The epidermal growth factor receptor family.

The epidermal growth factor receptor family consists of four receptor genes and at least 11 ligands, several of which are produced in different protein forms. They create an interacting system that has the ability to receive and process information that results in multiple outputs. The family has an important role in directing and coordinating many normal processes, including growth and development, normal tissue turnover and wound healing. Its members are also aberrantly activated by overexpression or mutation in many common human tumour types and as such have been the target for anticancer drug development.

[1]  W. Gullick,et al.  Identification of c‐erbB‐3 binding sites for phosphatidylinositol 3′‐kinase and SHC using an EGF receptor/c‐erbB‐3 chimera. , 1994, The EMBO journal.

[2]  D. Osoba,et al.  Health-related quality of life in women with metastatic breast cancer treated with trastuzumab (Herceptin). , 1999, Seminars in oncology.

[3]  D. Engelman,et al.  Two EGF molecules contribute additively to stabilization of the EGFR dimer , 1997, The EMBO journal.

[4]  M. Sliwkowski,et al.  Axon-induced mitogenesis of human Schwann cells involves heregulin and p185erbB2. , 1995, Proceedings of the National Academy of Sciences of the United States of America.

[5]  A. M. Stanley,et al.  Structure of the extracellular region of HER 2 alone and in complex with the Herceptin Fab , 2022 .

[6]  S. Hubbard,et al.  Protein tyrosine kinase structure and function. , 2000, Annual review of biochemistry.

[7]  C R King,et al.  erbB-2 is a potent oncogene when overexpressed in NIH/3T3 cells. , 1987, Science.

[8]  A. Ullrich,et al.  Heregulin‐dependent regulation of HER2/neu oncogenic signaling by heterodimerization with HER3. , 1995, The EMBO journal.

[9]  G. Carpenter,et al.  All ErbB Receptors Other Than the Epidermal Growth Factor Receptor Are Endocytosis Impaired (*) , 1996, The Journal of Biological Chemistry.

[10]  A. Lenferink,et al.  ErbB2/neu kinase modulates cellular p27(Kip1) and cyclin D1 through multiple signaling pathways. , 2001, Cancer research.

[11]  G. Carpenter,et al.  Epidermal growth factor stimulates phosphorylation in membrane preparations in vitro , 1978, Nature.

[12]  T. Pawson,et al.  The PTB domain: a new protein module implicated in signal transduction. , 1995, Trends in biochemical sciences.

[13]  Colin G. Johnson,et al.  Simulating complex intracellular processes using object-oriented computational modelling. , 2004, Progress in biophysics and molecular biology.

[14]  Antony W Burgess,et al.  Epidermal growth factor receptor: mechanisms of activation and signalling. , 2003, Experimental cell research.

[15]  Y. Yarden,et al.  Coupling of the c-Cbl protooncogene product to ErbB-1/EGF-receptor but not to other ErbB proteins. , 1996, Oncogene.

[16]  Y. Yarden,et al.  A single autophosphorylation site confers oncogenicity to the Neu/ErbB‐2 receptor and enables coupling to the MAP kinase pathway. , 1994, The EMBO journal.

[17]  L. Cantley,et al.  A neu acquaintance for ErbB3 and ErbB4: A role for receptor heterodimerization in growth signaling , 1994, Cell.

[18]  J. Schlessinger,et al.  Activation of phospholipase Cγ by PI 3‐kinase‐induced PH domain‐mediated membrane targeting , 1998 .

[19]  T. Pawson,et al.  Signaling through scaffold, anchoring, and adaptor proteins. , 1997, Science.

[20]  B. Margolis,et al.  Proteins with SH2 domains: transducers in the tyrosine kinase signaling pathway. , 1992, Cell growth & differentiation : the molecular biology journal of the American Association for Cancer Research.

[21]  M. Sternberg,et al.  A sequence motif in the transmembrane region of growth factor receptors with tyrosine kinase activity mediates dimerization. , 1990, Protein engineering.

