1nql › Citations

EGF activates its receptor by removing interactions that autoinhibit ectodomain dimerization.

Ferguson KM, Berger MB, Mendrola JM, Cho HS, Leahy DJ, Lemmon MA
Mol Cell 11 507-17 (2003)
Cited: 450 times
EuropePMC logo PMID: 12620237

Abstract

Epidermal growth factor (EGF) receptor is the prototype of the ErbB (HER) family receptor tyrosine kinases (RTKs), which regulate cell growth and differentiation and are implicated in many human cancers. EGF activates its receptor by inducing dimerization of the 621 amino acid EGF receptor extracellular region. We describe the 2.8 A resolution crystal structure of this entire extracellular region (sEGFR) in an unactivated state. The structure reveals an autoinhibited configuration, where the dimerization interface recently identified in activated sEGFR structures is completely occluded by intramolecular interactions. To activate the receptor, EGF binding must promote a large domain rearrangement that exposes this dimerization interface. This contrasts starkly with other RTK activation mechanisms and suggests new approaches for designing ErbB receptor antagonists.

Reviews - 1nql mentioned but not cited (16)

  1. Receptor tyrosine kinases: mechanisms of activation and signaling. Hubbard SR, Miller WT. Curr Opin Cell Biol 19 117-123 (2007)
  2. Yeast surface display for protein engineering and characterization. Gai SA, Wittrup KD. Curr Opin Struct Biol 17 467-473 (2007)
  3. Structure-based view of epidermal growth factor receptor regulation. Ferguson KM. Annu Rev Biophys 37 353-373 (2008)
  4. A structural perspective on the regulation of the epidermal growth factor receptor. Kovacs E, Zorn JA, Huang Y, Barros T, Kuriyan J. Annu Rev Biochem 84 739-764 (2015)
  5. Peptide and protein nanoparticle conjugates: versatile platforms for biomedical applications. Spicer CD, Jumeaux C, Gupta B, Stevens MM. Chem Soc Rev 47 3574-3620 (2018)
  6. Transmembrane helix-helix interactions involved in ErbB receptor signaling. Cymer F, Schneider D. Cell Adh Migr 4 299-312 (2010)
  7. Molecular Targeting of Epidermal Growth Factor Receptor (EGFR) and Vascular Endothelial Growth Factor Receptor (VEGFR). Kaufman NEM, Dhingra S, Jois SD, Vicente MDGH. Molecules 26 1076 (2021)
  8. Insulin and epidermal growth factor receptor family members share parallel activation mechanisms. Ferguson KM, Hu C, Lemmon MA. Protein Sci 29 1331-1344 (2020)
  9. Structure and Dynamics of the EGF Receptor as Revealed by Experiments and Simulations and Its Relevance to Non-Small Cell Lung Cancer. Martin-Fernandez ML, Clarke DT, Roberts SK, Zanetti-Domingues LC, Gervasio FL. Cells 8 E316 (2019)
  10. More than the sum of the parts: Toward full-length receptor tyrosine kinase structures. Diwanji D, Thaker T, Jura N. IUBMB Life 71 706-720 (2019)
  11. Piecing it together: Unraveling the elusive structure-function relationship in single-pass membrane receptors. Valley CC, Lewis AK, Sachs JN. Biochim Biophys Acta Biomembr 1859 1398-1416 (2017)
  12. Homo- and Heterodimerization of Proteins in Cell Signaling: Inhibition and Drug Design. Singh SS, Jois SD. Adv Protein Chem Struct Biol 111 1-59 (2018)
  13. Structural Perspectives on Extracellular Recognition and Conformational Changes of Several Type-I Transmembrane Receptors. Chataigner LMP, Leloup N, Janssen BJC. Front Mol Biosci 7 129 (2020)
  14. Targeting Intramembrane Protein-Protein Interactions: Novel Therapeutic Strategy of Millions Years Old. Sigalov AB. Adv Protein Chem Struct Biol 111 61-99 (2018)
  15. Cryo-electron Microscopic Analysis of Single-Pass Transmembrane Receptors. Cai K, Zhang X, Bai XC. Chem Rev 122 13952-13988 (2022)
  16. EGFR trafficking: effect of dimerization, dynamics, and mutation. Schultz DF, Billadeau DD, Jois SD. Front Oncol 13 1258371 (2023)

Articles - 1nql mentioned but not cited (63)

  1. Mechanism for activation of the EGF receptor catalytic domain by the juxtamembrane segment. Jura N, Endres NF, Engel K, Deindl S, Das R, Lamers MH, Wemmer DE, Zhang X, Kuriyan J. Cell 137 1293-1307 (2009)
  2. Architecture and membrane interactions of the EGF receptor. Arkhipov A, Shan Y, Das R, Endres NF, Eastwood MP, Wemmer DE, Kuriyan J, Shaw DE. Cell 152 557-569 (2013)
  3. Structural evidence for loose linkage between ligand binding and kinase activation in the epidermal growth factor receptor. Lu C, Mi LZ, Grey MJ, Zhu J, Graef E, Yokoyama S, Springer TA. Mol Cell Biol 30 5432-5443 (2010)
  4. Phenobarbital indirectly activates the constitutive active androstane receptor (CAR) by inhibition of epidermal growth factor receptor signaling. Mutoh S, Sobhany M, Moore R, Perera L, Pedersen L, Sueyoshi T, Negishi M. Sci Signal 6 ra31 (2013)
  5. Structural evaluation of EGFR inhibition mechanisms for nanobodies/VHH domains. Schmitz KR, Bagchi A, Roovers RC, van Bergen en Henegouwen PM, Ferguson KM. Structure 21 1214-1224 (2013)
  6. Matuzumab binding to EGFR prevents the conformational rearrangement required for dimerization. Schmiedel J, Blaukat A, Li S, Knöchel T, Ferguson KM. Cancer Cell 13 365-373 (2008)
  7. Combination antibody treatment down-regulates epidermal growth factor receptor by inhibiting endosomal recycling. Spangler JB, Neil JR, Abramovitch S, Yarden Y, White FM, Lauffenburger DA, Wittrup KD. Proc Natl Acad Sci U S A 107 13252-13257 (2010)
  8. N-Glycosylation as determinant of epidermal growth factor receptor conformation in membranes. Kaszuba K, Grzybek M, Orłowski A, Danne R, Róg T, Simons K, Coskun Ü, Vattulainen I. Proc Natl Acad Sci U S A 112 4334-4339 (2015)
  9. PRMT1-mediated methylation of the EGF receptor regulates signaling and cetuximab response. Liao HW, Hsu JM, Xia W, Wang HL, Wang YN, Chang WC, Arold ST, Chou CK, Tsou PH, Yamaguchi H, Fang YF, Lee HJ, Lee HH, Tai SK, Yang MH, Morelli MP, Sen M, Ladbury JE, Chen CH, Grandis JR, Kopetz S, Hung MC. J Clin Invest 125 4529-4543 (2015)
  10. The tethered configuration of the EGF receptor extracellular domain exerts only a limited control of receptor function. Mattoon D, Klein P, Lemmon MA, Lax I, Schlessinger J. Proc Natl Acad Sci U S A 101 923-928 (2004)
  11. Single-molecule imaging and fluorescence lifetime imaging microscopy show different structures for high- and low-affinity epidermal growth factor receptors in A431 cells. Webb SE, Roberts SK, Needham SR, Tynan CJ, Rolfe DJ, Winn MD, Clarke DT, Barraclough R, Martin-Fernandez ML. Biophys J 94 803-819 (2008)
  12. Complex relationship between ligand binding and dimerization in the epidermal growth factor receptor. Bessman NJ, Bagchi A, Ferguson KM, Lemmon MA. Cell Rep 9 1306-1317 (2014)
  13. Phthalocyanine-peptide conjugates for epidermal growth factor receptor targeting. Ongarora BG, Fontenot KR, Hu X, Sehgal I, Satyanarayana-Jois SD, Vicente MG. J Med Chem 55 3725-3738 (2012)
  14. The architecture of EGFR's basal complexes reveals autoinhibition mechanisms in dimers and oligomers. Zanetti-Domingues LC, Korovesis D, Needham SR, Tynan CJ, Sagawa S, Roberts SK, Kuzmanic A, Ortiz-Zapater E, Jain P, Roovers RC, Lajevardipour A, van Bergen En Henegouwen PMP, Santis G, Clayton AHA, Clarke DT, Gervasio FL, Shan Y, Shaw DE, Rolfe DJ, Parker PJ, Martin-Fernandez ML. Nat Commun 9 4325 (2018)
  15. Her2 activation mechanism reflects evolutionary preservation of asymmetric ectodomain dimers in the human EGFR family. Arkhipov A, Shan Y, Kim ET, Dror RO, Shaw DE. Elife 2 e00708 (2013)
  16. Protein domain-level landscape of cancer-type-specific somatic mutations. Yang F, Petsalaki E, Rolland T, Hill DE, Vidal M, Roth FP. PLoS Comput Biol 11 e1004147 (2015)
  17. A conformationally constrained peptidomimetic binds to the extracellular region of HER2 protein. Banappagari S, Ronald S, Satyanarayanajois SD. J Biomol Struct Dyn 28 289-308 (2010)
  18. Epidermal growth factor receptor mutation mediates cross-resistance to panitumumab and cetuximab in gastrointestinal cancer. Braig F, März M, Schieferdecker A, Schulte A, Voigt M, Stein A, Grob T, Alawi M, Indenbirken D, Kriegs M, Engel E, Vanhoefer U, Grundhoff A, Loges S, Riecken K, Fehse B, Bokemeyer C, Binder M. Oncotarget 6 12035-12047 (2015)
  19. Molecular determinants of epidermal growth factor binding: a molecular dynamics study. Sanders JM, Wampole ME, Thakur ML, Wickstrom E. PLoS One 8 e54136 (2013)
  20. The antibody zalutumumab inhibits epidermal growth factor receptor signaling by limiting intra- and intermolecular flexibility. Lammerts van Bueren JJ, Bleeker WK, Brännström A, von Euler A, Jansson M, Peipp M, Schneider-Merck T, Valerius T, van de Winkel JG, Parren PW. Proc Natl Acad Sci U S A 105 6109-6114 (2008)
  21. Differential binding patterns of monoclonal antibody 2C4 to the ErbB3-p185her2/neu and the EGFR-p185her2/neu complexes. Cai Z, Zhang G, Zhou Z, Bembas K, Drebin JA, Greene MI, Zhang H. Oncogene 27 3870-3874 (2008)
  22. Human epidermal growth factor receptor (EGFR) aligned on the plasma membrane adopts key features of Drosophila EGFR asymmetry. Tynan CJ, Roberts SK, Rolfe DJ, Clarke DT, Loeffler HH, Kästner J, Winn MD, Parker PJ, Martin-Fernandez ML. Mol Cell Biol 31 2241-2252 (2011)
  23. Oncogenic mutations at the EGFR ectodomain structurally converge to remove a steric hindrance on a kinase-coupled cryptic epitope. Orellana L, Thorne AH, Lema R, Gustavsson J, Parisian AD, Hospital A, Cordeiro TN, Bernadó P, Scott AM, Brun-Heath I, Lindahl E, Cavenee WK, Furnari FB, Orozco M. Proc Natl Acad Sci U S A 116 10009-10018 (2019)
  24. Epidermal Growth Factor Receptor Signaling Disruption by Endocrine and Metabolic Disrupting Chemicals. Hardesty JE, Al-Eryani L, Wahlang B, Falkner KC, Shi H, Jin J, Vivace BJ, Ceresa BP, Prough RA, Cave MC. Toxicol Sci 162 622-634 (2018)
  25. The free energy landscape in translational science: how can somatic mutations result in constitutive oncogenic activation? Tsai CJ, Nussinov R. Phys Chem Chem Phys 16 6332-6341 (2014)
  26. Protein-bound uremic toxins induce tissue remodeling by targeting the EGF receptor. Sun CY, Young GH, Hsieh YT, Chen YH, Wu MS, Wu VC, Lee JH, Lee CC. J Am Soc Nephrol 26 281-290 (2015)
  27. Antibodies Targeting Closely Adjacent or Minimally Overlapping Epitopes Can Displace One Another. Abdiche YN, Yeung AY, Ni I, Stone D, Miles A, Morishige W, Rossi A, Strop P. PLoS One 12 e0169535 (2017)
  28. Epidermal growth factor receptor downregulation by small heterodimeric binding proteins. Hackel BJ, Neil JR, White FM, Wittrup KD. Protein Eng Des Sel 25 47-57 (2012)
  29. A molecular mechanism for the generation of ligand-dependent differential outputs by the epidermal growth factor receptor. Huang Y, Ognjenovic J, Karandur D, Miller K, Merk A, Subramaniam S, Kuriyan J. Elife 10 e73218 (2021)
  30. Geometry and expression enhance enrichment of functional yeast-displayed ligands via cell panning. Stern LA, Schrack IA, Johnson SM, Deshpande A, Bennett NR, Harasymiw LA, Gardner MK, Hackel BJ. Biotechnol Bioeng 113 2328-2341 (2016)
  31. Inhibiting EGFR dimerization using triazolyl-bridged dimerization arm mimics. Hanold LE, Oruganty K, Ton NT, Beedle AM, Kannan N, Kennedy EJ. PLoS One 10 e0118796 (2015)
  32. Synthesis of BODIPY-Peptide Conjugates for Fluorescence Labeling of EGFR Overexpressing Cells. Zhao N, Williams TM, Zhou Z, Fronczek FR, Sibrian-Vazquez M, Jois SD, Vicente MGH. Bioconjug Chem 28 1566-1579 (2017)
  33. The tethering arm of the EGF receptor is required for negative cooperativity and signal transduction. Adak S, DeAndrade D, Pike LJ. J Biol Chem 286 1545-1555 (2011)
  34. The epidermal growth factor receptor (EGFR)-S442F mutant displays increased affinity for neuregulin-2beta and agonist-independent coupling with downstream signalling events. Gilmore JL, Gallo RM, Riese DJ. Biochem J 396 79-88 (2006)
  35. Determination of the glycoprotein specificity of lectins on cell membranes through oxidative proteomics. Xie Y, Sheng Y, Li Q, Ju S, Reyes J, Lebrilla CB. Chem Sci 11 9501-9512 (2020)
