Proto-oncogene tyrosine-protein kinase receptor Ret
Also known as: CDHF12, CDHR16, PTC, RET
Function
Receptor tyrosine-protein kinase involved in numerous cellular mechanisms including cell proliferation, neuronal navigation, cell migration, and cell differentiation in response to glia cell line-derived growth family factors (GDNF, NRTN, ARTN, PSPN and GDF15). In contrast to most receptor tyrosine kinases, RET requires not only its cognate ligands but also coreceptors, for activation. GDNF ligands (GDNF, NRTN, ARTN, PSPN and GDF15) first bind their corresponding GDNFR coreceptors (GFRA1, GFRA2, GFRA3, GFRA4 and GFRAL, respectively), triggering RET autophosphorylation and activation, leading to activation of downstream signaling pathways, including the MAPK- and AKT-signaling pathways. Acts as a dependence receptor via the GDNF-GFRA1 signaling: in the presence of the ligand GDNF in somatotrophs within pituitary, promotes survival and down regulates growth hormone (GH) production, but triggers apoptosis in absence of GDNF. Required for the molecular mechanisms orchestration during intestine organogenesis via the ARTN-GFRA3 signaling: involved in the development of enteric nervous system and renal organogenesis during embryonic life, and promotes the formation of Peyer's patch-like structures, a major component of the gut-associated lymphoid tissue (By similarity). Mediates, through interaction with GDF15-receptor GFRAL, GDF15-induced cell-signaling in the brainstem which triggers an aversive response, characterized by nausea, vomiting, and/or loss of appetite in response to various stresses. Modulates cell adhesion via its cleavage by caspase in sympathetic neurons and mediates cell migration in an integrin (e.g. ITGB1 and ITGB3)-dependent manner. Also active in the absence of ligand, triggering apoptosis through a mechanism that requires receptor intracellular caspase cleavage. Triggers the differentiation of rapidly adapting (RA) mechanoreceptors. Involved in the development of the neural crest (By similarity). Regulates nociceptor survival and size (By similarity). Phosphorylates PTK2/FAK1.
Classification
- Family (Pfam)
- PF00028 Cadherin, PF07714 PK_Tyr_Ser-Thr, PF17756 RET_CLD1, PF17812 RET_CLD3, PF17813 RET_CLD4, PF22540 RET_CRD
- InterPro
- Cadherin-like_dom, Cadherin-like_sf, Kinase-like_dom_sf, Prot_kinase_dom, Protein_kinase_ATP_BS, Ret_CLD1, Ret_CLD3, RET_CLD4, RET_CRD, RTK, Ser-Thr/Tyr_kinase_cat_dom, Tyr_kinase_AS, Tyr_kinase_cat_dom, Tyr_kinase_Ret_rcpt
- Functional cluster
- Immunoglobulin-Domain Cell Adhesion Proteins
Experimental structures · PDB · 34
- 2IVS X-ray 2.00A
- 2IVT X-ray 2.60A
- 2IVU X-ray 2.50A
- 2IVV X-ray 2.25A
- 2X2K X-ray 2.60A
- 2X2L X-ray 2.00A
- 2X2M X-ray 2.50A
- 2X2U X-ray 2.00A
- 4CKI X-ray 2.12A
- 4CKJ X-ray 1.65A
- 4UX8 EM 24.00A
- 5AMN X-ray 2.57A
- … and 22 more
A predicted model is available from AlphaFold.