[22]  Y. Yarden,et al.  The basic biology of HER2. , 2001, Annals of oncology : official journal of the European Society for Medical Oncology.

[23]  W. Gullick,et al.  Neu receptor dimerization , 1989, Nature.

[24]  Rainer Pepperkok,et al.  Intracellular Movement of Green Fluorescent Protein–Tagged Phosphatidylinositol 3-Kinase in Response to Growth Factor Receptor Signaling , 1999, The Journal of cell biology.

[25]  Jae-Hoon Kim,et al.  Crystal Structure of the Complex of Human Epidermal Growth Factor and Receptor Extracellular Domains , 2002, Cell.

[26]  J. Taylor‐Papadimitriou,et al.  Collagen-induced morphogenesis and expression of the alpha 2-integrin subunit is inhibited in c-erbB2-transfected human mammary epithelial cells. , 1993, Oncogene.

[27]  Y Yarden,et al.  An oncogenic point mutation confers high affinity ligand binding to the neu receptor. Implications for the generation of site heterogeneity. , 1992, The Journal of biological chemistry.

[28]  I. Lax,et al.  Real-time measurements of kinetics of EGF binding to soluble EGF receptor monomers and dimers support the dimerization model for receptor activation. , 1993, Biochemistry.

[29]  C. Mol,et al.  Switching on kinases: oncogenic activation of BRAF and the PDGFR family , 2004, Nature Reviews Cancer.

[30]  Yosef Yarden,et al.  Molecular mechanisms underlying ErbB2/HER2 action in breast cancer , 2000, Oncogene.

[31]  S. Higashiyama,et al.  Neuroglycan C, a novel member of the neuregulin family. , 2004, Biochemical and biophysical research communications.

[32]  P. Seeburg,et al.  Tyrosine kinase receptor with extensive homology to EGF receptor shares chromosomal location with neu oncogene. , 1985, Science.

[33]  S. Sharpe,et al.  Val(659)-->Glu mutation within the transmembrane domain of ErbB-2: effects measured by (2)H NMR in fluid phospholipid bilayers. , 2000, Biochemistry.

[34]  John M. Daly,et al.  ErbB2 Potentiates Breast Tumor Proliferation through Modulation of p27Kip1-Cdk2 Complex Formation: Receptor Overexpression Does Not Determine Growth Dependency , 2000, Molecular and Cellular Biology.

[35]  G. Carpenter.  The EGF receptor: a nexus for trafficking and signaling , 2000, BioEssays : news and reviews in molecular, cellular and developmental biology.

[36]  Y. Yarden,et al.  The ErbB signaling network in embryogenesis and oncogenesis: signal diversification through combinatorial ligand‐receptor interactions , 1997, FEBS letters.

[37]  J. Chou,et al.  Reciprocal changes in p27(Kip1) and p21(Cip1) in growth inhibition mediated by blockade or overstimulation of epidermal growth factor receptors. , 1997, Clinical cancer research : an official journal of the American Association for Cancer Research.

[38]  Y. Yarden,et al.  Differential expression of NDF/neuregulin receptors ErbB-3 and ErbB-4 and involvement in inhibition of neuronal differentiation , 1997, Oncogene.

[39]  Jun Yao,et al.  Overexpression of ErbB2 blocks Taxol-induced apoptosis by upregulation of p21Cip1, which inhibits p34Cdc2 kinase. , 1998, Molecular cell.

[40]  W. Gullick,et al.  The Type 1 growth factor receptors and their ligands considered as a complex system. , 2001, Endocrine-related cancer.

[41]  Y. Yarden,et al.  Roles for a Cytoplasmic Tyrosine and Tyrosine Kinase Activity in the Interactions of Neu Receptors with Coated Pits (*) , 1995, The Journal of Biological Chemistry.

[42]  K. Carraway,et al.  Ligand discrimination by ErbB receptors: differential signaling through differential phosphorylation site usage , 2000, Oncogene.

