Structure and Dynamics of the EGF Receptor as Revealed by Experiments and Simulations and Its Relevance to Non-Small Cell Lung Cancer

scientific article published on 05 April 2019

Structure and Dynamics of the EGF Receptor as Revealed by Experiments and Simulations and Its Relevance to Non-Small Cell Lung Cancer is …
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scholarly articleQ13442814

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P356DOI10.3390/CELLS8040316
P932PMC publication ID6523254
P698PubMed publication ID30959819

P50authorFrancesco Luigi GervasioQ54665519
P2093author name stringDavid T Clarke
Laura C Zanetti-Domingues
Marisa L Martin-Fernandez
Selene K Roberts
P2860cites workAn allosteric mechanism for activation of the kinase domain of epidermal growth factor receptorQ24293598
EGF activates its receptor by removing interactions that autoinhibit ectodomain dimerizationQ24296900
Inhibition of the EGF receptor by binding of MIG6 to an activating kinase domain interfaceQ24301761
Crystal structure of a truncated epidermal growth factor receptor extracellular domain bound to transforming growth factor alphaQ24307630
Crystal structure of the complex of human epidermal growth factor and receptor extracellular domainsQ24307661
Mechanism for activation of the EGF receptor catalytic domain by the juxtamembrane segmentQ24309071
Conformational coupling across the plasma membrane in activation of the EGF receptorQ24313122
Oncogenic mutations counteract intrinsic disorder in the EGFR kinase and promote receptor dimerizationQ24321210
The Protein Data BankQ24515306
The extracellular region of ErbB4 adopts a tethered conformation in the absence of ligandQ24536067
Cell signaling by receptor tyrosine kinasesQ24598357
Energy transfer: a spectroscopic rulerQ24618609
ErbB3/HER3 intracellular domain is competent to bind ATP and catalyze autophosphorylationQ24621754
The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATPQ24649549
Cholesterol depletion results in site-specific increases in epidermal growth factor receptor phosphorylation due to membrane level effects. Studies with cholesterol enantiomersQ24650803
A conserved protonation-dependent switch controls drug binding in the Abl kinaseQ24657421
Non-small cell lung cancer: current treatment and future advancesQ26740333
Molecular dynamics simulations: advances and applicationsQ26775869
A practical guide to small angle X-ray scattering (SAXS) of flexible and intrinsically disordered proteinsQ26796304
Markov state models of biomolecular conformational dynamicsQ26827934
Enhanced dimerization drives ligand-independent activity of mutant epidermal growth factor receptor in lung cancerQ27305848
A primer to single-particle cryo-electron microscopyQ27322872
Conformational Changes in the Epidermal Growth Factor Receptor: Role of the Transmembrane Domain Investigated by Coarse-Grained MetaDynamics Free Energy CalculationsQ27336007
Crystal structures of the kinase domain of c-Abl in complex with the small molecule inhibitors PD173955 and imatinib (STI-571)Q27639449
Structure of the epidermal growth factor receptor kinase domain alone and in complex with a 4-anilinoquinazoline inhibitorQ27639528
The crystal structure of a truncated ErbB2 ectodomain reveals an active conformation, poised to interact with other ErbB receptorsQ27640631
Structures of Lung Cancer-Derived EGFR Mutants and Inhibitor Complexes: Mechanism of Activation and Insights into Differential Inhibitor SensitivityQ27644014
The Juxtamembrane Region of the EGF Receptor Functions as an Activation DomainQ27646344
Structural analysis of the catalytically inactive kinase domain of the human EGF receptor 3Q27646596
6-Ethynylthieno[3,2-d]- and 6-ethynylthieno[2,3-d]pyrimidin-4-anilines as tunable covalent modifiers of ErbB kinasesQ27649889
4-Amino-6-arylamino-pyrimidine-5-carbaldehyde hydrazones as potent ErbB-2/EGFR dual kinase inhibitorsQ27651329
ErbB2 resembles an autoinhibited invertebrate epidermal growth factor receptorQ27657234
Novel mutant-selective EGFR kinase inhibitors against EGFR T790MQ27658766
Structural Evidence for Loose Linkage between Ligand Binding and Kinase Activation in the Epidermal Growth Factor ReceptorQ27664452
