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Description: Assay used purified human TGF R1 kinase domain produced in Sf9 insect cells. Description: Inhibition of a 6×-HIS tagged cytoplasmic kinase domain representing TGF R1 EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen ![\"Click](\"https://www.guidetopharmacology.org/GRAC/images/help_blue_small_transparent_bkground.png\")
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1 M and 10 M against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5 M 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 Clinically-Relevant Mutations and Pathophysiology Synonyms: Familial abdominal aortic aneurysm [Disease Ontology: DOID:0050306]Familial thoracic aortic aneurysm and aortic dissection [Orphanet: ORPHA91387] Synonyms: Multiple keratoacanthoma, Ferguson-Smith type [Orphanet: ORPHA65748] 1. Adams JL, Smothers J, Srinivasan R, Hoos A.(2015)Big opportunities for small molecules in immuno-oncology. 2. 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Engers DW, Frist AY, Lindsley CW, Hong CC, Hopkins CR.(2013)Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe. 7. 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. 8. Jin CH, Krishnaiah M, Sreenu D, Subrahmanyam VB, Rao KS, Lee HJ, Park SJ, Park HJ, Lee K, Sheen YY et al..(2014)Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/antifibrotic agent. 9. Jin CH, Sreenu D, Krishnaiah M, Subrahmanyam VB, Rao KS, Nagendra Mohan AV, Park CY, Son JY, Son DH, Park HJ et al..(2011)Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors. 10. Johnston CJC, Smyth DJ, Kodali RB, White MPJ, Harcus Y, Filbey KJ, Hewitson JP, Hinck CS, Ivens A, Kemter AM et al..(2017)A structurally distinct TGF-β mimic from an intestinal helminth parasite potently induces regulatory T cells. 11. Li HY, Wang Y, Heap CR, King CH, Mundla SR, Voss M, Clawson DK, Yan L, Campbell RM, Anderson BD et al..(2006)Dihydropyrrolopyrazole transforming growth factor-beta type I receptor kinase domain inhibitors: a novel benzimidazole series with selectivity versus transforming growth factor-beta type II receptor kinase and mixed lineage kinase-7. 12. Melisi D, Ishiyama S, Sclabas GM, Fleming JB, Xia Q, Tortora G, Abbruzzese JL, Chiao PJ.(2008)LY2109761, a novel transforming growth factor beta receptor type I and type II dual inhibitor, as a therapeutic approach to suppressing pancreatic cancer metastasis. 13. Mohedas AH, Wang Y, Sanvitale CE, Canning P, Choi S, Xing X, Bullock AN, Cuny GD, Yu PB.(2014)Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. 14. Ogunjimi AA, Zeqiraj E, Ceccarelli DF, Sicheri F, Wrana JL, David L.(2012)Structural basis for specificity of TGFβ family receptor small molecule inhibitors. 15. Raboisson P, Lenz O, Lin TI, Surleraux D, Chakravarty S, Scholliers A, Vermeiren K, Delouvroy F, Verbinnen T, Simmen K.(2007)Evaluation of the anti-hepatitis C virus effect of novel potent, selective, and orally bioavailable JNK and VEGFR kinase inhibitors. 16. Sawyer JS, Beight DW, Britt KS, Anderson BD, Campbell RM, Goodson T, Herron DK, Li HY, McMillen WT, Mort N et al..(2004)Synthesis and activity of new aryl- and heteroaryl-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain. 17. Tatake RJ, O\'Neill MM, Kennedy CA, Wayne AL, Jakes S, Wu D, Kugler Jr SZ, Kashem MA, Kaplita P, Snow RJ.(2008)Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. 18. Velaparthi U, Darne CP, Warrier J, Liu P, Rahaman H, Augustine-Rauch K, Parrish K, Yang Z, Swanson J, Brown J et al..(2020)Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGFβR1 Inhibitor as an Immuno-oncology Agent. 19. 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. 20. Yingling JM, McMillen WT, Yan L, Huang H, Sawyer JS, Graff J, Clawson DK, Britt KS, Anderson BD, Beight DW et al..(2018)Preclinical assessment of galunisertib (LY2157299 monohydrate), a first-in-class transforming growth factor-β receptor type I inhibitor. Type I receptor serine/threonine kinases: transforming growth factor beta receptor 1. Last modified on 11/02/2020. Accessed on 18/05/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1788.>>> 更多资讯详情请访问蚂蚁淘商城
