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Target has curated data in GtoImmuPdb
Target id: 1836
Nomenclature: TYRO3 protein tyrosine kinase
Abbreviated Name: Tyro3
Family: Type XI RTKs: TAM (TYRO3-, AXL- and MER-TK) receptor family
Gene and Protein Information | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | 1 | 890 | 15q15.1 | TYRO3 | TYRO3 protein tyrosine kinase | |
Mouse | 1 | 880 | 2 59.97 cM | Tyro3 | TYRO3 protein tyrosine kinase 3 | |
Rat | 1 | 880 | 3q35 | Tyro3 | TYRO3 protein tyrosine kinase |
Previous and Unofficial Names |
Brt | Dtk | RSE | Tif | Bruton agammaglobulinemia tyrosine kinase | tyrosine-protein kinase SKY | Etk-2 |
Database Links | |
Alphafold | Q06418 (Hs), P55144 (Mm), P55146 (Rn) |
BRENDA | 2.7.10.1 |
CATH/Gene3D | 2.60.40.10 |
ChEMBL Target | CHEMBL5314 (Hs) |
Ensembl Gene | ENSG00000092445 (Hs), ENSMUSG00000027298 (Mm), ENSRNOG00000058586 (Rn) |
Entrez Gene | 7301 (Hs), 22174 (Mm), 25232 (Rn) |
Human Protein Atlas | ENSG00000092445 (Hs) |
KEGG Enzyme | 2.7.10.1 |
KEGG Gene | hsa:7301 (Hs), mmu:22174 (Mm), rno:25232 (Rn) |
OMIM | 600341 (Hs) |
Pharos | Q06418 (Hs) |
RefSeq Nucleotide | NM_006293 (Hs), NM_019392 (Mm), NM_017092 (Rn) |
RefSeq Protein | NP_006284 (Hs), NP_062265 (Mm), NP_058788 (Rn) |
UniProtKB | Q06418 (Hs), P55144 (Mm), P55146 (Rn) |
Wikipedia | TYRO3 (Hs) |
Selected 3D Structures | |||||||||||
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Enzyme Reaction | ||||
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Natural/Endogenous Ligands |
growth arrest specific protein 6 {Sp: Human} |
protein S {Sp: Human} |
Download all structure-activity data for this target as a CSV file
Inhibitors | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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DiscoveRx KINOMEscan® screen | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform. http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan Reference: 3,10 |
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Key to terms and symbols | Click column headers to sort | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Target used in screen: TYRO3 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service. A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform. http://www.millipore.com/techpublications/tech1/pf3036 http://www.reactionbiology.com/webapps/main/pages/kinase.aspx Reference: 1,4 |
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Target used in screen: Rse/TYRO3(SKY) | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
Immunopharmacology Comments |
TYRO3 is a negative regulator of type 2 immunity [2]. |
Immuno Process Associations | ||
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1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1039-45. [PMID:22037377]
2. Chan PY, Carrera Silva EA, De Kouchkovsky D, Joannas LD, Hao L, Hu D, Huntsman S, Eng C, Licona-Limón P, Weinstein JS et al.. (2016) The TAM family receptor tyrosine kinase TYRO3 is a negative regulator of type 2 immunity. Science, 352 (6281): 99-103. [PMID:27034374]
3. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1046-51. [PMID:22037378]
4. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem J, 451 (2): 313-28. [PMID:23398362]
5. Heiring C, Dahlbäck B, Muller YA. (2004) Ligand recognition and homophilic interactions in Tyro3: structural insights into the Axl/Tyro3 receptor tyrosine kinase family. J Biol Chem, 279 (8): 6952-8. [PMID:14623883]
6. Kong D, Tian Q, Chen Z, Zheng H, Stashko MA, Yan D, Earp HS, Frye SV, DeRyckere D, Kireev D et al.. (2024) Discovery of Novel Macrocyclic MERTK/AXL Dual Inhibitors. J Med Chem, 67 (7): 5866-5882. [PMID:38556760]
7. Paolino M, Choidas A, Wallner S, Pranjic B, Uribesalgo I, Loeser S, Jamieson AM, Langdon WY, Ikeda F, Fededa JP et al.. (2014) The E3 ligase Cbl-b and TAM receptors regulate cancer metastasis via natural killer cells. Nature, 507 (7493): 508-12. [PMID:24553136]
8. Powell NA, Hoffman JK, Ciske FL, Kohrt JT, Baxi SM, Peng YW, Zhong M, Catana C, Ohren J, Perrin LA et al.. (2013) Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase. Bioorg Med Chem Lett, 23 (4): 1051-5. [PMID:23312943]
9. Schroeder GM, An Y, Cai ZW, Chen XT, Clark C, Cornelius LA, Dai J, Gullo-Brown J, Gupta A, Henley B et al.. (2009) Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the Met kinase superfamily. J Med Chem, 52 (5): 1251-4. [PMID:19260711]
10. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem Biol, 17 (11): 1241-9. [PMID:21095574]
11. Zhang Z. (2015) Aminopyridine derivatives as tam family kinase inhibitors. Patent number: WO2015081257A2. Assignee: Signalchem Lifesciences Corporation. Priority date: 26/11/2014. Publication date: 04/06/2015.
12. Zhao J, Zhang D, Zhang W, Stashko MA, DeRyckere D, Vasileiadi E, Parker RE, Hunter D, Liu Q, Zhang Y et al.. (2018) Highly Selective MERTK Inhibitors Achieved by a Single Methyl Group. J Med Chem, 61 (22): 10242-10254. [PMID:30347155]
Type XI RTKs: TAM (TYRO3-, AXL- and MER-TK) receptor family: TYRO3 protein tyrosine kinase. Last modified on 02/04/2024. Accessed on 02/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1836.