Erlotinib binds both inactive and active conformations of the EGFR tyrosine kinase domainQ27674725
Structural basis for the altered drug sensitivities of non-small cell lung cancer-associated mutants of human epidermal growth factor receptorQ27677383
Sequence Determinants of a Specific Inactive Protein Kinase ConformationQ27678722
Structural Evaluation of EGFR Inhibition Mechanisms for Nanobodies/VHH DomainsQ27678732
Mechanism for activation of mutated epidermal growth factor receptors in lung cancerQ27679902
A single ligand is sufficient to activate EGFR dimersQ27681167
Insights into the Aberrant Activity of Mutant EGFR Kinase Domain and Drug RecognitionQ27683650
Structures of the tyrosine kinase domain of fibroblast growth factor receptor in complex with inhibitorsQ27737008
N-Glycan fucosylation of epidermal growth factor receptor modulates receptor activity and sensitivity to epidermal growth factor receptor tyrosine kinase inhibitorQ39946177
Alternative packing of EGFR transmembrane domain suggests that protein-lipid interactions underlie signal conduction across membrane.Q39977877
Unligated epidermal growth factor receptor forms higher order oligomers within microclusters on A431 cells that are sensitive to tyrosine kinase inhibitor binding.Q40155127
Functional effects of glycosylation at Asn-579 of the epidermal growth factor receptorQ40353804
Ligand-induced dimer-tetramer transition during the activation of the cell surface epidermal growth factor receptor-A multidimensional microscopy analysisQ40402524
Epidermal growth factor stimulates phosphorylation in membrane preparations in vitroQ40693948
Activation of preformed EGF receptor dimers by ligand-induced rotation of the transmembrane domainQ40782870
Functional analysis of the ligand binding site of EGF-receptor utilizing chimeric chicken/human receptor molecules.Q40817131
Growth Factor Identity Is Encoded by Discrete Coiled-Coil Rotamers in the EGFR Juxtamembrane Region.Q40820169
How Hsp90 and Cdc37 Lubricate Kinase Molecular SwitchesQ41596905
Occupy EGFR.Q41976220
Interactions of the EGFR juxtamembrane domain with PIP2-containing lipid bilayers: Insights from multiscale molecular dynamics simulationsQ41984481
Regulation of receptor tyrosine kinase ligand processingQ41994915
Ligand-induced structural transitions in ErbB receptor extracellular domainsQ42032357
Neratinib, an irreversible pan-ErbB receptor tyrosine kinase inhibitor: results of a phase II trial in patients with advanced non-small-cell lung cancerQ43061055
EGFR: Tale of the C‐terminal tailQ43080915
Fluorescence Lifetime Imaging Microscopy for Quantitative Biological ImagingQ44732189
Structural basis for inhibition of the epidermal growth factor receptor by cetuximabQ45345151
Incidence and mortality of lung cancer: global trends and association with socioeconomic statusQ45489340
A structural model for the membrane-bound form of the juxtamembrane domain of the epidermal growth factor receptorQ46445840
Structure of the kinase domain of an imatinib-resistant Abl mutant in complex with the Aurora kinase inhibitor VX-680.Q46462162
N-glycan of ErbB family plays a crucial role in dimer formation and tumor promotion.Q46883768
Pockets as structural descriptors of EGFR kinase conformationsQ47162698
The Interplay between Structural Stability and Plasticity Determines Mutation Profiles and Chaperone Dependence in Protein Kinases.Q47269892
EGFR Ligands Differentially Stabilize Receptor Dimers to Specify Signaling KineticsQ47680913
Conformational stability of the epidermal growth factor (EGF) receptor as influenced by glycosylation, dimerization and EGF hormone binding.Q48117891
Glycosylation as a Main Regulator of Growth and Death Factor Receptors SignalingQ49805726
The biology and management of non-small cell lung cancerQ49826396
Wild-type EGFR is stabilized by direct interaction with HSP90 in cancer cells and tumorsQ36200403
HER2 amplification: a potential mechanism of acquired resistance to EGFR inhibition in EGFR-mutant lung cancers that lack the second-site EGFRT790M mutationQ36322762
Heterogeneity in EGF-binding affinities arises from negative cooperativity in an aggregating systemQ36423352
The epidermal growth factor receptor pathway: a model for targeted therapyQ36603677