  36. Glioblastoma mutations alter EGFR dimer structure to prevent ligand bias. Hu C, Leche CA, Kiyatkin A, Yu Z, Stayrook SE, Ferguson KM, Lemmon MA. Nature 602 518-522 (2022)
  37. Synthesis, Characterization, and Evaluation of Near-IR Boron Dipyrromethene Bioconjugates for Labeling of Adenocarcinomas by Selectively Targeting the Epidermal Growth Factor Receptor. Kaufman NEM, Meng Q, Griffin KE, Singh SS, Dahal A, Zhou Z, Fronczek FR, Mathis JM, Jois SD, Vicente MGH. J Med Chem 62 3323-3335 (2019)
  38. Targeting of the epidermal growth factor receptor with mesoporphyrin IX-peptide conjugates. Fontenot KR, Ongarora BG, LeBlanc LE, Zhou Z, Jois SD, Vicente MG. J Porphyr Phthalocyanines 20 352-366 (2016)
  39. Unraveling the differential impact of PAHs and dioxin-like compounds on AKR1C3 reveals the EGFR extracellular domain as a critical determinant of the AHR response. Vogeley C, Sondermann NC, Woeste S, Momin AA, Gilardino V, Hartung F, Heinen M, Maaß SK, Mescher M, Pollet M, Rolfes KM, Vogel CFA, Rossi A, Lang D, Arold ST, Nakamura M, Haarmann-Stemmann T. Environ Int 158 106989 (2022)
  40. Phosphorylation-Dependent Conformations of the Disordered Carboxyl-Terminus Domain in the Epidermal Growth Factor Receptor. Regmi R, Srinivasan S, Latham AP, Kukshal V, Cui W, Zhang B, Bose R, Schlau-Cohen GS. J Phys Chem Lett 11 10037-10044 (2020)
  41. A bioinformatics investigation into the pharmacological mechanisms of the effect of the Yinchenhao decoction on hepatitis C based on network pharmacology. Zhang J, Liu X, Wu J, Zhou W, Tian J, Guo S, Jia SS, Meng Z, Ni M. BMC Complement Med Ther 20 50 (2020)
  42. Ligand binding and dynamics of the monomeric epidermal growth factor receptor ectodomain. Loeffler HH, Winn MD. Proteins 81 1931-1943 (2013)
  43. Peptide ligands for targeting the extracellular domain of EGFR: Comparison between linear and cyclic peptides. Williams TM, Sable R, Singh S, Vicente MGH, Jois SD. Chem Biol Drug Des 91 605-619 (2018)
  44. A reinforced merging methodology for mapping unique peptide motifs in members of protein families. Chang HT, Pai TW, Fan TC, Su BH, Wu PC, Tang CY, Chang CT, Liu SH, Chang MD. BMC Bioinformatics 7 38 (2006)
  45. ALCAM-EGFR interaction regulates myelomagenesis. Luo H, Zhang D, Wang F, Wang Q, Wu Y, Gou M, Hu Y, Zhang W, Huang J, Gong Y, Pan L, Li T, Zhao P, Zhang D, Qu Y, Liu Z, Jiang T, Dai Y, Guo T, Zhu J, Ye L, Zhang L, Liu W, Yi Q, Zheng Y. Blood Adv 5 5269-5282 (2021)
  46. Anti-EGFR antibody 528 binds to domain III of EGFR at a site shifted from the cetuximab epitope. Makabe K, Yokoyama T, Uehara S, Uchikubo-Kamo T, Shirouzu M, Kimura K, Tsumoto K, Asano R, Tanaka Y, Kumagai I. Sci Rep 11 5790 (2021)
  47. How to choose templates for modeling of protein complexes: Insights from benchmarking template-based docking. Chakravarty D, McElfresh GW, Kundrotas PJ, Vakser IA. Proteins 88 1070-1081 (2020)
  48. Ligand-induced transmembrane conformational coupling in monomeric EGFR. Srinivasan S, Regmi R, Lin X, Dreyer CA, Chen X, Quinn SD, He W, Coleman MA, Carraway KL, Zhang B, Schlau-Cohen GS. Nat Commun 13 3709 (2022)
  49. A generalizable nanopore sensor for highly specific protein detection at single-molecule precision. Ahmad M, Ha JH, Mayse LA, Presti MF, Wolfe AJ, Moody KJ, Loh SN, Movileanu L. Nat Commun 14 1374 (2023)
  50. Cells diversify transmembrane signaling through the controlled chaos of protein disorder. Sigalov AB. Self Nonself 2 75-79 (2011)
  51. Computer-guided binding mode identification and affinity improvement of an LRR protein binder without structure determination. Choi Y, Jeong S, Choi JM, Ndong C, Griswold KE, Bailey-Kellogg C, Kim HS. PLoS Comput Biol 16 e1008150 (2020)
  52. Poly-Lysine Dendritic Nanocarrier to Target Epidermal Growth Factor Receptor Overexpressed Breast Cancer for Methotrexate Delivery. Narayanan P, Anitha AK, Ajayakumar N, Kumar KS. Materials (Basel) 15 800 (2022)
  53. Targeting EGFR Overexpression at the Surface of Colorectal Cancer Cells by Exploiting Amidated BODIPY-Peptide Conjugates. Williams TM, Zhou Z, Singh SS, Sibrian-Vazquez M, Jois SD, Henriques Vicente MDG. Photochem Photobiol 96 581-595 (2020)
  54. A systematic study of traditional Chinese medicine treating hepatitis B virus-related hepatocellular carcinoma based on target-driven reverse network pharmacology. Yin X, Li J, Hao Z, Ding R, Qiao Y. Front Cell Infect Microbiol 12 964469 (2022)
  55. A toolkit for recombinant production of seven human EGF family growth factors in active conformation. Ferreira AS, Lopacinski A, Batista M, Hiraiwa PM, Guimarães BG, Zanchin NIT. Sci Rep 12 5034 (2022)
  56. Amivantamab and Mobocertinib in Exon 20 insertions EGFR Mutant Lung Cancer, Challenge To The Current Guidelines. Olivier T, Prasad V. Transl Oncol 23 101475 (2022)
  57. Biodistribution and Activity of EGFR Targeted Polymeric Micelles Delivering a New Inhibitor of DNA Repair to Orthotopic Colorectal Cancer Xenografts with Metastasis. de Paiva IM, Vakili MR, Soleimani AH, Tabatabaei Dakhili SA, Munira S, Paladino M, Martin G, Jirik FR, Hall DG, Weinfeld M, Lavasanifar A. Mol Pharm 19 1825-1838 (2022)
  58. Discrete Coiled Coil Rotamers Form within the EGFRvIII Juxtamembrane Domain. Mozumdar D, Doerner A, Zhang JY, Rafizadeh DN, Schepartz A. Biochemistry 59 3965-3972 (2020)
  59. Nanoscape, a data-driven 3D real-time interactive virtual cell environment. Kadir SR, Lilja A, Gunn N, Strong C, Hughes RT, Bailey BJ, Rae J, Parton RG, McGhee J. Elife 10 e64047 (2021)
  60. Allosteric activation of preformed EGF receptor dimers by a single ligand binding event. Purba ER, Saita EI, Akhouri RR, Öfverstedt LG, Wilken G, Skoglund U, Maruyama IN. Front Endocrinol (Lausanne) 13 1042787 (2022)
  61. CARDIO-PRED: an in silico tool for predicting cardiovascular-disorder associated proteins. Jain P, Thukral N, Gahlot LK, Hasija Y. Syst Synth Biol 9 55-66 (2015)
  62. Genetic variants of the EGFR ligand-binding domain and their association with structural alterations in Arab cancer patients. Marzouq M, Nairouz A, Ben Khalaf N, Bourguiba-Hachemi S, Quaddorah R, Ashoor D, Fathallah MD. BMC Res Notes 14 146 (2021)
  63. Network Pharmacology-Based Strategy to Investigate Pharmacological Mechanisms of the Drug Pair Astragalus-Angelica for Treatment of Male Infertility. Zhao F, Deng Y, Du G, Liu S, Guo J, Wang H, Chen Y, Wang F, Geng Q. Evid Based Complement Alternat Med 2021 8281506 (2021)


Reviews citing this publication (106)

  1. Cell signaling by receptor tyrosine kinases. Lemmon MA, Schlessinger J. Cell 141 1117-1134 (2010)
  2. ERBB receptors and cancer: the complexity of targeted inhibitors. Hynes NE, Lane HA. Nat Rev Cancer 5 341-354 (2005)
  3. Epidermal growth factor receptor (EGFR) signaling in cancer. Normanno N, De Luca A, Bianco C, Strizzi L, Mancino M, Maiello MR, Carotenuto A, De Feo G, Caponigro F, Salomon DS. Gene 366 2-16 (2006)
  4. ADAMs: key components in EGFR signalling and development. Blobel CP. Nat Rev Mol Cell Biol 6 32-43 (2005)
  5. Novel anticancer targets: revisiting ERBB2 and discovering ERBB3. Baselga J, Swain SM. Nat Rev Cancer 9 463-475 (2009)
  6. The ErbB/HER family of protein-tyrosine kinases and cancer. Roskoski R. Pharmacol Res 79 34-74 (2014)
  7. An open-and-shut case? Recent insights into the activation of EGF/ErbB receptors. Burgess AW, Cho HS, Eigenbrot C, Ferguson KM, Garrett TP, Leahy DJ, Lemmon MA, Sliwkowski MX, Ward CW, Yokoyama S. Mol Cell 12 541-552 (2003)
  8. Epidermal Growth Factor Receptor Cell Proliferation Signaling Pathways. Wee P, Wang Z. Cancers (Basel) 9 E52 (2017)
  9. The ERBB network: at last, cancer therapy meets systems biology. Yarden Y, Pines G. Nat Rev Cancer 12 553-563 (2012)
  10. Targeting the EGFR signaling pathway in cancer therapy. Seshacharyulu P, Ponnusamy MP, Haridas D, Jain M, Ganti AK, Batra SK. Expert Opin Ther Targets 16 15-31 (2012)
  11. ErbB receptors: directing key signaling networks throughout life. Holbro T, Hynes NE. Annu Rev Pharmacol Toxicol 44 195-217 (2004)
  12. Molecular mechanisms of steroid hormone signaling in plants. Vert G, Nemhauser JL, Geldner N, Hong F, Chory J. Annu Rev Cell Dev Biol 21 177-201 (2005)
  13. The emerging treatment landscape of targeted therapy in non-small-cell lung cancer. Yuan M, Huang LL, Chen JH, Wu J, Xu Q. Signal Transduct Target Ther 4 61 (2019)
  14. The ErbB/HER receptor protein-tyrosine kinases and cancer. Roskoski R. Biochem Biophys Res Commun 319 1-11 (2004)
  15. The EGFR family: not so prototypical receptor tyrosine kinases. Lemmon MA, Schlessinger J, Ferguson KM. Cold Spring Harb Perspect Biol 6 a020768 (2014)
  16. Epidermal growth factor receptor targeting in cancer: a review of trends and strategies. Yewale C, Baradia D, Vhora I, Patil S, Misra A. Biomaterials 34 8690-8707 (2013)
  17. International Union of Basic and Clinical Pharmacology. LXVII. Recommendations for the recognition and nomenclature of G protein-coupled receptor heteromultimers. Pin JP, Neubig R, Bouvier M, Devi L, Filizola M, Javitch JA, Lohse MJ, Milligan G, Palczewski K, Parmentier M, Spedding M. Pharmacol Rev 59 5-13 (2007)
  18. Small-molecule modulation of neurotrophin receptors: a strategy for the treatment of neurological disease. Longo FM, Massa SM. Nat Rev Drug Discov 12 507-525 (2013)
  19. EGFR family: structure physiology signalling and therapeutic targets. Burgess AW. Growth Factors 26 263-274 (2008)
  20. Form and function of developing heart valves: coordination by extracellular matrix and growth factor signaling. Schroeder JA, Jackson LF, Lee DC, Camenisch TD. J Mol Med (Berl) 81 392-403 (2003)
  21. Role of receptor tyrosine kinase transmembrane domains in cell signaling and human pathologies. Li E, Hristova K. Biochemistry 45 6241-6251 (2006)
  22. Endocytic downregulation of ErbB receptors: mechanisms and relevance in cancer. Roepstorff K, Grøvdal L, Grandal M, Lerdrup M, van Deurs B. Histochem Cell Biol 129 563-578 (2008)
  23. Ligand-induced ErbB receptor dimerization. Lemmon MA. Exp Cell Res 315 638-648 (2009)
  24. ABCG2: structure, function and role in drug response. Polgar O, Robey RW, Bates SE. Expert Opin Drug Metab Toxicol 4 1-15 (2008)
  25. Molecular predictors of response to trastuzumab and lapatinib in breast cancer. Esteva FJ, Yu D, Hung MC, Hortobagyi GN. Nat Rev Clin Oncol 7 98-107 (2010)
  26. The complexity of complexes in signal transduction. Hlavacek WS, Faeder JR, Blinov ML, Perelson AS, Goldstein B. Biotechnol Bioeng 84 783-794 (2003)
  27. Targeting of erbB3 receptor to overcome resistance in cancer treatment. Ma J, Lyu H, Huang J, Liu B. Mol Cancer 13 105 (2014)
  28. EGFR-targeted therapies in the post-genomic era. Xu MJ, Johnson DE, Grandis JR. Cancer Metastasis Rev 36 463-473 (2017)
  29. Signaling through ERBB receptors: multiple layers of diversity and control. Warren CM, Landgraf R. Cell Signal 18 923-933 (2006)
  30. The insulin and EGF receptor structures: new insights into ligand-induced receptor activation. Ward CW, Lawrence MC, Streltsov VA, Adams TE, McKern NM. Trends Biochem Sci 32 129-137 (2007)
  31. The EGFR odyssey - from activation to destruction in space and time. Bakker J, Spits M, Neefjes J, Berlin I. J Cell Sci 130 4087-4096 (2017)
  32. Asymmetric tyrosine kinase arrangements in activation or autophosphorylation of receptor tyrosine kinases. Bae JH, Schlessinger J. Mol Cells 29 443-448 (2010)
  33. Signaling pathways in cancer-associated fibroblasts and targeted therapy for cancer. Wu F, Yang J, Liu J, Wang Y, Mu J, Zeng Q, Deng S, Zhou H. Signal Transduct Target Ther 6 218 (2021)
  34. Activation of the EGF Receptor by Ligand Binding and Oncogenic Mutations: The "Rotation Model". Purba ER, Saita EI, Maruyama IN. Cells 6 E13 (2017)
