An Allosteric Mechanism for Activation of the Kinase Domain of Epidermal Growth Factor Receptor

Activating Mutations in the Epidermal Growth Factor Receptor Underlying Responsiveness of Non–Small-Cell Lung Cancer to Gefitinib

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EGFR Mutations in Lung Cancer: Correlation with Clinical Response to Gefitinib Therapy

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Untangling the ErbB signalling network

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EGF receptor gene mutations are common in lung cancers from “never smokers” and are associated with sensitivity of tumors to gefitinib and erlotinib

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Clinical and biological features associated with epidermal growth factor receptor gene mutations in lung cancers

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The Conformational Plasticity of Protein Kinases

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Gefitinib-Sensitizing EGFR Mutations in Lung Cancer Activate Anti-Apoptotic Pathways

Sordella, R., Bell, D. W., Haber, D. A., & Settleman, J. E. (2004) · Science · doi:10.1126/science.1101637 · Cited by 1,605

Structure of the Epidermal Growth Factor Receptor Kinase Domain Alone and in Complex with a 4-Anilinoquinazoline Inhibitor

Stamos, J. L., Sliwkowski, M. X., & Eigenbrot, C. W. (2002) · Journal of Biological Chemistry · doi:10.1074/jbc.m207135200 · Cited by 1,594

Mechanism of CDK activation revealed by the structure of a cyclinA-CDK2 complex

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Crystal Structure of the Complex of Human Epidermal Growth Factor and Receptor Extracellular Domains

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Identification of phosphotyrosine as a product of epidermal growth factor-activated protein kinase in A-431 cell membranes.

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A Unique Structure for Epidermal Growth Factor Receptor Bound to GW572016 (Lapatinib)

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Ligand-Induced, Receptor-Mediated Dimerization and Activation of EGF Receptor

Schlessinger, J. (2002) · Cell · doi:10.1016/s0092-8674(02)00966-2 · Cited by 995

Crystal structure of cyclin-dependent kinase 2

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An Open-and-Shut Case? Recent Insights into the Activation of EGF/ErbB Receptors

Burgess, A. W., Cho, H., Eigenbrot, C. W., Ferguson, K. M., Garrett, T., Leahy, D. J., Lemmon, M. A., Sliwkowski, M. X., Ward, C. W., & Yokoyama, S. (2003) · Molecular Cell · doi:10.1016/s1097-2765(03)00350-2 · Cited by 936

Crystal Structures of c-Src Reveal Features of Its Autoinhibitory Mechanism

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EGF Activates Its Receptor by Removing Interactions that Autoinhibit Ectodomain Dimerization

Ferguson, K. M., Berger, M. B., Mendrola, J. M., Cho, H., Leahy, D. J., & Lemmon, M. A. (2003) · Molecular Cell · doi:10.1016/s1097-2765(03)00047-9 · Cited by 801

Crystal Structure of a Truncated Epidermal Growth Factor Receptor Extracellular Domain Bound to Transforming Growth Factor α

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Somatic mutations of epidermal growth factor receptor signaling pathway in lung cancers

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Self-phosphorylation of epidermal growth factor receptor: evidence for a model of intermolecular allosteric activation

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Structure of the Extracellular Region of HER3 Reveals an Interdomain Tether

Cho, H., & Leahy, D. J. (2002) · Science · doi:10.1126/science.1074611 · Cited by 447

Crystal Structure of Hck in Complex with a Src Family–Selective Tyrosine Kinase Inhibitor

Schindler, T. H., Sicheri, F., Pico, A. R., Gazit, A., Levitzki, A., & Kuriyan, J. (1999) · Molecular Cell · doi:10.1016/s1097-2765(00)80357-3 · Cited by 433

Activation of preformed EGF receptor dimers by ligand-induced rotation of the transmembrane domain11Edited by B. Holland

Moriki, T., Maruyama, H., & MARUYAMA, I. N. (2001) · Journal of Molecular Biology · doi:10.1006/jmbi.2001.4923 · Cited by 350

Biological role of epidermal growth factor-receptor clustering. Investigation with monoclonal anti-receptor antibodies.