An Allosteric Cross-Talk Between the Activation Loop and the ATP Binding Site Regulates the Activation of Src KinaseQ36785393
Transitions to catalytically inactive conformations in EGFR kinaseQ36820157
Architecture and membrane interactions of the EGF receptorQ36923502
Effects of oncogenic mutations on the conformational free-energy landscape of EGFR kinaseQ36967631
Molecular basis for multimerization in the activation of the epidermal growth factor receptorQ36993693
Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitorsQ37057914
Origins of growth factors: NGF and EGF.Q37142765
Structure-based view of epidermal growth factor receptor regulationQ37197992
Using plasma membrane nanoclusters to build better signaling circuitsQ37213906
The epidermal growth factor receptor ligands at a glanceQ37324458
Characterization of Glycosylation Sites of the Epidermal Growth Factor ReceptorQ37396323
The genesis of tyrosine phosphorylationQ37718124
A systematic approach to protein glycosylation analysis: a path through the mazeQ37790268
Feedback regulation of EGFR signalling: decision making by early and delayed loops.Q37831109
The EGFR family: not so prototypical receptor tyrosine kinasesQ38201344
Investigating drug-target association and dissociation mechanisms using metadynamics-based algorithmsQ38286343
Synthesis of epidermal growth factor receptor in human A431 cells. Glycosylation-dependent acquisition of ligand binding activity occurs post-translationally in the endoplasmic reticulum.Q38350230
Analysis of the glycosylation patterns of the extracellular domain of the epidermal growth factor receptor expressed in Chinese hamster ovary fibroblastsQ38363065
Classification of small molecule protein kinase inhibitors based upon the structures of their drug-enzyme complexesQ38623447
Advances in free-energy-based simulations of protein folding and ligand binding.Q38698407
EGFR Dynamics Change during Activation in Native Membranes as Revealed by NMR.Q38731480
Role of N-glycosylation in EGFR ectodomain ligand bindingQ38795554
Changes in the free-energy landscape of p38α MAP kinase through its canonical activation and binding events as studied by enhanced molecular dynamics simulationsQ38818757
Inhibition of IGF1R signaling abrogates resistance to afatinib (BIBW2992) in EGFR T790M mutant lung cancer cellsQ38866417
Next-Generation EGFR Tyrosine Kinase Inhibitors for Treating EGFR-Mutant Lung Cancer beyond First LineQ39114552
Activation of the EGF Receptor by Ligand Binding and Oncogenic Mutations: The "Rotation Model".Q39346046
Irreversible inhibition of epidermal growth factor receptor activity by 3-aminopropanamides.Q39405800
Evidence for extended YFP-EGFR dimers in the absence of ligand on the surface of living cellsQ39468370
Ligand-independent dimer formation of epidermal growth factor receptor (EGFR) is a step separable from ligand-induced EGFR signalingQ39616171
Spatial control of EGF receptor activation by reversible dimerization on living cellsQ39731307
Activation of ER stress and inhibition of EGFR N-glycosylation by tunicamycin enhances susceptibility of human non-small cell lung cancer cells to erlotinibQ39897755
Dynamic conformational transitions of the EGF receptor in living mammalian cells determined by FRET and fluorescence lifetime imaging microscopyQ50847753
Ins and Outs of Kinase DFG MotifsQ50888279
Structural Stability and Flexibility Direct the Selection of Activating Mutations in Epidermal Growth Factor Receptor KinaseQ50959142
Free-energy landscape for beta hairpin folding from combined parallel tempering and metadynamicsQ51931397
Impact of EGFR point mutations on the sensitivity to gefitinib: insights from comparative structural analyses and molecular dynamics simulationsQ51934736
Therapeutic uses of HSP90 inhibitors in Non-Small Cell Lung Carcinoma (NSCLC).Q52665088
New developments in force fields for biomolecular simulations.Q52687239
The effect of a widespread cancer-causing mutation on the inactive to active dynamics of the B-Raf kinaseQ54278360
Conformational regulation of the EGFR kinase core by the juxtamembrane and C‐terminal tail: A molecular dynamics studyQ54644212
EGFR signaling patterns are regulated by its different ligands.Q55070997