  35. Signaling receptome: a genomic and evolutionary perspective of plasma membrane receptors involved in signal transduction. Ben-Shlomo I, Yu Hsu S, Rauch R, Kowalski HW, Hsueh AJ. Sci STKE 2003 RE9 (2003)
  36. Epidermal growth factor receptor and cancer: control of oncogenic signalling by endocytosis. Grandal MV, Madshus IH. J Cell Mol Med 12 1527-1534 (2008)
  37. Rational bases for the development of EGFR inhibitors for cancer treatment. Bianco R, Gelardi T, Damiano V, Ciardiello F, Tortora G. Int J Biochem Cell Biol 39 1416-1431 (2007)
  38. Regulation of the catalytic activity of the EGF receptor. Endres NF, Engel K, Das R, Kovacs E, Kuriyan J. Curr Opin Struct Biol 21 777-784 (2011)
  39. Targeting EGFR and HER-2 receptor tyrosine kinases for cancer drug discovery and development. Kamath S, Buolamwini JK. Med Res Rev 26 569-594 (2006)
  40. Interaction of antibodies with ErbB receptor extracellular regions. Schmitz KR, Ferguson KM. Exp Cell Res 315 659-670 (2009)
  41. Mutational activation of ErbB family receptor tyrosine kinases: insights into mechanisms of signal transduction and tumorigenesis. Riese DJ, Gallo RM, Settleman J. Bioessays 29 558-565 (2007)
  42. Mechanisms of tumor resistance to EGFR-targeted therapies. Hopper-Borge EA, Nasto RE, Ratushny V, Weiner LM, Golemis EA, Astsaturov I. Expert Opin Ther Targets 13 339-362 (2009)
  43. The dissociation activation model of B cell antigen receptor triggering. Yang J, Reth M. FEBS Lett 584 4872-4877 (2010)
  44. Dynamic dissociating homo-oligomers and the control of protein function. Selwood T, Jaffe EK. Arch Biochem Biophys 519 131-143 (2012)
  45. Targeting tumor micro-environment for design and development of novel anti-angiogenic agents arresting tumor growth. Gacche RN, Meshram RJ. Prog Biophys Mol Biol 113 333-354 (2013)
  46. Receptor tyrosine kinase activation: From the ligand perspective. Trenker R, Jura N. Curr Opin Cell Biol 63 174-185 (2020)
  47. Survey of the year 2003 commercial optical biosensor literature. Rich RL, Myszka DG. J Mol Recognit 18 1-39 (2005)
  48. ERBB3 mutations in cancer: biological aspects, prevalence and therapeutics. Kiavue N, Cabel L, Melaabi S, Bataillon G, Callens C, Lerebours F, Pierga JY, Bidard FC. Oncogene 39 487-502 (2020)
  49. ErbB-directed immunotherapy: antibodies in current practice and promising new agents. Friedländer E, Barok M, Szöllosi J, Vereb G. Immunol Lett 116 126-140 (2008)
  50. Understanding the biology of HER3 receptor as a therapeutic target in human cancer. Lyu H, Han A, Polsdofer E, Liu S, Liu B. Acta Pharm Sin B 8 503-510 (2018)
  51. The ErbB kinase domain: structural perspectives into kinase activation and inhibition. Bose R, Zhang X. Exp Cell Res 315 649-658 (2009)
  52. Dynamic equilibrium between multiple active and inactive conformations explains regulation and oncogenic mutations in ErbB receptors. Landau M, Ben-Tal N. Biochim Biophys Acta 1785 12-31 (2008)
  53. Physical-chemical principles underlying RTK activation, and their implications for human disease. He L, Hristova K. Biochim Biophys Acta 1818 995-1005 (2012)
  54. HER2 therapy. HER2 (ERBB2): functional diversity from structurally conserved building blocks. Landgraf R. Breast Cancer Res 9 202 (2007)
  55. Targeted therapy in NSCLC driven by HER2 insertions. Peters S, Zimmermann S. Transl Lung Cancer Res 3 84-88 (2014)
  56. Roles for neuregulins in human cancer. Stove C, Bracke M. Clin Exp Metastasis 21 665-684 (2004)
  57. HER2 targeting as a two-sided strategy for breast cancer diagnosis and treatment: Outlook and recent implications in nanomedical approaches. Colombo M, Corsi F, Foschi D, Mazzantini E, Mazzucchelli S, Morasso C, Occhipinti E, Polito L, Prosperi D, Ronchi S, Verderio P. Pharmacol Res 62 150-165 (2010)
  58. Novel human antibody therapeutics: the age of the Umabs. Ruuls SR, Lammerts van Bueren JJ, van de Winkel JG, Parren PW. Biotechnol J 3 1157-1171 (2008)
  59. Putting together structures of epidermal growth factor receptors. Bessman NJ, Freed DM, Lemmon MA. Curr Opin Struct Biol 29 95-101 (2014)
  60. Extracellular molecules involved in cancer cell invasion. Stivarou T, Patsavoudi E. Cancers (Basel) 7 238-265 (2015)
  61. Targeting HER3 using mono- and bispecific antibodies or alternative scaffolds. Malm M, Frejd FY, Ståhl S, Löfblom J. MAbs 8 1195-1209 (2016)
  62. Autoinhibition in Ras effectors Raf, PI3Kα, and RASSF5: a comprehensive review underscoring the challenges in pharmacological intervention. Nussinov R, Zhang M, Tsai CJ, Liao TJ, Fushman D, Jang H. Biophys Rev 10 1263-1282 (2018)
  63. Role of erbB3 receptors in cancer therapeutic resistance. Lee Y, Ma J, Lyu H, Huang J, Kim A, Liu B. Acta Biochim Biophys Sin (Shanghai) 46 190-198 (2014)
  64. Targeting the heparin-binding epidermal growth factor-like growth factor in ovarian cancer therapy. Tsujioka H, Yotsumoto F, Hikita S, Ueda T, Kuroki M, Miyamoto S. Curr Opin Obstet Gynecol 23 24-30 (2011)
  65. The transition model of RTK activation: A quantitative framework for understanding RTK signaling and RTK modulator activity. Paul MD, Hristova K. Cytokine Growth Factor Rev 49 23-31 (2019)
  66. Mechanisms of Receptor Tyrosine-Protein Kinase ErbB-3 (ERBB3) Action in Human Neoplasia. Black LE, Longo JF, Carroll SL. Am J Pathol 189 1898-1912 (2019)
  67. ErbB receptors and epithelial-cadherin-catenin complex in human carcinomas. Yasmeen A, Bismar TA, Al Moustafa AE. Future Oncol 2 765-781 (2006)
  68. Membrane receptor activation mechanisms and transmembrane peptide tools to elucidate them. Westerfield JM, Barrera FN. J Biol Chem 295 1792-1814 (2020)
  69. Development of Effective Therapeutics Targeting HER3 for Cancer Treatment. Liu X, Liu S, Lyu H, Riker AI, Zhang Y, Liu B. Biol Proced Online 21 5 (2019)
  70. Emerging Allosteric Mechanism of EGFR Activation in Physiological and Pathological Contexts. Tsai CJ, Nussinov R. Biophys J 117 5-13 (2019)
  71. Receptor tyrosine kinase (RTK) signalling in the control of neural stem and progenitor cell (NSPC) development. Annenkov A. Mol Neurobiol 49 440-471 (2014)
  72. Structure-function relationships and supramolecular organization of the EGFR (epidermal growth factor receptor) on the cell surface. Needham SR, Zanetti-Domingues LC, Hirsch M, Rolfe DJ, Tynan CJ, Roberts SK, Martin-Fernandez ML, Clarke DT. Biochem Soc Trans 42 114-119 (2014)
  73. The role of ErbB3 binding protein 1 in cancer: Friend or foe? Nguyen DQ, Hoang DH, Nguyen Vo TT, Huynh V, Ghoda L, Marcucci G, Nguyen LXT. J Cell Physiol 233 9110-9120 (2018)
  74. A new paradigm for hormone recognition and allosteric receptor activation revealed from structural studies of NPR-C. He XL, Dukkipati A, Wang X, Garcia KC. Peptides 26 1035-1043 (2005)
  75. Advances in Targeting the Epidermal Growth Factor Receptor Pathway by Synthetic Products and Its Regulation by Epigenetic Modulators As a Therapy for Glioblastoma. Nadeem Abbas M, Kausar S, Wang F, Zhao Y, Cui H. Cells 8 E350 (2019)
  76. A tale of the epidermal growth factor receptor: The quest for structural resolution on cells. Tynan CJ, Lo Schiavo V, Zanetti-Domingues L, Needham SR, Roberts SK, Hirsch M, Rolfe DJ, Korovesis D, Clarke DT, Martin-Fernandez ML. Methods 95 86-93 (2016)
  77. Regulation of EGFR signalling by palmitoylation and its role in tumorigenesis. Kadry YA, Lee JY, Witze ES. Open Biol 11 210033 (2021)
  78. Chronicles of EGFR Tyrosine Kinase Inhibitors: Targeting EGFR C797S Containing Triple Mutations. Duggirala KB, Lee Y, Lee K. Biomol Ther (Seoul) 30 19-27 (2022)
  79. Mechanisms of Action of EGFR Tyrosine Kinase Receptor Incorporated in Extracellular Vesicles. Zanetti-Domingues LC, Bonner SE, Martin-Fernandez ML, Huber V. Cells 9 E2505 (2020)
  80. Structure-function relationships of ErbB RTKs in the plasma membrane of living cells. Arndt-Jovin DJ, Botelho MG, Jovin TM. Cold Spring Harb Perspect Biol 6 a008961 (2014)
  81. Receptor tyrosine kinase signaling--a proteomic perspective. Biarc J, Chalkley RJ, Burlingame AL, Bradshaw RA. Adv Enzyme Regul 51 293-305 (2011)
  82. The role of cetuximab in the management of non-small-cell lung cancer. Owonikoko TK, Sun SY, Ramalingam SS. Clin Lung Cancer 10 230-238 (2009)
  83. A Brief History of Single-Particle Tracking of the Epidermal Growth Factor Receptor. Clarke DT, Martin-Fernandez ML. Methods Protoc 2 E12 (2019)
  84. It Takes More than Two to Tango: Complex, Hierarchal, and Membrane-Modulated Interactions in the Regulation of Receptor Tyrosine Kinases. Kovacs T, Zakany F, Nagy P. Cancers (Basel) 14 944 (2022)
  85. Recent progress in protein-protein interaction study for EGFR-targeted therapeutics. Feiner RC, Müller KM. Expert Rev Proteomics 13 817-832 (2016)
  86. New ways to target old receptors. Whitty A, Riera TV. Curr Opin Chem Biol 12 427-433 (2008)
  87. Recent Advances in Monoclonal Antibody Therapy for Colorectal Cancers. Hwang K, Yoon JH, Lee JH, Lee S. Biomedicines 9 39 (2021)
  88. Role of microRNAs in epidermal growth factor receptor signaling pathway in cervical cancer. Hemmat N, Mokhtarzadeh A, Aghazadeh M, Jadidi-Niaragh F, Baradaran B, Bannazadeh Baghi H. Mol Biol Rep 47 4553-4568 (2020)
  89. Anti-EGFR Agents: Current Status, Forecasts and Future Directions. Kwapiszewski R, Pawlak SD, Adamkiewicz K. Target Oncol 11 739-752 (2016)
  90. Chemical synthesis of transmembrane peptide and its application for research on the transmembrane-juxtamembrane region of membrane protein. Sato T. Biopolymers 106 613-621 (2016)
  91. Molecularly Targeted Therapy towards Genetic Alterations in Advanced Bladder Cancer. Thomas J, Sonpavde G. Cancers (Basel) 14 1795 (2022)
  92. Reversion of the ErbB malignant phenotype and the DNA damage response. Runkle EA, Zhang H, Cai Z, Zhu Z, Karger BL, Wu SL, O'Rourke DM, Zhou Z, Wang Q, Greene MI. Exp Mol Pathol 93 324-333 (2012)
  93. Syndecans and Their Synstatins: Targeting an Organizer of Receptor Tyrosine Kinase Signaling at the Cell-Matrix Interface. Rapraeger AC. Front Oncol 11 775349 (2021)
  94. Signalling dynamics in embryonic development. Sonnen KF, Janda CY. Biochem J 478 4045-4070 (2021)
  95. A brief perspective of drug resistance toward EGFR inhibitors: the crystal structures of EGFRs and their variants. Guan H, Du Y, Ning Y, Cao X. Future Med Chem 9 693-704 (2017)
  96. Expanding the Disorder-Function Paradigm in the C-Terminal Tails of Erbbs. Pinet L, Assrir N, van Heijenoort C. Biomolecules 11 1690 (2021)
  97. Fluorescence Imaging of Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor Resistance in Non-Small Cell Lung Cancer. Martin-Fernandez ML. Cancers (Basel) 14 686 (2022)
  98. Deciphering the Impact of HER2 Alterations on Non-Small-Cell Lung Cancer: From Biological Mechanisms to Therapeutic Approaches. Bontoux C, Benzaquen J, Hofman V, Heeke S, Hannetel P, Capela-Brosseau-Laborde P, Marquette CH, Ilié M, Hofman P. J Pers Med 12 1651 (2022)
  99. Epigallocatechin-3-Gallate Therapeutic Potential in Cancer: Mechanism of Action and Clinical Implications. Kciuk M, Alam M, Ali N, Rashid S, Głowacka P, Sundaraj R, Celik I, Yahya EB, Dubey A, Zerroug E, Kontek R. Molecules 28 5246 (2023)
  100. Negative regulation of receptor tyrosine kinases by ubiquitination: Key roles of the Cbl family of E3 ubiquitin ligases. Tang R, Langdon WY, Zhang J. Front Endocrinol (Lausanne) 13 971162 (2022)
  101. Shifting the Focus of Signaling Abnormalities in Colon Cancer. Brown MA, Ried T. Cancers (Basel) 14 784 (2022)
  102. Structure-Guided Strategies of Targeted Therapies for Patients with EGFR-Mutant Non-Small Cell Lung Cancer. Du Z, Sun J, Zhang Y, Hesilaiti N, Xia Q, Cui H, Fan N, Xu X. Biomolecules 13 210 (2023)
  103. Target-Based Small Molecule Drug Discovery for Colorectal Cancer: A Review of Molecular Pathways and In Silico Studies. Moshawih S, Lim AF, Ardianto C, Goh KW, Kifli N, Goh HP, Jarrar Q, Ming LC. Biomolecules 12 878 (2022)
