Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDR00928

Target Information
NameMitogen-activated protein kinase 10    
Type of targetResearch target    
SynonymsC-Jun N-terminal kinase 3    
JNK3    
MAP kinase p49 3F12    
Stress-activated protein kinase JNK3    
DiseaseIschemic stroke
[ICD9: 434.91   ICD10: I61-I63]
[1]
Neurological diseases[2]
BioChemical ClassTransferases transferring phosphorus-containing groups    
EC NumberEC 2.7.1.37
PathwayAdipocytokine signaling pathway
Colorectal cancer
Epithelial cell signaling in Helicobacter pylori
ErbB signaling pathway
Fc epsilon RI signaling pathway
Focal adhesion
GnRH signaling pathway
Insulin signaling pathway
MAPK signaling pathway
Pancreatic cancer
Pathways in cancer
Toll-like receptor signaling pathway
Type II diabetes mellitus
Wnt signaling pathway
UniProt IDP53779
PDB Structure1JNK; 1PMN; 1PMQ; 1PMU; 1PMV; 2B1P; 2EXC; 2O0U; 2O2U; 2OK1; 2P33; 2R9S; 2WAJ; 2ZDT; 2ZDU; 3CGF; 3CGO; 3DA6; 3FI2; 3FI3; 3FV8; 3G90; 3G9L; 3G9N; 3KVX; 3OXI; 3OY1; 3PTG; 3RTP; 3TTI; 3TTJ; 3V6R; 3V6S; 4H36; 4H39; 4H3B.    
FunctionResponds to activation by environmental stress and pro- inflammatory cytokines by phosphorylating a number of transcription factors, primarily components of ap-1 such as c-jun and atf2 and thus regulates ap-1 transcriptional activity.    
SequenceMSLHFLYYCSEPTLDVKIAFCQGFDKQVDVSYIAKHYNMSKSKVDNQFYSVEVGDSTFTV LKRYQNLKPIGSGAQGIVCAAYDAVLDRNVAIKKLSRPFQNQTHAKRAYRELVLMKCVNH KNIISLLNVFTPQKTLEEFQDVYLVMELMDANLCQVIQMELDHERMSYLLYQMLCGIKHL HSAGIIHRDLKPSNIVVKSDCTLKILDFGLARTAGTSFMMTPYVVTRYYRAPEVILGMGY KENVDIWSVGCIMGEMVRHKILFPGRDYIDQWNKVIEQLGTPCPEFMKKLQPTVRNYVEN RPKYAGLTFPKLFPDSLFPADSEHNKLKASQARDLLSKMLVIDPAKRISVDDALQHPYIN VWYDPAEVEAPPPQIYDKQLDEREHTIEEWKELIYKEVMNSEEKTKNGVVKGQPSPSGAA VNSSESLPPSSSVNDISSMSTDQTLASDTDSSLEASAGPLGCCR
Target ValidationClick to Find Target Validation Information.    
Inhibitor2,6-Dihydroanthra/1,9-Cd/Pyrazol-6-One[3]
9- (4-Hydroxyphenyl)-2,7-Phenanthroline[3]
AS-601245[4]
N- (4-amino-5-cyano-6-ethoxypyridin-2-yl)acetamide[5]
N- (4-amino-5-cyano-6-phenylpyridin-2-yl)acetamide[5]
NSC-656158[6]
Phenyl- (3-phenyl-1H-indazol-6-yl)-amine[7]
Phosphoaminophosphonic Acid-Adenylate Ester[8]
SB-203580[9]
SP-600125[4]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1A critical role of neural-specific JNK3 for ischemic apoptosis. Proc Natl Acad Sci U S A. 2003 Dec 9;100(25):15184-9. Epub 2003 Dec 1. To Reference
Ref 2The structure of JNK3 in complex with small molecule inhibitors: structural basis for potency and selectivity. Chem Biol. 2003 Aug;10(8):705-12. To Reference
Ref 3Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 4Proc Natl Acad Sci U S A. 2007 Dec 18;104(51):20523-8. Epub 2007 Dec 11.A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. To Reference
Ref 5J Med Chem. 2006 Jun 15;49(12):3563-80.Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity. To Reference
Ref 6J Med Chem. 2010 Feb 25;53(4):1616-26.Synthesis and preclinical evaluations of 2-(2-fluorophenyl)-6,7-methylenedioxyquinolin-4-one monosodium phosphate (CHM-1-P-Na) as a potent antitumor agent. To Reference
Ref 7Bioorg Med Chem Lett. 2005 Nov 15;15(22):5095-9.Design and synthesis of 6-anilinoindazoles as selective inhibitors of c-Jun N-terminal kinase-3. To Reference
Ref 8Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. To Reference
Ref 9J Med Chem. 2008 Jul 24;51(14):4122-49. Epub 2008 Jun 26.Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region. To Reference



 

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