Developing a molecular dynamics force field for both folded and disordered protein states.Q55310411
Monoclonal antibodies against EGFRvIII are tumor specific and react with breast and lung carcinomas and malignant gliomasQ55480632
Anatomy of a structural pathway for activation of the catalytic domain of Src kinase HckQ56770481
New advances in immunotherapy for non-small cell lung cancerQ56890070
Allosteric Modulators of HSP90 and HSP70: Dynamics Meets Function through Structure-Based Drug DesignQ57794187
The Different Flexibility of c-Src and c-Abl Kinases Regulates the Accessibility of a Druggable Inactive ConformationQ58465773
Protein Conformational Transitions: The Closure Mechanism of a Kinase Explored by Atomistic SimulationsQ58465787
The architecture of EGFR's basal complexes reveals autoinhibition mechanisms in dimers and oligomersQ58600328
Status of Agents Targeting the HGF/c-Met Axis in Lung CancerQ58726253
Prognostic and Therapeutic Implications of EGFR and KRAS Mutations in Resected Lung AdenocarcinomaQ59566032
Mechanism of Resistance to Epidermal Growth Factor Receptor-Tyrosine Kinase Inhibitors and a Potential Treatment StrategyQ59800637
Conformational landscape of the epidermal growth factor receptor kinase reveals a mutant specific allosteric pocketQ59828149
Characterization of the N-oligosaccharides attached to the atypical Asn-X-Cys sequence of recombinant human epidermal growth factor receptorQ73580767
The Asn-420-linked sugar chain in human epidermal growth factor receptor suppresses ligand-independent spontaneous oligomerization. Possible role of a specific sugar chain in controllable receptor activationQ73763333
Epidermal growth factor receptor tyrosine kinase inhibitorsQ80103312
Targeting tyrosine kinases in cancer: the second waveQ83854401
On the nature of low- and high-affinity EGF receptors on living cellsQ34595942
Oligomerization and nanocluster organization render specificityQ34681546
Endocytosis and intracellular trafficking of ErbBsQ34827744
Regulation of human EGF receptor by lipidsQ35021986
Solid-state NMR and membrane proteinsQ35214037
Catalytic control in the EGF receptor and its connection to general kinase regulatory mechanisms.Q35219426
N-Glycosylation as determinant of epidermal growth factor receptor conformation in membranesQ35378448
ErbB1 dimerization is promoted by domain co-confinement and stabilized by ligand bindingQ35534115
Rapid phospho-turnover by receptor tyrosine kinases impacts downstream signaling and drug bindingQ35568374
The Membrane-proximal Intracellular Domain of the Epidermal Growth Factor Receptor Underlies Negative Cooperativity in Ligand BindingQ35639911
A structural perspective on the regulation of the epidermal growth factor receptorQ35674768
Effect of sialylation on EGFR phosphorylation and resistance to tyrosine kinase inhibitionQ35699603
The tethered configuration of the EGF receptor extracellular domain exerts only a limited control of receptor functionQ35729931
Ligand regulation of a constitutively dimeric EGF receptorQ35733874
Activation pathway of Src kinase reveals intermediate states as targets for drug designQ35738216
The Effect of Mutations on Drug Sensitivity and Kinase Activity of Fibroblast Growth Factor Receptors: A Combined Experimental and Theoretical StudyQ35752926
Structural analysis of the EGFR/HER3 heterodimer reveals the molecular basis for activating HER3 mutationsQ35820920
Investigation of the dimerization of proteins from the epidermal growth factor receptor family by single wavelength fluorescence cross-correlation spectroscopyQ35850949
Oligomerization of the EGF receptor investigated by live cell fluorescence intensity distribution analysisQ35878699
Analysis of the Role of the C-Terminal Tail in the Regulation of the Epidermal Growth Factor ReceptorQ35917462
The ErbB receptors and their ligands in cancer: an overview.Q36108987
Demonstrating an Order-of-Magnitude Sampling Enhancement in Molecular Dynamics Simulations of Complex Protein SystemsQ87271292
Immune Checkpoint Inhibitors (ICIs) in Non-Small Cell Lung Cancer (NSCLC)Q89170235
Towards simple kinetic models of functional dynamics for a kinase subfamilyQ89486452
