TGF-beta receptor type-1
Also known as: ALK5, SKR4, TGFBR1
Function
Transmembrane serine/threonine kinase forming with the TGF-beta type II serine/threonine kinase receptor, TGFBR2, the non-promiscuous receptor for the TGF-beta cytokines TGFB1, TGFB2 and TGFB3. Transduces the TGFB1, TGFB2 and TGFB3 signal from the cell surface to the cytoplasm and is thus regulating a plethora of physiological and pathological processes including cell cycle arrest in epithelial and hematopoietic cells, control of mesenchymal cell proliferation and differentiation, wound healing, extracellular matrix production, immunosuppression and carcinogenesis. The formation of the receptor complex composed of 2 TGFBR1 and 2 TGFBR2 molecules symmetrically bound to the cytokine dimer results in the phosphorylation and the activation of TGFBR1 by the constitutively active TGFBR2. Activated TGFBR1 phosphorylates SMAD2 which dissociates from the receptor and interacts with SMAD4. The SMAD2-SMAD4 complex is subsequently translocated to the nucleus where it modulates the transcription of the TGF-beta-regulated genes. This constitutes the canonical SMAD-dependent TGF-beta signaling cascade. Also involved in non-canonical, SMAD-independent TGF-beta signaling pathways. For instance, TGFBR1 induces TRAF6 autoubiquitination which in turn results in MAP3K7 ubiquitination and activation to trigger apoptosis. Also regulates epithelial to mesenchymal transition through a SMAD-independent signaling pathway through PARD6A phosphorylation and activation.
Classification
- Family (Pfam)
- PF01064 Activin_recp, PF00069 Pkinase, PF08515 TGF_beta_GS
- InterPro
- Activin_recp, GS_dom, Kinase-like_dom_sf, Prot_kinase_dom, Protein_kinase_ATP_BS, Ser/Thr_kinase_AS, Snake_toxin-like_sf, TGFB_receptor
- Functional cluster
- Immunoglobulin-Domain Cell Adhesion Proteins
Experimental structures · PDB · 44
- 1B6C X-ray 2.60A
- 1IAS X-ray 2.90A
- 1PY5 X-ray 2.30A
- 1RW8 X-ray 2.40A
- 1VJY X-ray 2.00A
- 2L5S NMR
- 2PJY X-ray 3.00A
- 2WOT X-ray 1.85A
- 2WOU X-ray 2.30A
- 2X7O X-ray 3.70A
- 3FAA X-ray 3.35A
- 3GXL X-ray 1.80A
- … and 32 more
A predicted model is available from AlphaFold.
Gene Ontology · 89
- GO:0048179 activin receptor complex
- GO:0005923 bicellular tight junction
- GO:0009986 cell surface
- GO:0005768 endosome
- GO:0016020 membrane
- GO:0045121 membrane raft
- GO:0005634 nucleus
- GO:0005886 plasma membrane
- GO:0043235 receptor complex
- GO:0048185 activin binding
- GO:0016361 activin receptor activity, type I
- GO:0005524 ATP binding
- GO:0070411 I-SMAD binding
- GO:0046872 metal ion binding
- GO:0004672 protein kinase activity
- GO:0004674 protein serine/threonine kinase activity
- GO:0046332 SMAD binding
- GO:0050431 transforming growth factor beta binding
- GO:0005024 transforming growth factor beta receptor activity
- GO:0005025 transforming growth factor beta receptor activity, type I
- GO:0004675 transmembrane receptor protein serine/threonine kinase activity
- GO:0005114 type II transforming growth factor beta receptor binding
- GO:0031625 ubiquitin protein ligase binding
- GO:0032924 activin receptor signaling pathway
- GO:0060978 angiogenesis involved in coronary vascular morphogenesis
- GO:0009952 anterior/posterior pattern specification
- GO:0006915 apoptotic process
- GO:0048844 artery morphogenesis
- GO:0060317 cardiac epithelial to mesenchymal transition
- GO:0048870 cell motility
- GO:0071363 cellular response to growth factor stimulus
- GO:0071560 cellular response to transforming growth factor beta stimulus
- GO:0030199 collagen fibril organization
- GO:0060982 coronary artery morphogenesis
- GO:0048701 embryonic cranial skeleton morphogenesis
- GO:0042118 endothelial cell activation
- GO:1905223 epicardium morphogenesis
- GO:0001837 epithelial to mesenchymal transition
- GO:0043062 extracellular structure organization
- GO:0008354 germ cell migration
- GO:0007507 heart development
- GO:0001701 in utero embryonic development
- GO:0035556 intracellular signal transduction
- GO:0001822 kidney development
- GO:0048762 mesenchymal cell differentiation
- GO:0036446 myofibroblast differentiation
- GO:0030336 negative regulation of cell migration
- GO:0032331 negative regulation of chondrocyte differentiation
- GO:2001237 negative regulation of extrinsic apoptotic signaling pathway
- GO:0007399 nervous system development
- GO:0048663 neuron fate commitment
- GO:0060017 parathyroid gland development
- GO:0018105 peptidyl-serine phosphorylation
- GO:0060037 pharyngeal system development
- GO:2001235 positive regulation of apoptotic signaling pathway
- GO:0030307 positive regulation of cell growth
- GO:0030335 positive regulation of cell migration