  104. Targeting Angiogenic Factors for the Treatment of Medulloblastoma. Saker Z, Rizk M, Bahmad HF, Nabha SM. Curr Treat Options Oncol 23 864-886 (2022)
  105. The ErbB Signaling Network and Its Potential Role in Endometrial Cancer. Androutsopoulos G, Styliara I, Zarogianni E, Lazurko N, Valasoulis G, Michail G, Adonakis G. Epigenomes 7 24 (2023)
  106. [Creation of artificial receptors activated by coiled-coil peptides and cellular regulation]. Nakase I. Yakugaku Zasshi 135 375-381 (2015)

Articles citing this publication (265)

  1. An allosteric mechanism for activation of the kinase domain of epidermal growth factor receptor. Zhang X, Gureasko J, Shen K, Cole PA, Kuriyan J. Cell 125 1137-1149 (2006)
  2. Insights into ErbB signaling from the structure of the ErbB2-pertuzumab complex. Franklin MC, Carey KD, Vajdos FF, Leahy DJ, de Vos AM, Sliwkowski MX. Cancer Cell 5 317-328 (2004)
  3. Structural basis for inhibition of the epidermal growth factor receptor by cetuximab. Li S, Schmitz KR, Jeffrey PD, Wiltzius JJ, Kussie P, Ferguson KM. Cancer Cell 7 301-311 (2005)
  4. Membranes are more mosaic than fluid. Engelman DM. Nature 438 578-580 (2005)
  5. Quantum dot ligands provide new insights into erbB/HER receptor-mediated signal transduction. Lidke DS, Nagy P, Heintzmann R, Arndt-Jovin DJ, Post JN, Grecco HE, Jares-Erijman EA, Jovin TM. Nat Biotechnol 22 198-203 (2004)
  6. The crystal structure of a truncated ErbB2 ectodomain reveals an active conformation, poised to interact with other ErbB receptors. Garrett TP, McKern NM, Lou M, Elleman TC, Adams TE, Lovrecz GO, Kofler M, Jorissen RN, Nice EC, Burgess AW, Ward CW. Mol Cell 11 495-505 (2003)
  7. Conformational coupling across the plasma membrane in activation of the EGF receptor. Endres NF, Das R, Smith AW, Arkhipov A, Kovacs E, Huang Y, Pelton JG, Shan Y, Shaw DE, Wemmer DE, Groves JT, Kuriyan J. Cell 152 543-556 (2013)
  8. Oncogenic ERBB3 mutations in human cancers. Jaiswal BS, Kljavin NM, Stawiski EW, Chan E, Parikh C, Durinck S, Chaudhuri S, Pujara K, Guillory J, Edgar KA, Janakiraman V, Scholz RP, Bowman KK, Lorenzo M, Li H, Wu J, Yuan W, Peters BA, Kan Z, Stinson J, Mak M, Modrusan Z, Eigenbrot C, Firestein R, Stern HM, Rajalingam K, Schaefer G, Merchant MA, Sliwkowski MX, de Sauvage FJ, Seshagiri S. Cancer Cell 23 603-617 (2013)
  9. Sialylation and fucosylation of epidermal growth factor receptor suppress its dimerization and activation in lung cancer cells. Liu YC, Yen HY, Chen CY, Chen CH, Cheng PF, Juan YH, Chen CH, Khoo KH, Yu CJ, Yang PC, Hsu TL, Wong CH. Proc Natl Acad Sci U S A 108 11332-11337 (2011)
  10. Closed state of both binding domains of homodimeric mGlu receptors is required for full activity. Kniazeff J, Bessis AS, Maurel D, Ansanay H, Prézeau L, Pin JP. Nat Struct Mol Biol 11 706-713 (2004)
  11. Epidermal growth factor receptor dimerization and activation require ligand-induced conformational changes in the dimer interface. Dawson JP, Berger MB, Lin CC, Schlessinger J, Lemmon MA, Ferguson KM. Mol Cell Biol 25 7734-7742 (2005)
  12. Ligand-induced dimer-tetramer transition during the activation of the cell surface epidermal growth factor receptor-A multidimensional microscopy analysis. Clayton AH, Walker F, Orchard SG, Henderson C, Fuchs D, Rothacker J, Nice EC, Burgess AW. J Biol Chem 280 30392-30399 (2005)
  13. ErbB1 dimerization is promoted by domain co-confinement and stabilized by ligand binding. Low-Nam ST, Lidke KA, Cutler PJ, Roovers RC, van Bergen en Henegouwen PM, Wilson BS, Lidke DS. Nat Struct Mol Biol 18 1244-1249 (2011)
  14. EGFR Ligands Differentially Stabilize Receptor Dimers to Specify Signaling Kinetics. Freed DM, Bessman NJ, Kiyatkin A, Salazar-Cavazos E, Byrne PO, Moore JO, Valley CC, Ferguson KM, Leahy DJ, Lidke DS, Lemmon MA. Cell 171 683-695.e18 (2017)
  15. The Sema domain of Met is necessary for receptor dimerization and activation. Kong-Beltran M, Stamos J, Wickramasinghe D. Cancer Cell 6 75-84 (2004)
  16. Oligomerization of the EGF receptor investigated by live cell fluorescence intensity distribution analysis. Saffarian S, Li Y, Elson EL, Pike LJ. Biophys J 93 1021-1031 (2007)
  17. Active macropinocytosis induction by stimulation of epidermal growth factor receptor and oncogenic Ras expression potentiates cellular uptake efficacy of exosomes. Nakase I, Kobayashi NB, Takatani-Nakase T, Yoshida T. Sci Rep 5 10300 (2015)
  18. Structural basis for negative cooperativity in growth factor binding to an EGF receptor. Alvarado D, Klein DE, Lemmon MA. Cell 142 568-579 (2010)
  19. Heterogeneity in EGF-binding affinities arises from negative cooperativity in an aggregating system. Macdonald JL, Pike LJ. Proc Natl Acad Sci U S A 105 112-117 (2008)
  20. The extracellular region of ErbB4 adopts a tethered conformation in the absence of ligand. Bouyain S, Longo PA, Li S, Ferguson KM, Leahy DJ. Proc Natl Acad Sci U S A 102 15024-15029 (2005)
  21. Mechanism of activation and inhibition of the HER4/ErbB4 kinase. Qiu C, Tarrant MK, Choi SH, Sathyamurthy A, Bose R, Banjade S, Pal A, Bornmann WG, Lemmon MA, Cole PA, Leahy DJ. Structure 16 460-467 (2008)
  22. Investigation of the dimerization of proteins from the epidermal growth factor receptor family by single wavelength fluorescence cross-correlation spectroscopy. Liu P, Sudhaharan T, Koh RM, Hwang LC, Ahmed S, Maruyama IN, Wohland T. Biophys J 93 684-698 (2007)
  23. Clinical benefit of lapatinib-based therapy in patients with human epidermal growth factor receptor 2-positive breast tumors coexpressing the truncated p95HER2 receptor. Scaltriti M, Chandarlapaty S, Prudkin L, Aura C, Jimenez J, Angelini PD, Sánchez G, Guzman M, Parra JL, Ellis C, Gagnon R, Koehler M, Gomez H, Geyer C, Cameron D, Arribas J, Arribas J, Rosen N, Baselga J. Clin Cancer Res 16 2688-2695 (2010)
  24. Argos inhibits epidermal growth factor receptor signalling by ligand sequestration. Klein DE, Nappi VM, Reeves GT, Shvartsman SY, Lemmon MA. Nature 430 1040-1044 (2004)
  25. Cholesterol depletion results in site-specific increases in epidermal growth factor receptor phosphorylation due to membrane level effects. Studies with cholesterol enantiomers. Westover EJ, Covey DF, Brockman HL, Brown RE, Pike LJ. J Biol Chem 278 51125-51133 (2003)
  26. An antibody that locks HER3 in the inactive conformation inhibits tumor growth driven by HER2 or neuregulin. Garner AP, Bialucha CU, Sprague ER, Garrett JT, Sheng Q, Li S, Sineshchekova O, Saxena P, Sutton CR, Chen D, Chen Y, Wang H, Liang J, Das R, Mosher R, Gu J, Huang A, Haubst N, Zehetmeier C, Haberl M, Elis W, Kunz C, Heidt AB, Herlihy K, Murtie J, Schuller A, Arteaga CL, Sellers WR, Ettenberg SA. Cancer Res 73 6024-6035 (2013)
  27. An electrostatic engine model for autoinhibition and activation of the epidermal growth factor receptor (EGFR/ErbB) family. McLaughlin S, Smith SO, Hayman MJ, Murray D. J Gen Physiol 126 41-53 (2005)
  28. Single-molecule analysis of epidermal growth factor binding on the surface of living cells. Teramura Y, Ichinose J, Takagi H, Nishida K, Yanagida T, Sako Y. EMBO J 25 4215-4222 (2006)
  29. Fine epitope mapping of anti-epidermal growth factor receptor antibodies through random mutagenesis and yeast surface display. Chao G, Cochran JR, Wittrup KD. J Mol Biol 342 539-550 (2004)
  30. Molecular basis for multimerization in the activation of the epidermal growth factor receptor. Huang Y, Bharill S, Karandur D, Peterson SM, Marita M, Shi X, Kaliszewski MJ, Smith AW, Isacoff EY, Kuriyan J. Elife 5 e14107 (2016)
  31. A single ligand is sufficient to activate EGFR dimers. Liu P, Cleveland TE, Bouyain S, Byrne PO, Longo PA, Leahy DJ. Proc Natl Acad Sci U S A 109 10861-10866 (2012)
  32. EGFR Dynamics Change during Activation in Native Membranes as Revealed by NMR. Kaplan M, Narasimhan S, de Heus C, Mance D, van Doorn S, Houben K, Popov-Čeleketić D, Damman R, Katrukha EA, Jain P, Geerts WJC, Heck AJR, Folkers GE, Kapitein LC, Lemeer S, van Bergen En Henegouwen PMP, Baldus M. Cell 167 1241-1251.e11 (2016)
  33. EGFR oligomerization organizes kinase-active dimers into competent signalling platforms. Needham SR, Roberts SK, Arkhipov A, Mysore VP, Tynan CJ, Zanetti-Domingues LC, Kim ET, Losasso V, Korovesis D, Hirsch M, Rolfe DJ, Clarke DT, Winn MD, Lajevardipour A, Clayton AH, Pike LJ, Perani M, Parker PJ, Shan Y, Shaw DE, Martin-Fernandez ML. Nat Commun 7 13307 (2016)
  34. EGF signalling amplification induced by dynamic clustering of EGFR. Ichinose J, Murata M, Yanagida T, Sako Y. Biochem Biophys Res Commun 324 1143-1149 (2004)
  35. A structure-based model for ligand binding and dimerization of EGF receptors. Klein P, Mattoon D, Lemmon MA, Schlessinger J. Proc Natl Acad Sci U S A 101 929-934 (2004)
  36. Structural basis for EGF receptor inhibition by the therapeutic antibody IMC-11F8. Li S, Kussie P, Ferguson KM. Structure 16 216-227 (2008)
  37. Phage display selection of Affibody molecules with specific binding to the extracellular domain of the epidermal growth factor receptor. Friedman M, Nordberg E, Höidén-Guthenberg I, Brismar H, Adams GP, Nilsson FY, Carlsson J, Ståhl S. Protein Eng Des Sel 20 189-199 (2007)
  38. Ligand-induced structural transitions in ErbB receptor extracellular domains. Dawson JP, Bu Z, Lemmon MA. Structure 15 942-954 (2007)
  39. Different epidermal growth factor (EGF) receptor ligands show distinct kinetics and biased or partial agonism for homodimer and heterodimer formation. Macdonald-Obermann JL, Pike LJ. J Biol Chem 289 26178-26188 (2014)
  40. Mechanisms of activation of receptor tyrosine kinases: monomers or dimers. Maruyama IN. Cells 3 304-330 (2014)
  41. On the nature of low- and high-affinity EGF receptors on living cells. Ozcan F, Klein P, Lemmon MA, Lax I, Schlessinger J. Proc Natl Acad Sci U S A 103 5735-5740 (2006)
  42. Functional and structural stability of the epidermal growth factor receptor in detergent micelles and phospholipid nanodiscs. Mi LZ, Grey MJ, Nishida N, Walz T, Lu C, Springer TA. Biochemistry 47 10314-10323 (2008)
  43. Structural analysis of the EGFR/HER3 heterodimer reveals the molecular basis for activating HER3 mutations. Littlefield P, Liu L, Mysore V, Shan Y, Shaw DE, Jura N. Sci Signal 7 ra114 (2014)
  44. Structural basis for eliciting a cytotoxic effect in HER2-overexpressing cancer cells via binding to the extracellular domain of HER2. Jost C, Schilling J, Tamaskovic R, Schwill M, Honegger A, Plückthun A. Structure 21 1979-1991 (2013)
  45. The intracellular juxtamembrane domain of the epidermal growth factor (EGF) receptor is responsible for the allosteric regulation of EGF binding. Macdonald-Obermann JL, Pike LJ. J Biol Chem 284 13570-13576 (2009)
  46. Rational identification of an optimal antibody mixture for targeting the epidermal growth factor receptor. Koefoed K, Steinaa L, Søderberg JN, Kjær I, Jacobsen HJ, Meijer PJ, Haurum JS, Jensen A, Kragh M, Andersen PS, Pedersen MW. MAbs 3 584-595 (2011)
  47. The FRET signatures of noninteracting proteins in membranes: simulations and experiments. King C, Sarabipour S, Byrne P, Leahy DJ, Hristova K. Biophys J 106 1309-1317 (2014)
  48. Domain-level antibody epitope mapping through yeast surface display of epidermal growth factor receptor fragments. Cochran JR, Kim YS, Olsen MJ, Bhandari R, Wittrup KD. J Immunol Methods 287 147-158 (2004)
  49. Molecular mechanisms of ubiquitin-dependent membrane traffic. Hurley JH, Stenmark H. Annu Rev Biophys 40 119-142 (2011)
  50. Effect of sialylation on EGFR phosphorylation and resistance to tyrosine kinase inhibition. Yen HY, Liu YC, Chen NY, Tsai CF, Wang YT, Chen YJ, Hsu TL, Yang PC, Wong CH. Proc Natl Acad Sci U S A 112 6955-6960 (2015)