Gene Ontology · 32
- GO:0030424 axon
- GO:0010008 endosome membrane
- GO:0005886 plasma membrane
- GO:0098797 plasma membrane protein complex
- GO:0043235 receptor complex
- GO:0005524 ATP binding
- GO:0005509 calcium ion binding
- GO:0004713 protein tyrosine kinase activity
- GO:0038023 signaling receptor activity
- GO:0004714 transmembrane receptor protein tyrosine kinase activity
- GO:0007411 axon guidance
- GO:0007169 cell surface receptor protein tyrosine kinase signaling pathway
- GO:0071300 cellular response to retinoic acid
- GO:0160144 GDF15-GFRAL signaling pathway
- GO:0035860 glial cell-derived neurotrophic factor receptor signaling pathway
- GO:0007156 homophilic cell-cell adhesion
- GO:0097021 lymphocyte migration into lymphoid organs
- GO:0033619 membrane protein proteolysis
- GO:0007158 neuron cell-cell adhesion
- GO:0061146 Peyer's patch morphogenesis
- GO:0033630 positive regulation of cell adhesion mediated by integrin
- GO:0030335 positive regulation of cell migration
- GO:0045893 positive regulation of DNA-templated transcription
- GO:2001241 positive regulation of extrinsic apoptotic signaling pathway in absence of ligand
- GO:0043410 positive regulation of MAPK cascade
- GO:0072300 positive regulation of metanephric glomerulus development
- GO:0010976 positive regulation of neuron projection development
- GO:0051897 positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction
- GO:0007497 posterior midgut development
- GO:0030155 regulation of cell adhesion
- GO:0048265 response to pain
- GO:0007165 signal transduction
Disease associations
- colorectal cancer MONDO:0005575
- Hirschsprung disease, susceptibility to, 1 MONDO:0007723
- familial medullary thyroid carcinoma MONDO:0007958
- multiple endocrine neoplasia type 2B MONDO:0008082
- pheochromocytoma MONDO:0008233
- multiple endocrine neoplasia type 2A MONDO:0008234
Drugs targeting this protein · 14
- SORAFENIB TOSYLATE inhibitor
- SUNITINIB MALATE inhibitor
- REGORAFENIB inhibitor
- CEP-32496 inhibitor
- VANDETANIB inhibitor
- ALECTINIB HYDROCHLORIDE inhibitor
- SELPERCATINIB inhibitor
- PRALSETINIB inhibitor
- SUNITINIB inhibitor
- MOTESANIB inhibitor
- AST-487 inhibitor
- QUIZARTINIB inhibitor
- LESTAURTINIB inhibitor
- CEP-2563 DIHYDROCHLORIDE inhibitor
Neighborhood · nearest proteins
Related proteins · sequence + function similarity
- Proto-oncogene tyrosine-protein kinase receptor Ret 0.98
- Proto-oncogene tyrosine-protein kinase receptor Ret 0.97
- Ephrin type-B receptor 4 0.80
- Macrophage colony-stimulating factor 1 receptor 0.80
- Macrophage colony-stimulating factor 1 receptor 0.80
- Tyrosine-protein kinase transforming protein fms 0.80
- Ephrin type-B receptor 4 0.79
- Macrophage colony-stimulating factor 1 receptor 0.79
- Macrophage colony-stimulating factor 1 receptor 0.79
- Platelet-derived growth factor receptor beta 0.78
- Receptor-type tyrosine-protein kinase FLT3 0.78
- Platelet-derived growth factor receptor beta 0.78
Co-cited proteins · studied together in the literature
- Coiled-coil domain-containing protein 6 1 shared papers
- AH receptor-interacting protein 1 shared papers
- Golgin subfamily A member 5 1 shared papers
- Glial cell line-derived neurotrophic factor 6 shared papers
- Proto-oncogene tyrosine-protein kinase receptor Ret 5 shared papers
- Receptor-type tyrosine-protein phosphatase eta 2 shared papers
- Zinc finger protein RFP 2 shared papers
- Endothelin receptor type B 2 shared papers
- GDNF family receptor alpha-1 2 shared papers
- Paired mesoderm homeobox protein 2A 1 shared papers
- GDNF family receptor alpha-like 5 shared papers
- Proto-oncogene tyrosine-protein kinase receptor Ret 3 shared papers
Literature · 108 cited papers
- Cryo-EM analyses reveal the common mechanism and diversification in the activation of RET by different ligands. Elife · 2019
- Structural basis of resistance of mutant RET protein-tyrosine kinase to its inhibitors nintedanib and vandetanib. J. Biol. Chem. · 2019
- PMID 30552125 Cancer Res. · 2018
- Drug resistance profiles of mutations in the RET kinase domain. Br. J. Pharmacol. · 2018
- Non-homeostatic body weight regulation through a brainstem-restricted receptor for GDF15. Nature · 2017
- Non-homeostatic body weight regulation through a brainstem-restricted receptor for GDF15. Nature · 2017
- GFRAL is the receptor for GDF15 and is required for the anti-obesity effects of the ligand. Nat. Med. · 2017
- GFRAL is the receptor for GDF15 and the ligand promotes weight loss in mice and nonhuman primates. Nat. Med. · 2017
- The active site of O-GlcNAc transferase imposes constraints on substrate sequence. Nat. Struct. Mol. Biol. · 2015
- RET recognition of GDNF-GFRalpha1 ligand by a composite binding site promotes membrane-proximal self-association. Cell Rep. · 2014
- Oncogenic RET kinase domain mutations perturb the autophosphorylation trajectory by enhancing substrate presentation in trans. Mol. Cell · 2014
- SorLA controls neurotrophic activity by sorting of GDNF and its receptors GFRalpha1 and RET. Cell Rep. · 2013
- … and 96 more in the literature graph