Receptor tyrosine-protein kinase erbB-4
Also known as: ERBB4, HER4
Function
Tyrosine-protein kinase that plays an essential role as cell surface receptor for neuregulins and EGF family members and regulates development of the heart, the central nervous system and the mammary gland, gene transcription, cell proliferation, differentiation, migration and apoptosis. Required for normal cardiac muscle differentiation during embryonic development, and for postnatal cardiomyocyte proliferation. Required for normal development of the embryonic central nervous system, especially for normal neural crest cell migration and normal axon guidance. Required for mammary gland differentiation, induction of milk proteins and lactation. Acts as cell-surface receptor for the neuregulins NRG1, NRG2, NRG3 and NRG4 and the EGF family members BTC, EREG and HBEGF. Ligand binding triggers receptor dimerization and autophosphorylation at specific tyrosine residues that then serve as binding sites for scaffold proteins and effectors. Ligand specificity and signaling is modulated by alternative splicing, proteolytic processing, and by the formation of heterodimers with other ERBB family members, thereby creating multiple combinations of intracellular phosphotyrosines that trigger ligand- and context-specific cellular responses. Mediates phosphorylation of SHC1 and activation of the MAP kinases MAPK1/ERK2 and MAPK3/ERK1. Isoform JM-A CYT-1 and isoform JM-B CYT-1 phosphorylate PIK3R1, leading to the activation of phosphatidylinositol 3-kinase and AKT1 and protect cells against apoptosis. Isoform JM-A CYT-1 and isoform JM-B CYT-1 mediate reorganization of the actin cytoskeleton and promote cell migration in response to NRG1. Isoform JM-A CYT-2 and isoform JM-B CYT-2 lack the phosphotyrosine that mediates interaction with PIK3R1, and hence do not phosphorylate PIK3R1, do not protect cells against apoptosis, and do not promote reorganization of the actin cytoskeleton and cell migration. Proteolytic processing of isoform JM-A CYT-1 and isoform JM-A CYT-2 gives rise to the corresponding soluble intracellular domains (4ICD) that translocate to the nucleus, promote nuclear import of STAT5A, activation of STAT5A, mammary epithelium differentiation, cell proliferation and activation of gene expression. The ERBB4 soluble intracellular domains (4ICD) colocalize with STAT5A at the CSN2 promoter to regulate transcription of milk proteins during lactation. The ERBB4 soluble intracellular domains can also translocate to mitochondria and promote apoptosis.
Classification
- Family (Pfam)
- PF00757 Furin-like, PF14843 GF_recep_IV, PF07714 PK_Tyr_Ser-Thr, PF01030 Recep_L_domain, PF21314 TM_ErbB1
- InterPro
- Furin-like_Cys-rich_dom, Furin_repeat, GF_recep_IV, Growth_fac_rcpt_cys_sf, Kinase-like_dom_sf, Prot_kinase_dom, Protein_kinase_ATP_BS, Rcpt_L-dom, Rcpt_L-dom_sf, RTK, Ser-Thr/Tyr_kinase_cat_dom, TM_ErbB1, Tyr_kinase_AS, Tyr_kinase_cat_dom, Tyr_kinase_EGF/ERB/XmrK_rcpt
- Functional cluster
- Mixed Regulatory & Membrane Proteins
Experimental structures · PDB · 14
- 2AHX X-ray 2.40A
- 2L2T NMR
- 2LCX NMR
- 2R4B X-ray 2.40A
- 3BBT X-ray 2.80A
- 3BBW X-ray 4.00A
- 3BCE X-ray 2.50A
- 3U2P X-ray 2.57A
- 3U7U X-ray 3.03A
- 3U9U X-ray 3.42A
- 8U4I EM 3.38A
- 8U4J EM 3.70A
- … and 2 more
A predicted model is available from AlphaFold.
Gene Ontology · 62
- GO:0009925 basal plasma membrane
- GO:0016323 basolateral plasma membrane
- GO:0005829 cytosol
- GO:0005576 extracellular region
- GO:0098982 GABA-ergic synapse
- GO:0098978 glutamatergic synapse
- GO:0005759 mitochondrial matrix
- GO:0005739 mitochondrion
- GO:0031594 neuromuscular junction
- GO:0005654 nucleoplasm
- GO:0005634 nucleus
- GO:0005886 plasma membrane
- GO:0098839 postsynaptic density membrane
- GO:0045211 postsynaptic membrane
- GO:0042734 presynaptic membrane
- GO:0043235 receptor complex
- GO:0005524 ATP binding
- GO:0005006 epidermal growth factor receptor activity
- GO:0005154 epidermal growth factor receptor binding
- GO:0050811 GABA receptor binding
- GO:0038131 neuregulin receptor activity
- GO:0042803 protein homodimerization activity
- GO:0004713 protein tyrosine kinase activity
- GO:0000976 transcription cis-regulatory region binding
- GO:0004714 transmembrane receptor protein tyrosine kinase activity
- GO:0061026 cardiac muscle tissue regeneration
- GO:0016477 cell migration
- GO:0007169 cell surface receptor protein tyrosine kinase signaling pathway
- GO:0007259 cell surface receptor signaling pathway via JAK-STAT
- GO:0021551 central nervous system morphogenesis
- GO:0006351 DNA-templated transcription
- GO:0009880 embryonic pattern specification
- GO:0007173 epidermal growth factor receptor signaling pathway
- GO:0038135 ERBB2-ERBB4 signaling pathway