  51. Cellular studies of binding, internalization and retention of a radiolabeled EGFR-binding affibody molecule. Nordberg E, Friedman M, Göstring L, Adams GP, Brismar H, Nilsson FY, Ståhl S, Glimelius B, Carlsson J. Nucl Med Biol 34 609-618 (2007)
  52. ERK-dependent threonine phosphorylation of EGF receptor modulates receptor downregulation and signaling. Li X, Huang Y, Jiang J, Frank SJ. Cell Signal 20 2145-2155 (2008)
  53. Effect of the anti-receptor ligand-blocking 225 monoclonal antibody on EGF receptor endocytosis and sorting. Jaramillo ML, Leon Z, Grothe S, Paul-Roc B, Abulrob A, O'Connor McCourt M. Exp Cell Res 312 2778-2790 (2006)
  54. ErbB2 resembles an autoinhibited invertebrate epidermal growth factor receptor. Alvarado D, Klein DE, Lemmon MA. Nature 461 287-291 (2009)
  55. MM-151 overcomes acquired resistance to cetuximab and panitumumab in colorectal cancers harboring EGFR extracellular domain mutations. Arena S, Siravegna G, Mussolin B, Kearns JD, Wolf BB, Misale S, Lazzari L, Bertotti A, Trusolino L, Adjei AA, Montagut C, Di Nicolantonio F, Nering R, Bardelli A. Sci Transl Med 8 324ra14 (2016)
  56. Mechanistic insights into the activation of oncogenic forms of EGF receptor. Wang Z, Longo PA, Tarrant MK, Kim K, Head S, Leahy DJ, Cole PA. Nat Struct Mol Biol 18 1388-1393 (2011)
  57. Mechanistic insights into EGFR membrane clustering revealed by super-resolution imaging. Gao J, Wang Y, Cai M, Pan Y, Xu H, Jiang J, Ji H, Wang H. Nanoscale 7 2511-2519 (2015)
  58. EGF-independent activation of cell-surface EGF receptors harboring mutations found in gefitinib-sensitive lung cancer. Choi SH, Mendrola JM, Lemmon MA. Oncogene 26 1567-1576 (2007)
  59. Antibodies specifically targeting a locally misfolded region of tumor associated EGFR. Garrett TP, Burgess AW, Gan HK, Luwor RB, Cartwright G, Walker F, Orchard SG, Clayton AH, Nice EC, Rothacker J, Catimel B, Cavenee WK, Old LJ, Stockert E, Ritter G, Adams TE, Hoyne PA, Wittrup D, Chao G, Cochran JR, Luo C, Lou M, Huyton T, Xu Y, Fairlie WD, Yao S, Scott AM, Johns TG. Proc Natl Acad Sci U S A 106 5082-5087 (2009)
  60. Mechanisms for kinase-mediated dimerization of the epidermal growth factor receptor. Lu C, Mi LZ, Schürpf T, Walz T, Springer TA. J Biol Chem 287 38244-38253 (2012)
  61. Structures of adnectin/protein complexes reveal an expanded binding footprint. Ramamurthy V, Krystek SR, Bush A, Wei A, Emanuel SL, Das Gupta R, Janjua A, Cheng L, Murdock M, Abramczyk B, Cohen D, Lin Z, Morin P, Davis JH, Dabritz M, McLaughlin DC, Russo KA, Chao G, Wright MC, Jenny VA, Engle LJ, Furfine E, Sheriff S. Structure 20 259-269 (2012)
  62. 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 SJ, Ben-Tal N. Structure 12 2265-2275 (2004)
  63. Directed evolution of the epidermal growth factor receptor extracellular domain for expression in yeast. Kim YS, Bhandari R, Cochran JR, Kuriyan J, Wittrup KD. Proteins 62 1026-1035 (2006)
  64. The alternatively spliced acid box region plays a key role in FGF receptor autoinhibition. Kalinina J, Dutta K, Ilghari D, Beenken A, Goetz R, Eliseenkova AV, Cowburn D, Mohammadi M. Structure 20 77-88 (2012)
  65. EGF-related growth factors in the pathogenesis of murine ARPKD. MacRae Dell K, Nemo R, Sweeney WE, Avner ED. Kidney Int 65 2018-2029 (2004)
  66. The extracellular domain of fibroblast growth factor receptor 3 inhibits ligand-independent dimerization. Chen L, Placone J, Novicky L, Hristova K. Sci Signal 3 ra86 (2010)
  67. Analysis of the Role of the C-Terminal Tail in the Regulation of the Epidermal Growth Factor Receptor. Kovacs E, Das R, Wang Q, Collier TS, Cantor A, Huang Y, Wong K, Mirza A, Barros T, Grob P, Jura N, Bose R, Kuriyan J. Mol Cell Biol 35 3083-3102 (2015)
  68. Cryo-EM structure of the complete and ligand-saturated insulin receptor ectodomain. Gutmann T, Schäfer IB, Poojari C, Brankatschk B, Vattulainen I, Strauss M, Coskun Ü. J Cell Biol 219 e201907210 (2020)
  69. Development and clinical application of an integrative genomic approach to personalized cancer therapy. Uzilov AV, Ding W, Fink MY, Antipin Y, Brohl AS, Davis C, Lau CY, Pandya C, Shah H, Kasai Y, Powell J, Micchelli M, Castellanos R, Zhang Z, Linderman M, Kinoshita Y, Zweig M, Raustad K, Cheung K, Castillo D, Wooten M, Bourzgui I, Newman LC, Deikus G, Mathew B, Zhu J, Glicksberg BS, Moe AS, Liao J, Edelmann L, Dudley JT, Maki RG, Kasarskis A, Holcombe RF, Mahajan M, Hao K, Reva B, Longtine J, Starcevic D, Sebra R, Donovan MJ, Li S, Schadt EE, Chen R. Genome Med 8 62 (2016)
  70. Differential ErbB1 signaling in squamous cell versus basal cell carcinoma of the skin. Rittié L, Kansra S, Stoll SW, Li Y, Gudjonsson JE, Shao Y, Michael LE, Fisher GJ, Johnson TM, Elder JT. Am J Pathol 170 2089-2099 (2007)
  71. Structural model of the mAb 806-EGFR complex using computational docking followed by computational and experimental mutagenesis. Sivasubramanian A, Chao G, Pressler HM, Wittrup KD, Gray JJ. Structure 14 401-414 (2006)
  72. Two GxxxG-like motifs facilitate promiscuous interactions of the human ErbB transmembrane domains. Escher C, Cymer F, Schneider D. J Mol Biol 389 10-16 (2009)
  73. In vitro enzymatic characterization of near full length EGFR in activated and inhibited states. Qiu C, Tarrant MK, Boronina T, Longo PA, Kavran JM, Cole RN, Cole PA, Leahy DJ. Biochemistry 48 6624-6632 (2009)
  74. HER2 stabilizes EGFR and itself by altering autophosphorylation patterns in a manner that overcomes regulatory mechanisms and promotes proliferative and transformation signaling. Hartman Z, Zhao H, Agazie YM. Oncogene 32 4169-4180 (2013)
  75. Insights into the evolution of the ErbB receptor family and their ligands from sequence analysis. Stein RA, Staros JV. BMC Evol Biol 6 79 (2006)
  76. Ligand regulates epidermal growth factor receptor kinase specificity: activation increases preference for GAB1 and SHC versus autophosphorylation sites. Fan YX, Wong L, Deb TB, Johnson GR. J Biol Chem 279 38143-38150 (2004)
  77. Loss of EGFR signaling regulated miR-203 promotes prostate cancer bone metastasis and tyrosine kinase inhibitors resistance. Siu MK, Abou-Kheir W, Yin JJ, Chang YS, Barrett B, Suau F, Casey O, Chen WY, Fang L, Hynes P, Hsieh YY, Liu YN, Huang J, Kelly K. Oncotarget 5 3770-3784 (2014)
  78. Quantitative analysis reveals how EGFR activation and downregulation are coupled in normal but not in cancer cells. Capuani F, Conte A, Argenzio E, Marchetti L, Priami C, Polo S, Di Fiore PP, Sigismund S, Ciliberto A. Nat Commun 6 7999 (2015)
  79. Dual fatty acid synthase and HER2 signaling blockade shows marked antitumor activity against breast cancer models resistant to anti-HER2 drugs. Blancafort A, Giró-Perafita A, Oliveras G, Palomeras S, Turrado C, Campuzano Ò, Carrión-Salip D, Massaguer A, Brugada R, Palafox M, Gómez-Miragaya J, González-Suárez E, Puig T. PLoS One 10 e0131241 (2015)
  80. EGF-dependent re-routing of vesicular recycling switches spontaneous phosphorylation suppression to EGFR signaling. Baumdick M, Brüggemann Y, Schmick M, Xouri G, Sabet O, Davis L, Chin JW, Bastiaens PI. Elife 4 e12223 (2015)
  81. Angiotensin-converting enzyme (ACE) dimerization is the initial step in the ACE inhibitor-induced ACE signaling cascade in endothelial cells. Kohlstedt K, Gershome C, Friedrich M, Müller-Esterl W, Alhenc-Gelas F, Busse R, Fleming I. Mol Pharmacol 69 1725-1732 (2006)
  82. Phosphorylated EGFR Dimers Are Not Sufficient to Activate Ras. Liang SI, van Lengerich B, Eichel K, Cha M, Patterson DM, Yoon TY, von Zastrow M, Jura N, Gartner ZJ. Cell Rep 22 2593-2600 (2018)
  83. Ectodomain orientation, conformational plasticity and oligomerization of ErbB1 receptors investigated by molecular dynamics. Kästner J, Loeffler HH, Roberts SK, Martin-Fernandez ML, Winn MD. J Struct Biol 167 117-128 (2009)
  84. Molecular analysis of the EGFR gene in astrocytic gliomas: mRNA expression, quantitative-PCR analysis of non-homogeneous gene amplification and DNA sequence alterations. Arjona D, Bello MJ, Alonso ME, Aminoso C, Isla A, De Campos JM, Sarasa JL, Gutierrez M, Villalobo A, Rey JA. Neuropathol Appl Neurobiol 31 384-394 (2005)
  85. Molecular modeling of nearly full-length ErbB2 receptor. Bagossi P, Horváth G, Vereb G, Szöllösi J, Tözsér J. Biophys J 88 1354-1363 (2005)
  86. Role of N-glycosylation in EGFR ectodomain ligand binding. Azimzadeh Irani M, Kannan S, Verma C. Proteins 85 1529-1549 (2017)
  87. Self-association of models of transmembrane domains of ErbB receptors in a lipid bilayer. Prakash A, Janosi L, Doxastakis M. Biophys J 99 3657-3665 (2010)
  88. Transmembrane helix orientation influences membrane binding of the intracellular juxtamembrane domain in Neu receptor peptides. Matsushita C, Tamagaki H, Miyazawa Y, Aimoto S, Smith SO, Sato T. Proc Natl Acad Sci U S A 110 1646-1651 (2013)
  89. Compensatory ErbB3/c-Src signaling enhances carcinoma cell survival to ionizing radiation. Contessa JN, Abell A, Mikkelsen RB, Valerie K, Schmidt-Ullrich RK. Breast Cancer Res Treat 95 17-27 (2006)
  90. Homodimerization controls the fibroblast growth factor 9 subfamily's receptor binding and heparan sulfate-dependent diffusion in the extracellular matrix. Kalinina J, Byron SA, Makarenkova HP, Olsen SK, Eliseenkova AV, Larochelle WJ, Dhanabal M, Blais S, Ornitz DM, Day LA, Neubert TA, Pollock PM, Mohammadi M. Mol Cell Biol 29 4663-4678 (2009)
  91. SPINK6 Promotes Metastasis of Nasopharyngeal Carcinoma via Binding and Activation of Epithelial Growth Factor Receptor. Zheng LS, Yang JP, Cao Y, Peng LX, Sun R, Xie P, Wang MY, Meng DF, Luo DH, Zou X, Chen MY, Mai HQ, Guo L, Guo X, Shao JY, Huang BJ, Zhang W, Qian CN. Cancer Res 77 579-589 (2017)
  92. Luciferase fragment complementation imaging of conformational changes in the epidermal growth factor receptor. Yang KS, Ilagan MX, Piwnica-Worms D, Pike LJ. J Biol Chem 284 7474-7482 (2009)
  93. Atomistic insights into regulatory mechanisms of the HER2 tyrosine kinase domain: a molecular dynamics study. Telesco SE, Radhakrishnan R. Biophys J 96 2321-2334 (2009)
  94. Growth Factor Identity Is Encoded by Discrete Coiled-Coil Rotamers in the EGFR Juxtamembrane Region. Doerner A, Scheck R, Schepartz A. Chem Biol 22 776-784 (2015)
  95. Inside-out Regulation of Ectodomain Cleavage of Cluster-of-Differentiation-44 (CD44) and of Neuregulin-1 Requires Substrate Dimerization. Hartmann M, Parra LM, Ruschel A, Lindner C, Morrison H, Herrlich A, Herrlich P. J Biol Chem 290 17041-17054 (2015)
  96. Peptide vaccines and peptidomimetics of EGFR (HER-1) ligand binding domain inhibit cancer cell growth in vitro and in vivo. Foy KC, Wygle RM, Miller MJ, Overholser JP, Bekaii-Saab T, Kaumaya PT. J Immunol 191 217-227 (2013)
  97. SEMA3C drives cancer growth by transactivating multiple receptor tyrosine kinases via Plexin B1. Peacock JW, Takeuchi A, Hayashi N, Liu L, Tam KJ, Al Nakouzi N, Khazamipour N, Tombe T, Dejima T, Lee KC, Shiota M, Thaper D, Lee WC, Hui DH, Kuruma H, Ivanova L, Yenki P, Jiao IZ, Khosravi S, Mui AL, Fazli L, Zoubeidi A, Daugaard M, Gleave ME, Ong CJ. EMBO Mol Med 10 219-238 (2018)
  98. Dynamic conformational transitions of the EGF receptor in living mammalian cells determined by FRET and fluorescence lifetime imaging microscopy. Ziomkiewicz I, Loman A, Klement R, Fritsch C, Klymchenko AS, Bunt G, Jovin TM, Arndt-Jovin DJ. Cytometry A 83 794-805 (2013)
  99. Quantitative proteomic analysis reveals effects of epidermal growth factor receptor (EGFR) on invasion-promoting proteins secreted by glioblastoma cells. Sangar V, Funk CC, Kusebauch U, Campbell DS, Moritz RL, Price ND. Mol Cell Proteomics 13 2618-2631 (2014)
  100. A growing family: adding mutated Erbb4 as a novel cancer target. Rudloff U, Samuels Y. Cell Cycle 9 1487-1503 (2010)
  101. Preparation and characterization of Alexa Fluor 594-labeled epidermal growth factor for fluorescence resonance energy transfer studies: application to the epidermal growth factor receptor. Whitson KB, Beechem JM, Beth AH, Staros JV. Anal Biochem 324 227-236 (2004)