Schreiber, A. B., Libermann, T. A., Lax, I., Yarden, Y., & Schlessinger, J. (1983) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(18)33127-2 · Cited by 328

A Src-Like Inactive Conformation in the Abl Tyrosine Kinase Domain

Levinson, N. M., Kuchment, O., Shen, K., Young, M. A., Koldobskiy, M. A., Karplus, M., Cole, P. A., & Kuriyan, J. (2006) · PLoS Biology · doi:10.1371/journal.pbio.0040144 · Cited by 312

A Dominant Negative Mutation Suppresses the Function of Normal Epidermal Growth Factor Receptors by Heterodimerization

Kashles, O., Yarden, Y., Fischer, R., Ullrich, A., & Schlessinger, J. (1991) · Molecular and Cellular Biology · doi:10.1128/mcb.11.3.1454 · Cited by 230

Mechanism-based design of a protein kinase inhibitor.

Hubbard, S. R., Cole, P. A., Parang, K., Till, J. H., Ablooglu, A. J., & Kohanski, R. A. (2001) · Nature Structural Biology · doi:10.1038/83028 · Cited by 192

Characterization of pp60c-src Tyrosine Kinase Activities Using a Continuous Assay: Autoactivation of the Enzyme Is an Intermolecular Autophosphorylation Process

Barker, S. C., Kassel, D. B., Weigl, D., Huang, X., Luther, M., & Knight, W. B. (1995) · Biochemistry · doi:10.1021/bi00045a027 · Cited by 190

Epidermal Growth Factor–Independent Transformation of Ba/F3 Cells with Cancer-Derived Epidermal Growth Factor Receptor Mutants Induces Gefitinib-Sensitive Cell Cycle Progression

Jiang, J., Greulich, H. E., Janne, P. A., Sellers, W. R., Meyerson, M. M., & Griffin, J. D. (2005) · Cancer Research · doi:10.1158/0008-5472.can-05-1829 · Cited by 188

An Electrostatic Engine Model for Autoinhibition and Activation of the Epidermal Growth Factor Receptor (EGFR/ErbB) Family

McLaughlin, S., Smith, S. O., Hayman, M. J., & Murray, D. (2005) · The Journal of General Physiology · doi:10.1085/jgp.200509274 · Cited by 135

A highly conserved tyrosine residue at codon 845 within the kinase domain is not required for the transforming activity of human epidermal growth factor receptor

Gotoh, N., Tojo, A., Hino, M., Yazaki, Y., & Shibuya, M. (1992) · Biochemical and Biophysical Research Communications · doi:10.1016/0006-291x(92)90812-y · Cited by 126

Molecular Recognition of Histidine-Tagged Molecules by Metal-Chelating Lipids Monitored by Fluorescence Energy Transfer and Correlation Spectroscopy

Dorn, I. T., Neumaier, K. R., & Tampé, R. (1998) · Journal of the American Chemical Society · doi:10.1021/ja9735620 · Cited by 110

Activation of Neu (ErbB-2) Mediated by Disulfide Bond-Induced Dimerization Reveals a Receptor Tyrosine Kinase Dimer Interface

Burke, C., & Stern, D. F. (1998) · Molecular and Cellular Biology · doi:10.1128/mcb.18.9.5371 · Cited by 103

Activation of the Purified Protein Tyrosine Kinase Domain of the Epidermal Growth Factor Receptor

Wedegaertner, P., & Gill, G. N. (1989) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(18)60470-3 · Cited by 92

Template-Directed Assembly of Receptor Signaling Complexes

Shrout, A. L., Montefusco, D. J., & Weis, R. M. (2003) · Biochemistry · doi:10.1021/bi0352769 · Cited by 73

A Putative Mechanism for Downregulation of the Catalytic Activity of the EGF Receptor via Direct Contact between Its Kinase and C-Terminal Domains