- GO:0008284 positive regulation of cell population proliferation
- GO:0045893 positive regulation of DNA-templated transcription
- GO:0001938 positive regulation of endothelial cell proliferation
- GO:0010718 positive regulation of epithelial to mesenchymal transition
- GO:1905007 positive regulation of epithelial to mesenchymal transition involved in endocardial cushion formation
- GO:1901203 positive regulation of extracellular matrix assembly
- GO:0010628 positive regulation of gene expression
- GO:1902462 positive regulation of mesenchymal stem cell proliferation
- GO:0051897 positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction
- GO:0060391 positive regulation of SMAD protein signal transduction
- GO:0051496 positive regulation of stress fiber assembly
- GO:1905075 positive regulation of tight junction disassembly
- GO:1904018 positive regulation of vasculature development
- GO:0060043 regulation of cardiac muscle cell proliferation
- GO:0051726 regulation of cell cycle
- GO:0006355 regulation of DNA-templated transcription
- GO:0010717 regulation of epithelial to mesenchymal transition
- GO:0010468 regulation of gene expression
- GO:0031396 regulation of protein ubiquitination
- GO:0070723 response to cholesterol
- GO:0060021 roof of mouth development
- GO:0007165 signal transduction
- GO:0001501 skeletal system development
- GO:0048705 skeletal system morphogenesis
- GO:0048538 thymus development
- GO:0007179 transforming growth factor beta receptor signaling pathway
- GO:0061450 trophoblast cell migration
- GO:0101023 vascular endothelial cell proliferation
- GO:0003223 ventricular compact myocardium morphogenesis
- GO:0060412 ventricular septum morphogenesis
- GO:0003222 ventricular trabecula myocardium morphogenesis
- GO:0042060 wound healing
Disease associations
- multiple self-healing squamous epithelioma MONDO:0007566
- Loeys-Dietz syndrome 1 MONDO:0012212
Drugs targeting this protein · 2
- GALUNISERTIB inhibitor
- VACTOSERTIB inhibitor
Related proteins · sequence + function similarity
- TGF-beta receptor type-1 0.99
- TGF-beta receptor type-1 0.99
- TGF-beta receptor type-1 0.98
- TGF-beta receptor type-1 0.98
- Activin receptor type-1B 0.96
- Activin receptor type-1B 0.96
- Activin receptor type-1B 0.96
- Activin receptor type-1C 0.96
- Activin receptor type-1C 0.96
- Activin receptor type-1C 0.95
- Activin receptor type-1 0.93
- Activin receptor type-1 0.92
Co-cited proteins · studied together in the literature
- TGF-beta receptor type-2 11 shared papers
- Peptidyl-prolyl cis-trans isomerase FKBP1A 2 shared papers
- SMAD family member 2 6 shared papers
- Bifunctional apoptosis regulator 1 shared papers
- SMAD family member 7 4 shared papers
- Ubiquitin carboxyl-terminal hydrolase 15 1 shared papers
- Melatonin-related receptor 1 shared papers
- CD109 antigen 1 shared papers
- Transforming growth factor beta-1 proprotein 3 shared papers
- Partitioning defective 6 homolog alpha 1 shared papers
- Melatonin-related receptor 1 shared papers
- SMAD family member 3 3 shared papers
Literature · 49 cited papers
- BFAR coordinates TGFbeta signaling to modulate Th9-mediated cancer immunotherapy. J. Exp. Med. · 2021
- The orphan GPR50 receptor promotes constitutive TGFbeta receptor signaling and protects against cancer development. Nat. Commun. · 2018
- APPL proteins promote TGFbeta-induced nuclear transport of the TGFbeta type I receptor intracellular domain. Oncotarget · 2016
- Syntenin regulates TGF-beta1-induced Smad activation and the epithelial-to-mesenchymal transition by inhibiting caveolin-mediated TGF-beta type I receptor internalization. Oncogene · 2016
- USP15 stabilizes TGF-beta receptor I and promotes oncogenesis through the activation of TGF-beta signaling in glioblastoma. Nat. Med. · 2012
- Clinical features and genetic analysis of Korean patients with Loeys-Dietz syndrome. J. Hum. Genet. · 2012
- TSC-22 promotes transforming growth factor beta-mediated cardiac myofibroblast differentiation by antagonizing Smad7 activity. Mol. Cell. Biol. · 2011
- Multiple self-healing squamous epithelioma is caused by a disease-specific spectrum of mutations in TGFBR1. Nat. Genet. · 2011
- Ternary complex of transforming growth factor-beta1 reveals isoform-specific ligand recognition and receptor recruitment in the superfamily. J. Biol. Chem. · 2010
- Loeys-Dietz syndrome type I and type II: clinical findings and novel mutations in two Italian patients. Orphanet J. Rare Dis. · 2009
- Large-scale proteomics analysis of the human kinome. Mol. Cell. Proteomics · 2009
- DNA sequencing of a cytogenetically normal acute myeloid leukaemia genome. Nature · 2008
- … and 37 more in the literature graph