Small molecule inhibitors targeting the EGFR/ErbB family of protein-tyrosine kinases in human cancersQ89998161
Overcoming resistance in non-small-cell lung cancer: A practical lesson for the medicinal chemistQ90910643
Understanding the biology of HER3 receptor as a therapeutic target in human cancerQ90952252
Landscape of EGFR-Dependent and -Independent Resistance Mechanisms to Osimertinib and Continuation Therapy Beyond Progression in EGFR-Mutant NSCLCQ91517934
EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapyQ27824812
All-atom empirical potential for molecular modeling and dynamics studies of proteinsQ27860468
Signal transduction by receptors with tyrosine kinase activityQ27860624
Untangling the ErbB signalling networkQ27860884
The conformational plasticity of protein kinasesQ27860946
Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinibQ27861059
An open-and-shut case? Recent insights into the activation of EGF/ErbB receptorsQ28207289
A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cellsQ28282744
Dynamics of folded proteinsQ28287584
Membrane interaction of bound ligands contributes to the negative binding cooperativity of the EGF receptorQ28541111
Towards a Molecular Understanding of the Link between Imatinib Resistance and Kinase Conformational DynamicsQ28551159
Mig6 is a negative regulator of EGF receptor-mediated skin morphogenesis and tumor formationQ28590384
Erlotinib in previously treated non-small-cell lung cancerQ29547546
Global survey of phosphotyrosine signaling identifies oncogenic kinases in lung cancerQ29547564
Human epidermal growth factor receptor cDNA sequence and aberrant expression of the amplified gene in A431 epidermoid carcinoma cellsQ29616544
Precise nanometer localization analysis for individual fluorescent probesQ29617300
HSP90 and the chaperoning of cancerQ29617504
Locking the active conformation of c-Src kinase through the phosphorylation of the activation loopQ30009548
A tale of the epidermal growth factor receptor: The quest for structural resolution on cells.Q30380491
Revealing Higher Order Protein Structure Using Mass Spectrometry.Q30386904
EGFR oligomerization organizes kinase-active dimers into competent signalling platformsQ30827493
Computation of conformational coupling in allosteric proteinsQ30872872
Computational modeling of allosteric communication reveals organizing principles of mutation-induced signaling in ABL and EGFR kinasesQ31036423
Structure of caveolaeQ33224886
Activating and resistance mutations of EGFR in non-small-cell lung cancer: role in clinical response to EGFR tyrosine kinase inhibitorsQ33769838
Co-conserved features associated with cis regulation of ErbB tyrosine kinasesQ33778237
Sialylation and fucosylation of epidermal growth factor receptor suppress its dimerization and activation in lung cancer cellsQ33944231
Simultaneous visualization of the extracellular and cytoplasmic domains of the epidermal growth factor receptorQ33981031
Conformational Transition Pathways of Epidermal Growth Factor Receptor Kinase Domain from Multiple Molecular Dynamics Simulations and Bayesian ClusteringQ34045014
EGF receptor ligandsQ34185050
Autophosphorylation sites on the epidermal growth factor receptor.Q34245370
Efficacy of gefitinib, an inhibitor of the epidermal growth factor receptor tyrosine kinase, in symptomatic patients with non-small cell lung cancer: a randomized trialQ34271566
Higher-Order Assemblies in a New Paradigm of Signal TransductionQ34338941
Multi-institutional randomized phase II trial of gefitinib for previously treated patients with advanced non-small-cell lung cancer (The IDEAL 1 Trial) [corrected].Q34533636
P275copyright licenseCreative Commons Attribution 4.0 InternationalQ20007257
P6216copyright statuscopyrightedQ50423863
P433issue4
P577publication date2019-04-05
P1433published inCellsQ27724621
P1476titleStructure and Dynamics of the EGF Receptor as Revealed by Experiments and Simulations and Its Relevance to Non-Small Cell Lung Cancer
P478volume8

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Q92068202Epidermal Growth Factor Receptor and Its Role in Pancreatic Cancer Treatment Mediated by Nanoparticlescites workP2860

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