  102. Structural and functional characterization of alternative transmembrane domain conformations in VEGF receptor 2 activation. Manni S, Mineev KS, Usmanova D, Lyukmanova EN, Shulepko MA, Kirpichnikov MP, Winter J, Matkovic M, Deupi X, Arseniev AS, Ballmer-Hofer K. Structure 22 1077-1089 (2014)
  103. Measuring EGFR separations on cells with ~10 nm resolution via fluorophore localization imaging with photobleaching. Needham SR, Hirsch M, Rolfe DJ, Clarke DT, Zanetti-Domingues LC, Wareham R, Martin-Fernandez ML. PLoS One 8 e62331 (2013)
  104. Stealth carriers for low-resolution structure determination of membrane proteins in solution. Maric S, Skar-Gislinge N, Midtgaard S, Thygesen MB, Schiller J, Frielinghaus H, Moulin M, Haertlein M, Forsyth VT, Pomorski TG, Arleth L. Acta Crystallogr D Biol Crystallogr 70 317-328 (2014)
  105. Structure-function analysis of nucleolin and ErbB receptors interactions. Farin K, Di Segni A, Mor A, Pinkas-Kramarski R. PLoS One 4 e6128 (2009)
  106. Quantitation of the effect of ErbB2 on epidermal growth factor receptor binding and dimerization. Li Y, Macdonald-Obermann J, Westfall C, Piwnica-Worms D, Pike LJ. J Biol Chem 287 31116-31125 (2012)
  107. A multiscale computational approach to dissect early events in the Erb family receptor mediated activation, differential signaling, and relevance to oncogenic transformations. Liu Y, Purvis J, Shih A, Weinstein J, Agrawal N, Radhakrishnan R. Ann Biomed Eng 35 1012-1025 (2007)
  108. Targeting the dimerization of epidermal growth factor receptors with small-molecule inhibitors. Yang RY, Yang KS, Pike LJ, Marshall GR. Chem Biol Drug Des 76 1-9 (2010)
  109. Dynamic analysis of the epidermal growth factor (EGF) receptor-ErbB2-ErbB3 protein network by luciferase fragment complementation imaging. Macdonald-Obermann JL, Adak S, Landgraf R, Piwnica-Worms D, Pike LJ. J Biol Chem 288 30773-30784 (2013)
  110. Five carboxyl-terminal residues of neuregulin2 are critical for stimulation of signaling by the ErbB4 receptor tyrosine kinase. Hobbs SS, Cameron EM, Hammer RP, Le AT, Gallo RM, Blommel EN, Coffing SL, Chang H, Riese DJ. Oncogene 23 883-893 (2004)
  111. The bioactivity and receptor affinity of recombinant tagged EGF designed for tissue engineering applications is defined by the nature and position of the tags. Boucher C, St-Laurent G, Loignon M, Jolicoeur M, De Crescenzo G, Durocher Y. Tissue Eng Part A 14 2069-2077 (2008)
  112. Extended and flexible domain solution structure of the extracellular matrix protein anosmin-1 by X-ray scattering, analytical ultracentrifugation and constrained modelling. Hu Y, Sun Z, Eaton JT, Bouloux PM, Perkins SJ. J Mol Biol 350 553-570 (2005)
  113. Tuning protein autoinhibition by domain destabilization. Cho JH, Muralidharan V, Vila-Perello M, Raleigh DP, Muir TW, Palmer AG. Nat Struct Mol Biol 18 550-555 (2011)
  114. EGFR-mediated signaling pathway influences the sensitivity of oral squamous cell carcinoma to JQ1. Liu X, Li Q, Huang P, Tong D, Wu H, Zhang F. J Cell Biochem 119 8368-8377 (2018)
  115. The N-terminal domains of neuregulin 1 confer signal attenuation. Warren CM, Kani K, Landgraf R. J Biol Chem 281 27306-27316 (2006)
  116. The oncoprotein ErbB3 is endocytosed in the absence of added ligand in a clathrin-dependent manner. Sak MM, Breen K, Rønning SB, Pedersen NM, Bertelsen V, Stang E, Madshus IH. Carcinogenesis 33 1031-1039 (2012)
  117. Evidence for extended YFP-EGFR dimers in the absence of ligand on the surface of living cells. Kozer N, Henderson C, Jackson JT, Nice EC, Burgess AW, Clayton AH. Phys Biol 8 066002 (2011)
  118. Glioma-specific Domain IV EGFR cysteine mutations promote ligand-induced covalent receptor dimerization and display enhanced sensitivity to dacomitinib in vivo. Greenall SA, Donoghue JF, Gottardo NG, Johns TG, Adams TE. Oncogene 34 1658-1666 (2015)
  119. Identification of in vitro autophosphorylation sites and effects of phosphorylation on the Arabidopsis CRINKLY4 (ACR4) receptor-like kinase intracellular domain: insights into conformation, oligomerization, and activity. Meyer MR, Lichti CF, Townsend RR, Rao AG. Biochemistry 50 2170-2186 (2011)
  120. Kinase activator-receiver preference in ErbB heterodimers is determined by intracellular regions and is not coupled to extracellular asymmetry. Ward MD, Leahy DJ. J Biol Chem 290 1570-1579 (2015)
  121. Pharmacophore modelling, molecular docking and virtual screening for EGFR (HER 1) tyrosine kinase inhibitors. Gupta AK, Bhunia SS, Balaramnavar VM, Saxena AK. SAR QSAR Environ Res 22 239-263 (2011)
  122. Analysis of Somatic Mutations in Cancer: Molecular Mechanisms of Activation in the ErbB Family of Receptor Tyrosine Kinases. Shih AJ, Telesco SE, Radhakrishnan R. Cancers (Basel) 3 1195-1231 (2011)
  123. Computational analysis of molecular basis of 1:1 interactions of NRG-1beta wild-type and variants with ErbB3 and ErbB4. Luo C, Xu L, Zheng S, Luo X, Shen J, Jiang H, Liu X, Zhou M. Proteins 59 742-756 (2005)
  124. Epidermal growth factor receptor domain II, IV, and kinase domain mutations in human solid tumors. Sihto H, Puputti M, Pulli L, Tynninen O, Koskinen W, Aaltonen LM, Tanner M, Böhling T, Visakorpi T, Bützow R, Knuuttila A, Nupponen NN, Joensuu H. J Mol Med (Berl) 83 976-983 (2005)
  125. Protein lysine methyltransferase SMYD3 is involved in tumorigenesis through regulation of HER2 homodimerization. Yoshioka Y, Suzuki T, Matsuo Y, Tsurita G, Watanabe T, Dohmae N, Nakamura Y, Hamamoto R. Cancer Med 6 1665-1672 (2017)
  126. Serine protease inhibitor Kazal type 1 (SPINK1) drives proliferation and anoikis resistance in a subset of ovarian cancers. Mehner C, Oberg AL, Kalli KR, Nassar A, Hockla A, Pendlebury D, Cichon MA, Goergen KM, Maurer MJ, Goode EL, Keeney GL, Jatoi A, Sahin-Tóth M, Copland JA, Radisky DC, Radisky ES. Oncotarget 6 35737-35754 (2015)
  127. The NMR solution structure of human epidermal growth factor (hEGF) at physiological pH and its interactions with suramin. Huang HW, Mohan SK, Yu C. Biochem Biophys Res Commun 402 705-710 (2010)
  128. The protein ERp57 contributes to EGF receptor signaling and internalization in MDA-MB-468 breast cancer cells. Gaucci E, Altieri F, Turano C, Chichiarelli S. J Cell Biochem 114 2461-2470 (2013)
  129. Androgen receptor in Sertoli cells regulates DNA double-strand break repair and chromosomal synapsis of spermatocytes partially through intercellular EGF-EGFR signaling. Chen SR, Hao XX, Zhang Y, Deng SL, Wang ZP, Wang YQ, Wang XX, Liu YX. Oncotarget 7 18722-18735 (2016)
  130. EGF receptor clustering is induced by a 0.4 mT power frequency magnetic field and blocked by the EGF receptor tyrosine kinase inhibitor PD153035. Jia C, Zhou Z, Liu R, Chen S, Xia R. Bioelectromagnetics 28 197-207 (2007)
  131. Signal transduction using an artificial receptor system that undergoes dimerization upon addition of a bivalent leucine-zipper ligand. Nakase I, Okumura S, Tanaka G, Osaki K, Imanishi M, Futaki S. Angew Chem Int Ed Engl 51 7464-7467 (2012)
  132. The membrane-proximal intracellular domain of the epidermal growth factor receptor underlies negative cooperativity in ligand binding. Adak S, Yang KS, Macdonald-Obermann J, Pike LJ. J Biol Chem 286 45146-45155 (2011)
  133. A truncated soluble epidermal growth factor receptor-Fc fusion ligand trap displays anti-tumour activity in vivo. Adams TE, Koziolek EJ, Hoyne PH, Bentley JD, Lu L, Lovrecz G, Ward CW, Lee FT, Scott AM, Nash AD, Rothacker J, Nice EC, Burgess AW, Johns TG. Growth Factors 27 141-154 (2009)
  134. Bipartite inhibition of Drosophila epidermal growth factor receptor by the extracellular and transmembrane domains of Kekkon1. Alvarado D, Rice AH, Duffy JB. Genetics 167 187-202 (2004)
  135. Resolving the EGF-EGFR interaction characteristics through a multiple-temperature, multiple-inhibitor, real-time interaction analysis approach. Björkelund H, Gedda L, Malmqvist M, Andersson K. Mol Clin Oncol 1 343-352 (2013)
  136. Structures of the HER2-HER3-NRG1β complex reveal a dynamic dimer interface. Diwanji D, Trenker R, Thaker TM, Wang F, Agard DA, Verba KA, Jura N. Nature 600 339-343 (2021)
  137. Whole exome sequencing to identify genetic markers for trastuzumab-induced cardiotoxicity. Udagawa C, Nakamura H, Ohnishi H, Tamura K, Shimoi T, Yoshida M, Yoshida T, Totoki Y, Shibata T, Zembutsu H. Cancer Sci 109 446-452 (2018)
  138. A structural model of the extracellular domain of the oncogenic EGFR variant Xmrk. Meierjohann S, Mueller T, Schartl M, Buehner M. Zebrafish 3 359-369 (2006)
  139. Lipid-Protein Interplay in Dimerization of Juxtamembrane Domains of Epidermal Growth Factor Receptor. Maeda R, Sato T, Okamoto K, Yanagawa M, Sako Y. Biophys J 114 893-903 (2018)
  140. Mechanism of Allosteric Coupling into and through the Plasma Membrane by EGFR. Sinclair JKL, Walker AS, Doerner AE, Schepartz A. Cell Chem Biol 25 857-870.e7 (2018)
  141. Plasma-Generated OH Radical Production for Analyzing Three-Dimensional Structure in Protein Therapeutics. Minkoff BB, Blatz JM, Choudhury FA, Benjamin D, Shohet JL, Sussman MR. Sci Rep 7 12946 (2017)
  142. Profiling epidermal growth factor receptor and heregulin receptor 3 heteromerization using receptor tyrosine kinase heteromer investigation technology. Ayoub MA, See HB, Seeber RM, Armstrong SP, Pfleger KD. PLoS One 8 e64672 (2013)
  143. A conformational sensor based on genetic code expansion reveals an autocatalytic component in EGFR activation. Baumdick M, Gelléri M, Uttamapinant C, Beránek V, Chin JW, Bastiaens PIH. Nat Commun 9 3847 (2018)
  144. Gemcitabine-loaded PLGA-PEG immunonanoparticles for targeted chemotherapy of pancreatic cancer. Aggarwal S, Gupta S, Pabla D, Murthy RS. Cancer Nanotechnol 4 145-157 (2013)
  145. Gene expression profiling of ErbB receptor and ligand-dependent transcription. Amin DN, Perkins AS, Stern DF. Oncogene 23 1428-1438 (2004)
  146. Orchestration of ErbB3 signaling through heterointeractions and homointeractions. McCabe Pryor M, Steinkamp MP, Halasz AM, Chen Y, Yang S, Smith MS, Zahoransky-Kohalmi G, Swift M, Xu XP, Hanein D, Volkmann N, Lidke DS, Edwards JS, Wilson BS. Mol Biol Cell 26 4109-4123 (2015)
  147. Overexpression-mediated activation of MET in the Golgi promotes HER3/ERBB3 phosphorylation. Frazier NM, Brand T, Gordan JD, Grandis J, Jura N. Oncogene 38 1936-1950 (2019)
  148. Palmitoylation of the EGF receptor impairs signal transduction and abolishes high-affinity ligand binding. Macdonald-Obermann JL, Pike LJ. Biochemistry 48 2505-2513 (2009)
  149. Quinone-induced Cdc25A inhibition causes ERK-dependent connexin phosphorylation. Melchheier I, von Montfort C, Stuhlmann D, Sies H, Klotz LO. Biochem Biophys Res Commun 327 1016-1023 (2005)
  150. Receptor clustering and activation by multivalent interaction through recognition peptides presented on exosomes. Nakase I, Ueno N, Katayama M, Noguchi K, Takatani-Nakase T, Kobayashi NB, Yoshida T, Fujii I, Futaki S. Chem Commun (Camb) 53 317-320 (2016)
  151. Suppression of heregulin β signaling by the single N-glycan deletion mutant of soluble ErbB3 protein. Takahashi M, Hasegawa Y, Ikeda Y, Wada Y, Tajiri M, Ariki S, Takamiya R, Nishitani C, Araki M, Yamaguchi Y, Taniguchi N, Kuroki Y. J Biol Chem 288 32910-32921 (2013)
  152. Allosteric regulation of epidermal growth factor (EGF) receptor ligand binding by tyrosine kinase inhibitors. Macdonald-Obermann JL, Pike LJ. J Biol Chem 293 13401-13414 (2018)
  153. Bad Tumors Made Worse: SPINK1. Mehner C, Radisky ES. Front Cell Dev Biol 7 10 (2019)
  154. Co-conserved features associated with cis regulation of ErbB tyrosine kinases. Mirza A, Mustafa M, Talevich E, Kannan N. PLoS One 5 e14310 (2010)
