseudokinase Domain Small Molecule Binders

(2017) David E. Puleo et al.   ACS Medicinal Chemistry Letters

JAK2 JH2 Fluorescence Polarization Assay and Crystal Structures for Complexes with Three Small Molecules

(2017) Ana S. Newton et al.   ACS Medicinal Chemistry Letters

TRIB2 confers resistance to anti-cancer therapy by activating the serine/threonine protein kinase AKT

(2017) Richard Hill et al.   Nature Communications

cAMP-dependent protein kinase (PKA) complexes probed by complementary differential scanning fluorimetry and ion mobility-mass spectrometry

(2016) D. P. Byrne et al.   BIOCHEMICAL JOURNAL

Neratinib induces ErbB2 ubiquitylation and endocytic degradation via HSP90 dissociation in breast cancer cells

(2016) Yingqiu Zhang et al.   CANCER LETTERS

The hVps34‐SGK3 pathway alleviates sustained PI3K/Akt inhibition by stimulating mTORC1 and tumour growth

(2016) Ruzica Bago et al.   EMBO JOURNAL

KinView: a visual comparative sequence analysis tool for integrated kinome research

(2016) Daniel Ian McSkimming et al.   Molecular BioSystems

Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors

(2016) Tinghu Zhang et al.   Nature Chemical Biology

Induced protein degradation: an emerging drug discovery paradigm

(2016) Ashton C. Lai et al.   NATURE REVIEWS DRUG DISCOVERY

The presence of C/EBPα and its degradation are both required for TRIB2-mediated leukaemia

(2016) C O'Connor et al.   ONCOGENE

Structural Basis for the Non-catalytic Functions of Protein Kinases

(2016) Jennifer E. Kung et al.   STRUCTURE

The Tribbles 2 (TRB2) pseudokinase binds to ATP and autophosphorylates in a metal-independent manner

(2015) Fiona P. Bailey et al.   BIOCHEMICAL JOURNAL

Going for broke: targeting the human cancer pseudokinome

(2015) Fiona P. Bailey et al.   BIOCHEMICAL JOURNAL

Tribbles pseudokinases: novel targets for chemical biology and drug discovery?

(2015) D. M. Foulkes et al.   BIOCHEMICAL SOCIETY TRANSACTIONS

TRIB2 and the ubiquitin proteasome system in cancer

(2015) M. Salome et al.   BIOCHEMICAL SOCIETY TRANSACTIONS

TRIB2 as a biomarker for diagnosis and progression of melanoma

(2015) Richard Hill et al.   CARCINOGENESIS

Comprehensive characterization of the Published Kinase Inhibitor Set

(2015) Jonathan M Elkins et al.   NATURE BIOTECHNOLOGY

Covalent docking using autodock: Two-point attractor and flexible side chain methods

(2015) Giulia Bianco et al.   PROTEIN SCIENCE

TRIBBLES: A Twist in the Pseudokinase Tail

(2015) Patrick A. Eyers   STRUCTURE

Molecular Mechanism of CCAAT-Enhancer Binding Protein Recruitment by the TRIB1 Pseudokinase

(2015) James M. Murphy et al.   STRUCTURE

Regulation of Trib2 by an E2F1-C/EBP  feedback loop in AML cell proliferation

(2014) L. Rishi et al.   BLOOD

Loss of Tribbles pseudokinase-3 promotes Akt-driven tumorigenesis via FOXO inactivation

(2014) M Salazar et al.   CELL DEATH AND DIFFERENTIATION

Conformation-Selective ATP-Competitive Inhibitors Control Regulatory Interactions and Noncatalytic Functions of Mitogen-Activated Protein Kinases

(2014) Sanjay B. Hari et al.   CHEMISTRY & BIOLOGY

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

(2014) Evandro de Azambuja et al.   LANCET ONCOLOGY

Pharmacological targeting of the pseudokinase Her3

(2014) Ting Xie et al.   Nature Chemical Biology

A unique inhibitor binding site in ERK1/2 is associated with slow binding kinetics

(2014) Apirat Chaikuad et al.   Nature Chemical Biology

A comprehensive review of the preclinical efficacy profile of the ErbB family blocker afatinib in cancer

(2014) Helmout Modjtahedi et al.   NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY

A Comparison of Protein Kinases Inhibitor Screening Methods Using Both Enzymatic Activity and Binding Affinity Determination

(2014) Amalie Frederikke Rudolf et al.   PLoS One

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

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

Day of the dead: pseudokinases and pseudophosphatases in physiology and disease

(2014) Veronika Reiterer et al.   TRENDS IN CELL BIOLOGY

Therapeutic Targeting of Oncogenic K-Ras by a Covalent Catalytic Site Inhibitor

(2013) Sang Min Lim et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Ubiquitin E3 ligase SCFβ-TRCP regulates TRIB2 stability in liver cancer cells