Landau, M., Fleishman, S. J., & Ben‐Tal, N. (2004) · Structure · doi:10.1016/j.str.2004.10.006 · Cited by 70

Epidermal Growth Factor (EGF) Receptor Kinase-independent Signaling by EGF

Deb, T. B., Su, L., Wong, L., Bonvini, E., Wells, A. H., David, M., & Johnson, G. R. (2001) · Journal of Biological Chemistry · doi:10.1074/jbc.m100928200 · Cited by 61

Aggregation-induced activation of the epidermal growth factor receptor protein tyrosine kinase

Mohammadi, M., Honegger, A., Sorokin, A., Ullrich, A., Schlessinger, J., & Hurwitz, D. R. (1993) · Biochemistry · doi:10.1021/bi00085a004 · Cited by 54

A Model for the Activation of the Epidermal Growth Factor Receptor Kinase: Involvement of an Asymmetric Dimer?

Groenen, L. C., Walker, F., Burgess, A. W., & Treutlein, H. R. (1997) · Biochemistry · doi:10.1021/bi9614141 · Cited by 35

Phosphorylation of Tyrosine 992, 1068, and 1086 Is Required for Conformational Change of the Human Epidermal Growth Factor Receptor C-Terminal Tail

Bishayee, A., Beguinot, L., & Bishayee, S. (1999) · Molecular Biology of the Cell · doi:10.1091/mbc.10.3.525 · Cited by 35

A minor tyrosine phosphorylation site located within the CAIN domain plays a critical role in regulating tissue-specific transformation by erbB kinase

Chang, C. M., Shu, H. G., Ravi, L., Pelley, R. J., Shu, H., & Kung, H. J. (1995) · Journal of Virology · doi:10.1128/jvi.69.2.1172-1180.1995 · Cited by 14

Cell Signaling by Receptor Tyrosine Kinases

Lemmon, M. A., & Schlessinger, J. (2010) · Cell · doi:10.1016/j.cell.2010.06.011 · Cited by 7,929

The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP

Yun, C.-H., Mengwasser, K. E., Toms, A. V., Woo, M. S., Greulich, H., Wong, K.-K., Meyerson, M., & Eck, M. J. (2008) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0709662105 · Cited by 2,118

Epidermal Growth Factor Receptor Cell Proliferation Signaling Pathways

Wee, P., & Wang, Z. (2017) · Cancers · doi:10.3390/cancers9050052 · Cited by 2,027

HSP90 at the hub of protein homeostasis: emerging mechanistic insights

Taipale, M., Jarosz, D. F., & Lindquist, S. (2010) · Nature Reviews Molecular Cell Biology · doi:10.1038/nrm2918 · Cited by 1,818

Emerging functions of the EGFR in cancer

Sigismund, S., Avanzato, D., & Lanzetti, L. (2017) · Molecular Oncology · doi:10.1002/1878-0261.12155 · Cited by 1,552

Research Highlights

(2006) · Nature Structural & Molecular Biology · doi:10.1038/nsmb0706-575

Studies of the Allosteric Activation of the Epidermal Growth Factor Receptor

Engel, K. A. (2013) · eScholarship (California Digital Library)

Emerging Allosteric Mechanism of EGFR Activation in Physiological and Pathological Contexts

Tsai, C., & Nussinov, R. (2019) · Biophysical Journal · doi:10.1016/j.bpj.2019.05.021 · Cited by 48

EGF Receptor Activation: Push Comes to Shove

Hubbard, S. R. (2006) · Cell · doi:10.1016/j.cell.2006.05.028 · Cited by 28

Activation Mechanism of Solubilized Epidermal Growth Factor Receptor Tyrosine Kinase

Ge, G., Wu, J., Wang, Y., & Lin, Q. (2002) · Biochemical and Biophysical Research Communications · doi:10.1006/bbrc.2001.6285 · Cited by 12