  155. Development of an epidermal growth factor derivative with EGFR blocking activity. Panosa C, Tebar F, Ferrer-Batallé M, Fonge H, Seno M, Reilly RM, Massaguer A, De Llorens R. PLoS One 8 e69325 (2013)
  156. EGFR forms ligand-independent oligomers that are distinct from the active state. Byrne PO, Hristova K, Leahy DJ. J Biol Chem 295 13353-13362 (2020)
  157. Functional and structural characterization of the kinase insert and the carboxy terminal domain in VEGF receptor 2 activation. Manni S, Kisko K, Schleier T, Missimer J, Ballmer-Hofer K. FASEB J 28 4914-4923 (2014)
  158. Ligand-assisted dual-site click labeling of EGFR on living cells. Yang Y, Lin S, Lin W, Chen PR. Chembiochem 15 1738-1743 (2014)
  159. Model-based analysis of HER activation in cells co-expressing EGFR, HER2 and HER3. Shankaran H, Zhang Y, Tan Y, Resat H. PLoS Comput Biol 9 e1003201 (2013)
  160. Th1 cytokines sensitize HER-expressing breast cancer cells to lapatinib. Showalter LE, Oechsle C, Ghimirey N, Steele C, Czerniecki BJ, Koski GK. PLoS One 14 e0210209 (2019)
  161. Ultrasound-Mediated EGF-Coated-Microbubble Cavitation in Dressings for Wound-Healing Applications. Liao AH, Hung CR, Chen HK, Chiang CP. Sci Rep 8 8327 (2018)
  162. Association of EGFR and HER2 polymorphisms with risk and clinical features of thyroid cancer. Rebaï M, Kallel I, Hamza F, Charfeddine S, Kaffel R, Guermazi F, Rebaï A. Genet Test Mol Biomarkers 13 779-784 (2009)
  163. Cell Derived Matrix Fibulin-1 Associates With Epidermal Growth Factor Receptor to Inhibit Its Activation, Localization and Function in Lung Cancer Calu-1 Cells. Harikrishnan K, Joshi O, Madangirikar S, Balasubramanian N. Front Cell Dev Biol 8 522 (2020)
  164. Cetuximab and biomarkers in non-small-cell lung carcinoma. Patil N, Abba M, Allgayer H. Biologics 6 221-231 (2012)
  165. Temperature-induced unfolding of epidermal growth factor (EGF): insight from molecular dynamics simulation. Yan C, Pattani V, Tunnell JW, Ren P. J Mol Graph Model 29 2-12 (2010)
  166. The ErbB4 extracellular region retains a tethered-like conformation in the absence of the tether. Liu P, Bouyain S, Eigenbrot C, Leahy DJ. Protein Sci 21 152-155 (2012)
  167. Blockade of a key region in the extracellular domain inhibits HER2 dimerization and signaling. Menendez JA, Schroeder B, Peirce SK, Vellon L, Papadimitropoulou A, Espinoza I, Lupu R. J Natl Cancer Inst 107 djv090 (2015)
  168. Dynamic transition states of ErbB1 phosphorylation predicted by spatial stochastic modeling. Pryor MM, Low-Nam ST, Halász AM, Lidke DS, Wilson BS, Edwards JS. Biophys J 105 1533-1543 (2013)
  169. Extracellular domain determinants of LET-23 (EGF) receptor tyrosine kinase activity in Caenorhabditis elegans. Moghal N, Sternberg PW. Oncogene 22 5471-5480 (2003)
  170. Insight into the recognition patterns of the ErbB receptor family transmembrane domains: heterodimerization models through molecular dynamics search. Samna Soumana O, Garnier N, Genest M. Eur Biophys J 37 851-864 (2008)
  171. Molecular dynamics (MD) investigations of preformed structures of the transmembrane domain of the oncogenic Neu receptor dimer in a DMPC bilayer. Aller P, Voiry L, Garnier N, Genest M. Biopolymers 77 184-197 (2005)
  172. Negative co-operativity in the EGF receptor. Pike LJ. Biochem Soc Trans 40 15-19 (2012)
  173. Peptides Targeting EGF Block the EGF-EGFR Interaction. Guardiola S, Díaz-Lobo M, Seco J, García J, Nevola L, Giralt E. Chembiochem 17 702-711 (2016)
  174. Polymorphism of the epidermal growth factor receptor extracellular ligand binding domain: the dimer interface depends on domain stabilization. Zhang Z, Wriggers W. Biochemistry 50 2144-2156 (2011)
  175. The signaling and transformation potency of the overexpressed HER2 protein is dependent on the normally-expressed EGFR. Zhou X, Agazie YM. Cell Signal 24 140-150 (2012)
  176. Analysis of Interactions between the Epidermal Growth Factor Receptor and Soluble Ligands on the Basis of Single-Molecule Diffusivity in the Membrane of Living Cells. Kim DH, Zhou K, Kim DK, Park S, Noh J, Kwon Y, Kim D, Song NW, Lee JB, Suh PG, Lee NK, Ryu SH. Angew Chem Int Ed Engl 54 7028-7032 (2015)
  177. BCAP31 drives TNBC development by modulating ligand-independent EGFR trafficking and spontaneous EGFR phosphorylation. Fu W, Sun H, Zhao Y, Chen M, Yang X, Liu Y, Jin W. Theranostics 9 6468-6484 (2019)
  178. Increased expression of the integral membrane protein ErbB2 in Chinese hamster ovary cells expressing the anti-apoptotic gene Bcl-xL. O'Connor S, Li E, Majors BS, He L, Placone J, Baycin D, Betenbaugh MJ, Hristova K. Protein Expr Purif 67 41-47 (2009)
  179. Interaction and molecular dynamics simulation study of Osimertinib (AstraZeneca 9291) anticancer drug with the EGFR kinase domain in native protein and mutated L844V and C797S. Assadollahi V, Rashidieh B, Alasvand M, Abdolahi A, Lopez JA. J Cell Biochem 120 13046-13055 (2019)
  180. Microplate-compatible total internal reflection fluorescence microscopy for receptor pharmacology. Chen M, Zaytseva NV, Wu Q, Li M, Fang Y. Appl Phys Lett 102 193702 (2013)
  181. N-glycosylated GPNMB ligand independently activates mutated EGFR signaling and promotes metastasis in NSCLC. Han CL, Chen XR, Lan A, Hsu YL, Wu PS, Hung PF, Hung CL, Pan SH. Cancer Sci 112 1911-1923 (2021)
  182. Phe45 of NRG2beta is critical for the affinity of NRG2beta for ErbB4 and for potent stimulation of ErbB4 signaling by NRG2beta*. Hobbs SS, Gallo RM, Riese DJ. Growth Factors 23 273-283 (2005)
  183. Regulation of the Drosophila epidermal growth factor-ligand vein is mediated by multiple domains. Donaldson T, Wang SH, Jacobsen TL, Schnepp B, Price J, Simcox A. Genetics 167 687-698 (2004)
  184. Screening and discovery of nitro-benzoxadiazole compounds activating epidermal growth factor receptor (EGFR) in cancer cells. Sakanyan V, Angelini M, Le Béchec M, Lecocq MF, Benaiteau F, Rousseau B, Gyulkhandanyan A, Gyulkhandanyan L, Logé C, Reiter E, Roussakis C, Fleury F. Sci Rep 4 3977 (2014)
  185. Size and conformational features of ErbB2 and ErbB3 receptors: a TEM and DLS comparative study. Vicente-Alique E, Núñez-Ramírez R, Vega JF, Hu P, Martínez-Salazar J. Eur Biophys J 40 835-842 (2011)
  186. The membrane proximal disulfides of the EGF receptor extracellular domain are required for high affinity binding and signal transduction but do not play a role in the localization of the receptor to lipid rafts. Macdonald J, Li Z, Su W, Pike LJ. Biochim Biophys Acta 1763 870-878 (2006)
  187. Trastuzumab Blocks the Receiver Function of HER2 Leading to the Population Shifts of HER2-Containing Homodimers and Heterodimers. Zhao J, Mohan N, Nussinov R, Ma B, Wu WJ. Antibodies (Basel) 10 7 (2021)
  188. Asp-960/Glu-961 controls the movement of the C-terminal tail of the epidermal growth factor receptor to regulate asymmetric dimer formation. Yang KS, Macdonald-Obermann JL, Piwnica-Worms D, Pike LJ. J Biol Chem 285 24014-24022 (2010)
  189. Autophosphorylation activation and inhibition by curcumin of the epidermal growth factor receptor reconstituted in liposomes. Doumiati S, Haupt K, Rossi C. J Mol Recognit 25 623-629 (2012)
  190. Blocking EGFR Activation with Anti-EGF Nanobodies via Two Distinct Molecular Recognition Mechanisms. Guardiola S, Varese M, Sánchez-Navarro M, Vincke C, Teixidó M, García J, Muyldermans S, Giralt E. Angew Chem Int Ed Engl 57 13843-13847 (2018)
  191. Direct interaction of avermectin with epidermal growth factor receptor mediates the penetration resistance in Drosophila larvae. Chen LP, Wang P, Sun YJ, Wu YJ. Open Biol 6 150231 (2016)
  192. Growth factor receptors and apoptosis regulators: signaling pathways, prognosis, chemosensitivity and treatment outcomes of breast cancer. Sarkar S, Mandal M. Breast Cancer (Auckl) 3 47-60 (2009)
  193. Modulating the structure of EGFR with UV light: new possibilities in cancer therapy. Correia M, Thiagarajan V, Coutinho I, Gajula GP, Petersen SB, Neves-Petersen MT. PLoS One 9 e111617 (2014)
  194. Molecular Mechanisms that Regulate Epidermal Growth Factor Receptor Inactivation. Ceresa BP, Vanlandingham PA. Clin Med Oncol 2 47-61 (2008)
  195. Optics clustered to output unique solutions: a multi-laser facility for combined single molecule and ensemble microscopy. Clarke DT, Botchway SW, Coles BC, Needham SR, Roberts SK, Rolfe DJ, Tynan CJ, Ward AD, Webb SE, Yadav R, Zanetti-Domingues L, Martin-Fernandez ML. Rev Sci Instrum 82 093705 (2011)
  196. Single-Molecule Fluorescence Detection of the Epidermal Growth Factor Receptor in Membrane Discs. Quinn SD, Srinivasan S, Gordon JB, He W, Carraway KL, Coleman MA, Schlau-Cohen GS. Biochemistry 58 286-294 (2019)
  197. Surfactant protein A down-regulates epidermal growth factor receptor by mechanisms different from those of surfactant protein D. Hasegawa Y, Takahashi M, Ariki S, Saito A, Uehara Y, Takamiya R, Kuronuma K, Chiba H, Sakuma Y, Takahashi H, Kuroki Y. J Biol Chem 292 18565-18576 (2017)
  198. Transmembrane helix packing of ErbB/Neu receptor in membrane environment: a molecular dynamics study. Aller P, Garnier N, Genest M. J Biomol Struct Dyn 24 209-228 (2006)
  199. B-cell epitope peptide vaccination targeting dimer interface of epidermal growth factor receptor (EGFR). Zhu L, Zhao L, Wu M, Chen Z, Li H. Immunol Lett 153 33-40 (2013)
  200. EGFR-Binding Peptides: From Computational Design towards Tumor-Targeting of Adeno-Associated Virus Capsids. Feiner RC, Kemker I, Krutzke L, Allmendinger E, Mandell DJ, Sewald N, Kochanek S, Müller KM. Int J Mol Sci 21 E9535 (2020)
  201. High-throughput de novo screening of receptor agonists with an automated single-cell analysis and isolation system. Yoshimoto N, Tatematsu K, Iijima M, Niimi T, Maturana AD, Fujii I, Kondo A, Tanizawa K, Kuroda S. Sci Rep 4 4242 (2014)
  202. Investigating Molecular Mechanisms of Activation and Mutation of the HER2 Receptor Tyrosine Kinase through Computational Modeling and Simulation. Telesco SE, Shih A, Liu Y, Radhakrishnan R. Cancer Res J 4 1-35 (2011)
  203. Lectin PCL inhibits the Warburg effect of PC3 cells by combining with EGFR and inhibiting HK2. Zhang H, Du X, Sun TT, Wang CL, Li Y, Wu SZ. Oncol Rep 37 1765-1771 (2017)
  204. Ligand-Independent EGFR Activation by Anchorage-Stimulated Src Promotes Cancer Cell Proliferation and Cetuximab Resistance via ErbB3 Phosphorylation. Nozaki M, Yasui H, Ohnishi Y. Cancers (Basel) 11 E1552 (2019)
  205. Old dog, new tricks: extracellular domain arginine methylation regulates EGFR function. Epstein DM, Buck E. J Clin Invest 125 4320-4322 (2015)
  206. Protein-protein interactions between SWCNT/chitosan/EGF and EGF receptor: a model of drug delivery system. Rungnim C, Rungrotmongkol T, Kungwan N, Hannongbua S. J Biomol Struct Dyn 34 1919-1929 (2016)
  207. Rational optimization of a bispecific ligand trap targeting EGF receptor family ligands. Jin P, Zhang J, Beryt M, Turin L, Brdlik C, Feng Y, Bai X, Liu J, Jorgensen B, Shepard HM. Mol Med 15 11-20 (2009)
  208. Rigidity of the extracellular part of HER2: Evidence from engineering subdomain interfaces and shared-helix DARPin-DARPin fusions. Jost C, Stüber JC, Honegger A, Wu Y, Batyuk A, Plückthun A. Protein Sci 26 1796-1806 (2017)
  209. Autophosphorylation of EGFR at Y954 Facilitated Homodimerization and Enhanced Downstream Signals. Thirukkumaran OM, Kluba M, Hofkens J, Mizuno H. Biophys J 119 2127-2137 (2020)
  210. Conformational flexibility of the ErbB2 ectodomain and trastuzumab antibody complex as revealed by molecular dynamics and principal component analysis. Franco-Gonzalez JF, Cruz VL, Ramos J, Martínez-Salazar J. J Mol Model 19 1227-1236 (2013)
  211. Effect of acute acid-base disturbances on ErbB1/2 tyrosine phosphorylation in rabbit renal proximal tubules. Skelton LA, Boron WF. Am J Physiol Renal Physiol 305 F1747-64 (2013)
  212. Investigating extracellular in situ EGFR structure and conformational changes using FRET microscopy. Roberts SK, Tynan CJ, Winn M, Martin-Fernandez ML. Biochem Soc Trans 40 189-194 (2012)