(2013) Yongxia Qiao et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

A robust methodology to subclassify pseudokinases based on their nucleotide-binding properties

(2013) James M. Murphy et al.   BIOCHEMICAL JOURNAL

Dawn of the dead: protein pseudokinases signal new adventures in cell biology

(2013) Patrick A. Eyers et al.   BIOCHEMICAL SOCIETY TRANSACTIONS

Tribbles in acute leukemia

(2013) K. L. Liang et al.   BLOOD

Developing Irreversible Inhibitors of the Protein Kinase Cysteinome

(2013) Qingsong Liu et al.   CHEMISTRY & BIOLOGY

Redox regulation of protein kinases

(2013) Aoife Corcoran et al.   FEBS Journal

Electrophilic Fragment-Based Design of Reversible Covalent Kinase Inhibitors

(2013) Rand M. Miller et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions

(2013) Jonathan M. Ostrem et al.   NATURE

Chaperones as thermodynamic sensors of drug-target interactions reveal kinase inhibitor specificities in living cells

(2013) Mikko Taipale et al.   NATURE BIOTECHNOLOGY

ATP-competitive inhibitors block protein kinase recruitment to the Hsp90-Cdc37 system

(2013) Sigrun Polier et al.   Nature Chemical Biology

A Pareto-Optimal Refinement Method for Protein Design Scaffolds

(2013) Lucas Gregorio Nivón et al.   PLoS One

Covalent EGFR inhibitor analysis reveals importance of reversible interactions to potency and mechanisms of drug resistance

(2013) P. A. Schwartz et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

(2013) D. M. Molina et al.   SCIENCE

Quantitative Analysis of Hsp90-Client Interactions Reveals Principles of Substrate Recognition

(2012) Mikko Taipale et al.   CELL

Discovery of Potent and Selective Covalent Inhibitors of JNK

(2012) Tinghu Zhang et al.   CHEMISTRY & BIOLOGY

Thiol–Ene Click Chemistry: Computational and Kinetic Analysis of the Influence of Alkene Functionality

(2012) Brian H. Northrop et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Molecular Interaction Studies Using Microscale Thermophoresis

(2011) Moran Jerabek-Willemsen et al.   ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES

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

Comprehensive analysis of kinase inhibitor selectivity

(2011) Mindy I Davis et al.   NATURE BIOTECHNOLOGY

Overexpression of TRIB2 in human lung cancers contributes to tumorigenesis through downregulation of C/EBPα

(2011) K B Grandinetti et al.   ONCOGENE

RosettaRemodel: A Generalized Framework for Flexible Backbone Protein Design

(2011) Po-Ssu Huang et al.   PLoS One

Drug-Resistant Aurora A Mutants for Cellular Target Validation of the Small Molecule Kinase Inhibitors MLN8054 and MLN8237

(2010) Dominic A. Sloane et al.   ACS Chemical Biology

Transformation by Tribbles homolog 2 (Trib2) requires both the Trib2 kinase domain and COP1 binding

(2010) K. Keeshan et al.   BLOOD

Activation State-Dependent Binding of Small Molecule Kinase Inhibitors: Structural Insights from Biochemistry

(2010) Lisa M. Wodicka et al.   CHEMISTRY & BIOLOGY

Neratinib, an Irreversible Pan-ErbB Receptor Tyrosine Kinase Inhibitor: Results of a Phase II Trial in Patients With Advanced Non–Small-Cell Lung Cancer

(2010) Lecia V. Sequist et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase I Trial of the Irreversible EGFR and HER2 Kinase Inhibitor BIBW 2992 in Patients With Advanced Solid Tumors

(2010) Timothy A. Yap et al.   JOURNAL OF CLINICAL ONCOLOGY

I-TASSER: a unified platform for automated protein structure and function prediction

(2010) Ambrish Roy et al.   Nature Protocols

Human TRIB2 is a repressor of FOXO that contributes to the malignant phenotype of melanoma cells

(2010) F Zanella 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

Neratinib: an oral, irreversible dual EGFR/HER2 inhibitor for breast and non-small cell lung cancer

(2009) Prithviraj Bose et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Discovery and Exploitation of Inhibitor-resistant Aurora and Polo Kinase Mutants for the Analysis of Mitotic Networks

(2009) Paul J. Scutt et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

AutoDock Vina: Improving the speed and accuracy of docking with a new scoring function, efficient optimization, and multithreading

(2009) Oleg Trott et al.   JOURNAL OF COMPUTATIONAL CHEMISTRY

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

Phosphoregulation of human Mps1 kinase

(2008) Rebecca K. Tyler et al.   BIOCHEMICAL JOURNAL

Thienopyrimidine-based dual EGFR/ErbB-2 inhibitors

(2008) Tara R. Rheault et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS