Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T89323
|
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| Former ID |
TTDR00340
|
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| Target Name |
Mitogen-activated protein kinase kinase kinase 10
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| Gene Name |
MAP3K10
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| Synonyms |
Mixed lineage kinase 2; Protein kinase MST; MAP3K10
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| Target Type |
Research
|
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| Function |
Activates the JUN N-terminal pathway.
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| BioChemical Class |
Kinase
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| Target Validation |
T89323
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| UniProt ID | |||||
| EC Number |
EC 2.7.11.25
|
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| Sequence |
MEEEEGAVAKEWGTTPAGPVWTAVFDYEAAGDEELTLRRGDRVQVLSQDCAVSGDEGWWT
GQLPSGRVGVFPSNYVAPGAPAAPAGLQLPQEIPFHELQLEEIIGVGGFGKVYRALWRGE EVAVKAARLDPEKDPAVTAEQVCQEARLFGALQHPNIIALRGACLNPPHLCLVMEYARGG ALSRVLAGRRVPPHVLVNWAVQVARGMNYLHNDAPVPIIHRDLKSINILILEAIENHNLA DTVLKITDFGLAREWHKTTKMSAAGTYAWMAPEVIRLSLFSKSSDVWSFGVLLWELLTGE VPYREIDALAVAYGVAMNKLTLPIPSTCPEPFARLLEECWDPDPHGRPDFGSILKRLEVI EQSALFQMPLESFHSLQEDWKLEIQHMFDDLRTKEKELRSREEELLRAAQEQRFQEEQLR RREQELAEREMDIVERELHLLMCQLSQEKPRVRKRKGNFKRSRLLKLREGGSHISLPSGF EHKITVQASPTLDKRKGSDGASPPASPSIIPRLRAIRLTPVDCGGSSSGSSSGGSGTWSR GGPPKKEELVGGKKKGRTWGPSSTLQKERVGGEERLKGLGEGSKQWSSSAPNLGKSPKHT PIAPGFASLNEMEEFAEAEDGGSSVPPSPYSTPSYLSVPLPAEPSPGARAPWEPTPSAPP ARWGHGARRRCDLALLGCATLLGAVGLGADVAEARAADGEEQRRWLDGLFFPRAGRFPRG LSPPARPHGRREDVGPGLGLAPSATLVSLSSVSDCNSTRSLLRSDSDEAAPAAPSPPPSP PAPTPTPSPSTNPLVDLELESFKKDPRQSLTPTHVTAACAVSRGHRRTPSDGALGQRGPP EPAGHGPGPRDLLDFPRLPDPQALFPARRRPPEFPGRPTTLTFAPRPRPAASRPRLDPWK LVSFGRTLTISPPSRPDTPESPGPPSVQPTLLDMDMEGQNQDSTVPLCGAHGSH |
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| Inhibitor | CEP-1374 | Drug Info | [1] | ||
| CEP-5104 | Drug Info | [2] | |||
| CEP-6331 | Drug Info | [2] | |||
| CEP1348 | Drug Info | [3] | |||
| URMC-099 | Drug Info | [4] | |||
| Pathways | |||||
| PANTHER Pathway | Huntington disease | ||||
| p38 MAPK pathway | |||||
| Pathway Interaction Database | p38 MAPK signaling pathway | ||||
| WikiPathways | Insulin Signaling | ||||
| References | |||||
| REF 1 | Cep-1347 (KT7515), a semisynthetic inhibitor of the mixed lineage kinase family. J Biol Chem. 2001 Jul 6;276(27):25302-8. Epub 2001 Apr 26. | ||||
| REF 2 | J Med Chem. 2008 Sep 25;51(18):5680-9. Epub 2008 Aug 21.Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models. | ||||
| REF 3 | Pharmacological inhibitors of MAPK pathways. Trends Pharmacol Sci. 2002 Jan;23(1):40-5. | ||||
| REF 4 | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. J Med Chem. 2013 Oct 24;56(20):8032-48. | ||||
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