- GO:0038130 ERBB4 signaling pathway
- GO:0038138 ERBB4-ERBB4 signaling pathway
- GO:0007507 heart development
- GO:0007595 lactation
- GO:0060749 mammary gland alveolus development
- GO:0060644 mammary gland epithelial cell differentiation
- GO:0043653 mitochondrial fragmentation involved in apoptotic process
- GO:0043066 negative regulation of apoptotic process
- GO:0008285 negative regulation of cell population proliferation
- GO:0007399 nervous system development
- GO:0001755 neural crest cell migration
- GO:0030182 neuron differentiation
- GO:0099645 neurotransmitter receptor localization to postsynaptic specialization membrane
- GO:0021889 olfactory bulb interneuron differentiation
- GO:0018108 peptidyl-tyrosine phosphorylation
- GO:0060045 positive regulation of cardiac muscle cell proliferation
- GO:0008284 positive regulation of cell population proliferation
- GO:0045893 positive regulation of DNA-templated transcription
- GO:0050679 positive regulation of epithelial cell proliferation
- GO:0070374 positive regulation of ERK1 and ERK2 cascade
- GO:0043410 positive regulation of MAPK cascade
- GO:0001934 positive regulation of protein phosphorylation
- GO:0046427 positive regulation of receptor signaling pathway via JAK-STAT
- GO:0042531 positive regulation of tyrosine phosphorylation of STAT protein
- GO:0046777 protein autophosphorylation
- GO:0030334 regulation of cell migration
- GO:0007165 signal transduction
- GO:0007416 synapse assembly
Disease associations
- amyotrophic lateral sclerosis type 19 MONDO:0014223
Drugs targeting this protein · 12
- AC-480 inhibitor
- NERATINIB inhibitor
- AFATINIB DIMALEATE inhibitor
- DACOMITINIB inhibitor
- DACOMITINIB ANHYDROUS inhibitor
- VANDETANIB inhibitor
- JNJ-26483327 inhibitor
- POZIOTINIB inhibitor
- BMS-690514 inhibitor
- NERATINIB MALEATE inhibitor
- TARLOXOTINIB inhibitor
- CANERTINIB DIHYDROCHLORIDE inhibitor
Related proteins · sequence + function similarity
- Receptor tyrosine-protein kinase erbB-4 1.00
- Receptor tyrosine-protein kinase erbB-4 1.00
- Epidermal growth factor receptor 0.79
- Epidermal growth factor receptor 0.78
- Epidermal growth factor receptor 0.78
- Gamma-aminobutyric acid type B receptor subunit 1 0.66
- Endosome/lysosome-associated apoptosis and autophagy regulator 1 0.66
- Gamma-aminobutyric acid type B receptor subunit 1 0.66
- Gamma-aminobutyric acid type B receptor subunit 1 0.66
- Receptor tyrosine-protein kinase erbB-2 0.64
- Receptor tyrosine-protein kinase erbB-2 0.64
- Follistatin-related protein 1 0.63
Co-cited proteins · studied together in the literature
- Receptor tyrosine-protein kinase erbB-4 5 shared papers
- Pro-neuregulin-4, membrane-bound isoform 1 shared papers
- Pro-neuregulin-1, membrane-bound isoform 3 shared papers
- Pro-neuregulin-2, membrane-bound isoform 1 shared papers
- Probetacellulin 2 shared papers
- Proheparin-binding EGF-like growth factor 1 shared papers
- Pro-neuregulin-3, membrane-bound isoform 1 shared papers
- Receptor tyrosine-protein kinase erbB-2 3 shared papers
- Pro-neuregulin-3, membrane-bound isoform 2 shared papers
- Proepiregulin 1 shared papers
- Signal transducer and activator of transcription 5A 1 shared papers
- WW domain-containing oxidoreductase 1 shared papers
Literature · 52 cited papers
- ERBB4 mutations that disrupt the neuregulin-ErbB4 pathway cause amyotrophic lateral sclerosis type 19. Am. J. Hum. Genet. · 2013
- Function of ERBB4 is determined by alternative splicing. Cell Cycle · 2011
- Small tyrosine kinase inhibitors interrupt EGFR signaling by interacting with erbB3 and erbB4 in glioblastoma cell lines. Exp. Cell Res. · 2011
- Neuregulin-1/ErbB signaling and chronic heart failure. Adv. Pharmacol. · 2010
- Interactions of ErbB4 and Kap1 connect the growth factor and DNA damage response pathways. Mol. Cancer Res. · 2010
- WW domain containing E3 ubiquitin protein ligase 1 targets the full-length ErbB4 for ubiquitin-mediated degradation in breast cancer. Oncogene · 2009
- Nedd4 mediates ErbB4 JM-a/CYT-1 ICD ubiquitination and degradation in MDCK II cells. FASEB J. · 2009
- Somatic mutations of ErbB4: selective loss-of-function phenotype affecting signal transduction pathways in cancer. J. Biol. Chem. · 2009
- System-wide investigation of ErbB4 reveals 19 sites of Tyr phosphorylation that are unusually selective in their recruitment properties. Chem. Biol. · 2008
- HER4 intracellular domain (4ICD) activity in the developing mammary gland and breast cancer. J. Mammary Gland Biol. Neoplasia · 2008
- Role of ErbB4 in breast cancer. J. Mammary Gland Biol. Neoplasia · 2008
- ErbB4/HER4: role in mammary gland development, differentiation and growth inhibition. J. Mammary Gland Biol. Neoplasia · 2008
- … and 40 more in the literature graph