[43]  L. Cantley,et al.  Differential Signaling by the Epidermal Growth Factor-like Growth Factors Neuregulin-1 and Neuregulin-2* , 1998, The Journal of Biological Chemistry.

[44]  T Pawson,et al.  SH2 and SH3 domains , 1993, Current Biology.

[45]  G. Carpenter,et al.  EGF-dependent translocation of green fluorescent protein-tagged PLC-gamma1 to the plasma membrane and endosomes. , 2001, Experimental cell research.

[46]  Tianhua Niu,et al.  Pin1 is overexpressed in breast cancer and cooperates with Ras signaling in increasing the transcriptional activity of c‐Jun towards cyclin D1 , 2001, The EMBO journal.

[47]  Y. Yarden,et al.  Cyclin D1 Is Required for Transformation by Activated Neu and Is Induced through an E2F-Dependent Signaling Pathway , 2000, Molecular and Cellular Biology.

[48]  R. Neve,et al.  Effects of oncogenic ErbB2 on G1 cell cycle regulators in breast tumour cells , 2000, Oncogene.

[49]  P. Sternberg,et al.  Multiple positive and negative regulators of signaling by the EGF-receptor. , 1999, Current opinion in cell biology.

[50]  Y. Yarden,et al.  A hierarchical network of interreceptor interactions determines signal transduction by Neu differentiation factor/neuregulin and epidermal growth factor , 1996, Molecular and cellular biology.

[51]  P. W. Janes,et al.  Inhibition of the MAP kinase cascade blocks heregulin-induced cell cycle progression in T-47D human breast cancer cells , 1998, Oncogene.

[52]  W. Dougall,et al.  Ligand and p185c-neu density govern receptor interactions and tyrosine kinase activation. , 1994, Proceedings of the National Academy of Sciences of the United States of America.

[53]  Y. Yarden,et al.  The ErbB-2/HER2 oncoprotein of human carcinomas may function solely as a shared coreceptor for multiple stroma-derived growth factors. , 1999, Proceedings of the National Academy of Sciences of the United States of America.

[54]  N. Lemoine,et al.  The erbB‐3 Gene in human pancreatic cancer , 1992, The Journal of pathology.

[55]  D. Robinson,et al.  The protein tyrosine kinase family of the human genome , 2000, Oncogene.

[56]  Douglas L Falls,et al.  Neuregulins: functions, forms, and signaling strategies. , 2003, Experimental cell research.

[57]  Yosef Yarden,et al.  A subclass of tumor-inhibitory monoclonal antibodies to ErbB-2/HER2 blocks crosstalk with growth factor receptors , 1997, Oncogene.

[58]  S. White,et al.  Membrane protein folding and stability: physical principles. , 1999, Annual review of biophysics and biomolecular structure.

[59]  Hyun-soo Cho,et al.  EGF activates its receptor by removing interactions that autoinhibit ectodomain dimerization. , 2003, Molecular cell.

[60]  Lin Yz,et al.  A soluble protein related to the HER-2 proto-oncogene product is released from human breast carcinoma cells. , 1991 .

[61]  Alessandro Senes,et al.  The Cα—H⋅⋅⋅O hydrogen bond: A determinant of stability and specificity in transmembrane helix interactions , 2001, Proceedings of the National Academy of Sciences of the United States of America.

[62]  B. Margolis.  The PTB Domain: The Name Doesn't Say It All , 1999, Trends in Endocrinology & Metabolism.

[63]  B. Bormann,et al.  Strong hydrogen bonding interactions involving a buried glutamic acid in the transmembrane sequence of the neu/erbB-2 receptor , 1996, Nature Structural Biology.

[64]  J. Doherty,et al.  NH2-terminally truncated HER-2/neu protein: relationship with shedding of the extracellular domain and with prognostic factors in breast cancer. , 1998, Cancer research.

[65]  H. Wiley,et al.  The Enhanced Tumorigenic Activity of a Mutant Epidermal Growth Factor Receptor Common in Human Cancers Is Mediated by Threshold Levels of Constitutive Tyrosine Phosphorylation and Unattenuated Signaling* , 1997, The Journal of Biological Chemistry.