  213. Real-Time Sensing of Single-Ligand Delivery with Nanoaperture-Integrated Microfluidic Devices. Martin WE, Ge N, Srijanto BR, Furnish E, Collier CP, Trinkle CA, Richards CI. ACS Omega 2 3858-3867 (2017)
  214. Simulation of homology models for the extracellular domains (ECD) of ErbB3, ErbB4 and the ErbB2-ErbB3 complex in their active conformations. Franco-Gonzalez JF, Ramos J, Cruz VL, Martínez-Salazar J. J Mol Model 19 931-941 (2013)
  215. UBTD1 regulates ceramide balance and endolysosomal positioning to coordinate EGFR signaling. Torrino S, Tiroille V, Dolfi B, Dufies M, Hinault C, Bonesso L, Dagnino S, Uhler J, Irondelle M, Gay AS, Fleuriot L, Debayle D, Lacas-Gervais S, Cormont M, Bertero T, Bost F, Gilleron J, Clavel S. Elife 10 e68348 (2021)
  216. A Generic Strategy to Generate Bifunctional Two-in-One Antibodies by Chicken Immunization. Harwardt J, Bogen JP, Carrara SC, Ulitzka M, Grzeschik J, Hock B, Kolmar H. Front Immunol 13 888838 (2022)
  217. A bispecific transmembrane antibody simultaneously targeting intra- and extracellular epitopes of the epidermal growth factor receptor inhibits receptor activation and tumor cell growth. Müller N, Hartmann C, Genssler S, Koch J, Kinner A, Grez M, Wels WS. Int J Cancer 134 2547-2559 (2014)
  218. Adaptive coarse-grained Monte Carlo simulation of reaction and diffusion dynamics in heterogeneous plasma membranes. Collins S, Stamatakis M, Vlachos DG. BMC Bioinformatics 11 218 (2010)
  219. Computational design of binding proteins to EGFR domain II. Choi YS, Yoon S, Kim KL, Yoo J, Song P, Kim M, Shin YE, Yang WJ, Noh JE, Cho HS, Kim S, Chung J, Ryu SH. PLoS One 9 e92513 (2014)
  220. Critical roles for EGFR and EGFR-HER2 clusters in EGF binding of SW620 human carcinoma cells. Wollman AJM, Fournier C, Llorente-Garcia I, Harriman O, Payne-Dwyer AL, Shashkova S, Zhou P, Liu TC, Ouaret D, Wilding J, Kusumi A, Bodmer W, Leake MC. J R Soc Interface 19 20220088 (2022)
  221. Deciphering the stepwise binding mode of HRG1β to HER3 by surface plasmon resonance and interaction map. Peess C, von Proff L, Goller S, Andersson K, Gerg M, Malmqvist M, Bossenmaier B, Schräml M. PLoS One 10 e0116870 (2015)
  222. Development of a Nanostructured Platform for Identifying HER2-Heterogeneity of Breast Cancer Cells by Surface-Enhanced Raman Scattering. Téllez-Plancarte A, Haro-Poniatowski E, Picquart M, Morales-Méndez JG, Lara-Cruz C, Jiménez-Salazar JE, Damián-Matsumura P, Escobar-Alarcón L, Batina N. Nanomaterials (Basel) 8 E549 (2018)
  223. Gatekeeper tyrosine phosphorylation is autoinhibitory for Symbiosis Receptor Kinase. Paul A, Samaddar S, Bhattacharya A, Banerjee A, Das A, Chakrabarti S, DasGupta M. FEBS Lett 588 2881-2889 (2014)
  224. Ligand binding effects on the activation of the EGFR extracellular domain. Shao Q, Zhu W. Phys Chem Chem Phys 21 8141-8151 (2019)
  225. Molecular dynamics simulations of transitions for ECD epidermal growth factor receptors show key differences between human and drosophila forms of the receptors. Perilla JR, Leahy DJ, Woolf TB. Proteins 81 1113-1126 (2013)
  226. Nectin-like molecule-4/cell adhesion molecule 4 inhibits the ligand-induced dimerization of ErbB3 with ErbB2. Mizutani K, Kedashiro S, Maruoka M, Ueda Y, Takai Y. Sci Rep 7 11375 (2017)
  227. Quantification of ErbB3 receptor density on human breast cancer cells, using a stable radio-labeled mutant of NRG1beta. van der Woning SP, van Zoelen EJ. Biochem Biophys Res Commun 378 285-289 (2009)
  228. Structural Basis for the Functional Changes by EGFR Exon 20 Insertion Mutations. Tamirat MZ, Kurppa KJ, Elenius K, Johnson MS. Cancers (Basel) 13 1120 (2021)
  229. Structure of HER receptors and intracellular localisation of downstream effector elements gives insight into mechanism of tumour growth promotion. Witton CJ. Breast Cancer Res 5 206-207 (2003)
  230. The kinetics of the hydrogen/deuterium exchange of epidermal growth factor receptor ligands. Iloro I, Narváez D, Guillén N, Camacho CM, Guillén L, Cora E, Pastrana-Ríos B. Biophys J 94 4041-4055 (2008)
  231. mAb806 binding to epidermal growth factor receptor: a computational study. Ng YZ, Kannan S, Lane DP, Fuentes G, Verma CS. Proteins 83 153-168 (2015)
  232. Compounds identified by virtual docking to a tetrameric EGFR extracellular domain can modulate Grb2 internalization. Ramirez UD, Nikonova AS, Liu H, Pecherskaya A, Lawrence SH, Serebriiskii IG, Zhou Y, Robinson MK, Einarson MB, Golemis EA, Jaffe EK. BMC Cancer 15 436 (2015)
  233. Effects of replacement and addition of an amino acid contained in a cyclic peptide corresponding to a β-hairpin loop sequence of human EGF receptor. Kobayashi K, Mizuguchi T, Hattori Y, Ohara N, Ninomiya R, Iida M, Ooe H, Yamazaki Y, Takata M, Tamamura H, Akaji K. J Pept Sci 23 581-586 (2017)
  234. Extracellular Juxtamembrane Motif Critical for TrkB Preformed Dimer and Activation. Shen J, Sun D, Shao J, Chen Y, Pang K, Guo W, Lu B. Cells 8 E932 (2019)
  235. Glycosylation promotes the cancer regulator EGFR-ErbB2 heterodimer formation - molecular dynamics study. Motamedi Z, Rajabi-Maham H, Azimzadeh Irani M. J Mol Model 27 361 (2021)
  236. Human epidermal growth factor receptor (HER1) aligned on the plasma membrane adopts key features of Drosophila EGFR asymmetry. Martin-Fernandez ML. Biochem Soc Trans 40 184-188 (2012)
  237. Identification of a novel antagonist of the ErbB1 receptor capable of inhibiting migration of human glioblastoma cells. Staberg M, Riemer C, Xu R, Dmytriyeva O, Bock E, Berezin V. Cell Oncol (Dordr) 36 201-211 (2013)
  238. Novel Pituitary Actions of Epidermal Growth Factor: Receptor Specificity and Signal Transduction for UTS1, EGR1, and MMP13 Regulation by EGF. Hu Q, Xu S, Ye C, Jia J, Zhou L, Hu G. Int J Mol Sci 20 E5172 (2019)
  239. Photon-Induced Near-Field Electron Microscopy of Eukaryotic Cells. Kaplan M, Yoo BK, Tang J, Karam TE, Liao B, Majumdar D, Baltimore D, Jensen GJ, Zewail AH. Angew Chem Int Ed Engl 56 11498-11501 (2017)
  240. ROR and RYK extracellular region structures suggest that receptor tyrosine kinases have distinct WNT-recognition modes. Shi F, Mendrola JM, Sheetz JB, Wu N, Sommer A, Speer KF, Noordermeer JN, Kan ZY, Perry K, Englander SW, Stayrook SE, Fradkin LG, Lemmon MA. Cell Rep 37 109834 (2021)
  241. Structural insights into the non-inhibitory mechanism of the anti-EGFR EgB4 nanobody. Zeronian MR, Doulkeridou S, van Bergen En Henegouwen PMP, Janssen BJC. BMC Mol Cell Biol 23 12 (2022)
  242. Theme: oncology--molecular mechanisms determining the efficacy of EGF receptor-specific tyrosine kinase inhibitors help to identify biomarker candidates. Yamauchi M, Gotoh N. Biomark Med 3 139-151 (2009)
  243. pH dependence of ligand-induced human epidermal growth factor receptor activation investigated by molecular dynamics simulations. Dong J, Zhang Y, Zhang Z. J Mol Model 22 131 (2016)
  244. Functional genomic characterization of a synthetic anti-HER3 antibody reveals a role for ubiquitination by RNF41 in the anti-proliferative response. Turowec JP, Lau EWT, Wang X, Brown KR, Fellouse FA, Jawanda KK, Pan J, Moffat J, Sidhu SS. J Biol Chem 294 1396-1409 (2019)
  245. Generation and Characterization of Rat Monoclonal Antibodies Against Epidermal Growth Factor Receptor. Osaki T, Wang CX, Tachibana T, Azuma M, Kitamura M, Nakanishi T. Monoclon Antib Immunodiagn Immunother 34 418-422 (2015)
  246. Hybrid Pharmacophore- and Structure-Based Virtual Screening Pipeline to Identify Novel EGFR Inhibitors That Suppress Non-Small Cell Lung Cancer Cell Growth. Weng CW, Wei CH, Tsai JY, Lai YH, Chang GC, Chen JJW. Int J Mol Sci 23 3487 (2022)
  247. Identification of EGFR as a Biomarker in Saliva and Buccal Cells from Oral Submucous Fibrosis Patients-A Baseline Study. Moorthy A, Venugopal DC, Shyamsundar V, Madhavan Y, Ravindran S, Kuppuloganathan M, Krishnamurthy A, Sankarapandian S, Ganapathy V, Ramshankar V. Diagnostics (Basel) 12 1935 (2022)
  248. In Silico Evaluation of Variable pH on the Binding of Epidermal Growth Factor Receptor Ectodomain to its Ligand Through Molecular Dynamics Simulation in Tumors. Singh I, Singh G, Verma V, Singh S, Chandra R. Interdiscip Sci 11 437-443 (2019)
  249. Potential of Epidermal Growth Factor-like Peptide from the Sea Cucumber Stichopus horrens to Increase the Growth of Human Cells: In Silico Molecular Docking Approach. Pilus NSM, Muhamad A, Shahidan MA, Yusof NYM. Mar Drugs 20 596 (2022)
  250. Probing the Anti-Cancer Potency of Sulfated Galactans on Cholangiocarcinoma Cells Using Synchrotron FTIR Microspectroscopy, Molecular Docking, and In Vitro Studies. Boonsri B, Choowongkomon K, Kuaprasert B, Thitiphatphuvanon T, Supradit K, Sayinta A, Duangdara J, Rudtanatip T, Wongprasert K. Mar Drugs 19 258 (2021)
  251. Restoration of microRNA-130b expression suppresses osteosarcoma cell malignant behavior in vitro. Wu Y, Sun W, Kong Y, Liu B, Zeng M, Wang W. Oncol Lett 16 97-104 (2018)
  252. News A monkey wrench in the kinase machine. Leahy DJ. Nat Struct Mol Biol 14 1120-1121 (2007)
  253. Cancer regulator EGFR-ErbB4 heterodimer is stabilized through glycans at the dimeric interface. Motamedi Z, Shahsavari M, Rajabi-Maham H, Azimzadeh Irani M. J Mol Model 28 399 (2022)
  254. Confinement of unliganded EGFR by tetraspanin nanodomains gates EGFR ligand binding and signaling. Sugiyama MG, Brown AI, Vega-Lugo J, Borges JP, Scott AM, Jaqaman K, Fairn GD, Antonescu CN. Nat Commun 14 2681 (2023)
  255. Development of 177Lu-Cetuximab-PAMAM dendrimeric nanosystem: a novel theranostic radioimmunoconjugate. Hosseini SM, Mohammadnejad J, Yousefnia H, Alirezapour B, Rezayan AH. J Cancer Res Clin Oncol 149 7779-7791 (2023)
  256. Development of Cyclic Peptides Targeting the Epidermal Growth Factor Receptor in Mesenchymal Triple-Negative Breast Cancer Subtype. Nisticò N, Aloisio A, Lupia A, Zimbo AM, Mimmi S, Maisano D, Russo R, Marino F, Scalise M, Chiarella E, Mancuso T, Fiume G, Omodei D, Zannetti A, Salvatore G, Quinto I, Iaccino E. Cells 12 1078 (2023)
  257. Efficient expression, purification, and visualization by cryo-EM of unliganded near full-length HER3. Diwanji D, Trenker R, Jura N, Verba KA. Methods Enzymol 667 611-632 (2022)
  258. Elucidating activation and deactivation dynamics of VEGFR-2 transmembrane domain with coarse-grained molecular dynamics simulations. Go YJ, Kalathingal M, Rhee YM. PLoS One 18 e0281781 (2023)
  259. Equilibrium Between Dimeric and Monomeric Forms of Human Epidermal Growth Factor is Shifted Towards Dimers in a Solution. Akunevich AA, Khrustalev VV, Khrustaleva TA, Poboinev VV, Shalygo NV, Stojarov AN, Arutyunyan AM, Kordyukova LV, Sapon YG. Protein J 41 245-259 (2022)
  260. Folding of Staphylococcal Nuclease Induced by Binding of Chemically Modified Substrate Analogues Sheds Light on Mechanisms of Coupled Folding/Binding Reactions. Mori Y, Mizukami T, Segawa S, Roder H, Maki K. Biochemistry 62 1670-1678 (2023)
  261. PDGFR dimer-specific activation, trafficking and downstream signaling dynamics. Rogers MA, Campaña MB, Long R, Fantauzzo KA. J Cell Sci 135 jcs259686 (2022)
  262. Piptides: New, Easily Accessible Chemotypes For Interactions With Biomolecules. Arancillo M, Taechalertpaisarn J, Liang X, Burgess K. Angew Chem Int Ed Engl 60 6653-6659 (2021)
  263. Probabilistic edge weights fine-tune Boolean network dynamics. Deritei D, Kunšič N, Csermely P. PLoS Comput Biol 18 e1010536 (2022)
  264. Selecting Nanobodies Specific for the Epidermal Growth Factor from a Synthetic Nanobody Library. Serrano-Rivero Y, Salazar-Uribe J, Rubio-Carrasquilla M, Camacho-Casanova F, Sánchez-Ramos O, González-Pose A, Moreno E. Molecules 28 4043 (2023)
  265. Congress Spotlight on cellular signaling. Marshall C, Müller-Esterl W. Mol Cell 15 849-852 (2004)


Quick links