[66]  Y. Yarden,et al.  Epidermal growth factor induces rapid, reversible aggregation of the purified epidermal growth factor receptor. , 1987, Biochemistry.

[67]  A. Ullrich,et al.  Functional analysis of the ligand binding site of EGF‐receptor utilizing chimeric chicken/human receptor molecules. , 1989, The EMBO journal.

[68]  A. Ullrich,et al.  Increased expression of the putative growth factor receptor p185HER2 causes transformation and tumorigenesis of NIH 3T3 cells. , 1987, Proceedings of the National Academy of Sciences of the United States of America.

[69]  A. Lenferink,et al.  The oncogenic ErbB-2/ErbB-3 heterodimer is a surrogate receptor of the epidermal growth factor and betacellulin , 1998, Oncogene.

[70]  D. Engelman,et al.  A dimerization motif for transmembrane α–helices , 1994, Nature Structural Biology.

[71]  Yosef Yarden,et al.  Neuregulins and Their Receptors: A Versatile Signaling Module in Organogenesis and Oncogenesis , 1997, Neuron.

[72]  M. Sliwkowski,et al.  Binding specificities and affinities of egf domains for ErbB receptors , 1999, FEBS letters.

[73]  D Cowburn,et al.  Modular peptide recognition domains in eukaryotic signaling. , 1997, Annual review of biophysics and biomolecular structure.

[74]  Hyun-soo Cho,et al.  Structure of the Extracellular Region of HER3 Reveals an Interdomain Tether , 2002, Science.

[75]  T. Pawson.  Protein Modules and Signaling Networks , 2000 .

[76]  L. Cantley,et al.  Insect cell-expressed p180erbB3 possesses an impaired tyrosine kinase activity. , 1994, Proceedings of the National Academy of Sciences of the United States of America.

[77]  J. Brugge,et al.  Controlled Dimerization of ErbB Receptors Provides Evidence for Differential Signaling by Homo- and Heterodimers , 1999, Molecular and Cellular Biology.

[78]  S. Aaronson,et al.  Different structural alterations upregulate in vitro tyrosine kinase activity and transforming potency of the erbB-2 gene , 1988, Molecular and cellular biology.

[79]  Y. Yarden,et al.  ErbB‐2 is a common auxiliary subunit of NDF and EGF receptors: implications for breast cancer. , 1996, The EMBO journal.

[80]  A. Ullrich,et al.  Close similarity of epidermal growth factor receptor and v-erb-B oncogene protein sequences , 1984, Nature.

[81]  K. Foon,et al.  Human anti-murine immunoglobulin responses in patients receiving monoclonal antibody therapy. , 1985, Cancer research.

[82]  W. Carney,et al.  The extracellular domain of p185/neu is released from the surface of human breast carcinoma cells, SK-BR-3. , 1991, The Journal of biological chemistry.

[83]  Monilola A. Olayioye,et al.  The ErbB signaling network: receptor heterodimerization in development and cancer , 2000, The EMBO journal.

[84]  S. Ménard,et al.  The extracellular domain of the c-erbB-2 oncoprotein is released from tumor cells by proteolytic cleavage. , 1993, Oncogene.

[85]  A. Citri,et al.  The deaf and the dumb: the biology of ErbB-2 and ErbB-3. , 2003, Experimental cell research.

[86]  S. Rackovsky,et al.  Correlation of the structure of the transmembrane domain of the neu oncogene-encoded p185 protein with its function. , 1990, Proceedings of the National Academy of Sciences of the United States of America.

[87]  M. Kraus,et al.  Efficient coupling with phosphatidylinositol 3-kinase, but not phospholipase C gamma or GTPase-activating protein, distinguishes ErbB-3 signaling from that of other ErbB/EGFR family members , 1994, Molecular and cellular biology.

[88]  E. Peles,et al.  ErbB-3 and ErbB-4 function as the respective low and high affinity receptors of all Neu differentiation factor/heregulin isoforms. , 1994, The Journal of biological chemistry.

[89]  H. Wiley,et al.  ErbB-2 Amplification Inhibits Down-regulation and Induces Constitutive Activation of Both ErbB-2 and Epidermal Growth Factor Receptors* , 1999, The Journal of Biological Chemistry.

[90]  Y. Yarden,et al.  Neu Differentiation Factor/Neuregulin Isoforms Activate Distinct Receptor Combinations* , 1996, The Journal of Biological Chemistry.

[91]  R. Stein,et al.  Evolutionary Analysis of the ErbB Receptor and Ligand Families , 2000, Journal of Molecular Evolution.

[92]  M. Roussel,et al.  Glycogen synthase kinase-3beta regulates cyclin D1 proteolysis and subcellular localization. , 1998, Genes & development.

[93]  William F. DeGrado,et al.  Asparagine-mediated self-association of a model transmembrane helix , 2000, Nature Structural Biology.

[94]  Edouard C. Nice,et al.  Crystal Structure of a Truncated Epidermal Growth Factor Receptor Extracellular Domain Bound to Transforming Growth Factor α , 2002, Cell.

[95]  Jiri Bartek,et al.  Cyclin D1 protein expression and function in human breast cancer , 1994, International journal of cancer.

[96]  A. Deblasio,et al.  Prolonged induction of p21Cip1/WAF1/CDK2/PCNA complex by epidermal growth factor receptor activation mediates ligand-induced A431 cell growth inhibition , 1995, The Journal of cell biology.

[97]  J. Schlessinger.  SH2/SH3 signaling proteins. , 1994, Current opinion in genetics & development.

[98]  J. Baselga,et al.  Cleavage of the HER2 ectodomain is a pervanadate-activable process that is inhibited by the tissue inhibitor of metalloproteases-1 in breast cancer cells. , 1999, Cancer research.

[99]  N. Normanno,et al.  Epidermal growth factor-related peptides and their receptors in human malignancies. , 1995, Critical reviews in oncology/hematology.

[100]  P. Fedi,et al.  Epidermal growth factor and betacellulin mediate signal transduction through co‐expressed ErbB2 and ErbB3 receptors , 1997, The EMBO journal.

[101]  S. Ethier,et al.  Phosphatidylinositol 3-kinase recruitment by p185erbB-2 and erbB-3 is potently induced by neu differentiation factor/heregulin during mitogenesis and is constitutively elevated in growth factor-independent breast carcinoma cells with c-erbB-2 gene amplification. , 1996, Cell growth & differentiation : the molecular biology journal of the American Association for Cancer Research.

[102]  I. Lax,et al.  The docking protein Gab1 is the primary mediator of EGF-stimulated activation of the PI-3K/Akt cell survival pathway , 2004, BMC Biology.

[103]  Tony Pawson,et al.  Protein modules and signalling networks , 1995, Nature.

[104]  W. Gullick,et al.  Green fluorescent protein as a tool to study epidermal growth factor receptor function. , 2004, Cancer letters.

[105]  W. Gullick,et al.  The type 1 growth factor receptor family: new ligands and receptors and their role in breast cancer , 2004, Breast Cancer Research and Treatment.

[106]  M. Hung,et al.  HER-2/neu Blocks Tumor Necrosis Factor-induced Apoptosis via the Akt/NF-κB Pathway* , 2000, The Journal of Biological Chemistry.

[107]  A. Ullrich,et al.  Aggregation-induced activation of the epidermal growth factor receptor protein tyrosine kinase. , 1993, Biochemistry.

[108]  G. Carpenter,et al.  The carboxyl terminus of epidermal growth factor receptor/erbB-2 chimerae is internalization impaired. , 1993, Oncogene.

[109]  S. Aaronson,et al.  The normal erbB-2 product is an atypical receptor-like tyrosine kinase with constitutive activity in the absence of ligand. , 1990, The New biologist.