Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDC00102

Target Information
NameMitogen-activated protein kinase 8    
Type of targetClinical trial target    
SynonymsC-Jun N-terminal kinase 1    
JNK-46    
JNK1    
Stress-activated protein kinase JNK1    
DiseaseCancer, unspecific
[ICD9: 140-229   ICD10: C00-C96]
[1][2]
Crohn's disease, unspecified
[ICD9: 555   ICD10: K50]
[3]
Hearing Loss
[ICD9: 389   ICD10: H90-H91]
[4][5]
Inflammatory Disorders, Unspecified[1][2]
Insulin resistance[6]
Obesity
[ICD9: 278   ICD10: E66]
[6]
Drug(s)AM-111Phase I/II completedHearing Loss[4][5]
CC-401Discontinued in Phase IMyeloid Leukemia[1][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 IDP45983
PDB Structure1UKH; 1UKI; 2G01; 2GMX; 2H96; 2NO3; 2XRW; 2XS0; 3ELJ; 3O17; 3O2M; 3PZE; 3V3V; 3VUD; 3VUG; 3VUH; 3VUI; 3VUK; 3VUL; 3VUM; 4AWI; 4E73.    
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.    
SequenceMSRSKRDNNFYSVEIGDSTFTVLKRYQNLKPIGSGAQGIVCAAYDAILERNVAIKKLSRP FQNQTHAKRAYRELVLMKCVNHKNIIGLLNVFTPQKSLEEFQDVYIVMELMDANLCQVIQ MELDHERMSYLLYQMLCGIKHLHSAGIIHRDLKPSNIVVKSDCTLKILDFGLARTAGTSF MMTPYVVTRYYRAPEVILGMGYKENVDLWSVGCIMGEMVCHKILFPGRDYIDQWNKVIEQ LGTPCPEFMKKLQPTVRTYVENRPKYAGYSFEKLFPDVLFPADSEHNKLKASQARDLLSK MLVIDASKRISVDEALQHPYINVWYDPSEAEAPPPKIPDKQLDEREHTIEEWKELIYKEV MDLEERTKNGVIRGQPSPLGAAVINGSQHPSSSSSVNDVSSMSTDPTLASDTDSSLEAAA GPLGCCR
Target ValidationClick to Find Target Validation Information.    
Inhibitor2,6-Dihydroanthra/1,9-Cd/Pyrazol-6-One[7]
2- (2-[8]
2- (2-[8]
2- (2-[8]
2- (2-butoxypyrimidin-4-ylamino)benzoic acid[8]
2- (2-phenoxypyrimidin-4-ylamino)benzoic acid[8]
2- (2-propoxypyrimidin-4-ylamino)benzoic acid[8]
2- (2-sec-butoxypyrimidin-4-ylamino)benzoic acid[8]
4,5,6,7-tetrabromobenzotriazole[9]
AM-111[4][5]
AS-601245[10]
BISINDOLYLMALEIMIDE IX[11]
CC-401[1][2]
CEP-1347[12]
CI-1040,   PD-18435,   PD-184352[11]
GF-109203[11]
Go-6976[11]
KN-62[11]
KT-5720[11]
LY-294002[11]
N- (4-amino-5-cyano-6-ethoxypyridin-2-yl)acetamide[13]
N- (4-amino-5-cyano-6-phenylpyridin-2-yl)acetamide[14]
N- (4-amino-6-butoxy-5-cyanopyridin-2-yl)acetamide[14]
N- (6-ethoxypyridin-2-yl)acetamide[14]
NM-PP1[10]
PD-98059[11]
RO-316233[11]
SB-202190[11]
SB-203580[11]
SP-600125[15]
STAUROSPORINONE[11]
U-0126[11]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Blockade of the c-Jun amino terminal kinase prevents crescent formation and halts established anti-GBM glomerulonephritis in the rat. Lab Invest. 2009 Apr;89(4):470-84. Epub 2009 Feb 2. To Reference
Ref 2A pathogenic role for JNK signaling in experimental anti-GBM glomerulonephritis. Kidney Int. 2007 Sep;72(6):698-708. Epub 2007 Jun 27. To Reference
Ref 3From extracellular to intracellular targets, inhibiting MAP kinases in treatment of Crohn's disease. Ann N Y Acad Sci. 2002 Nov;973:349-58. To Reference
Ref 4AM-111 reduces hearing loss in a guinea pig model of acute labyrinthitis. Laryngoscope. 2007 Dec;117(12):2174-82. To Reference
Ref 5Intratympanic treatment of acute acoustic trauma with a cell-permeable JNK ligand: a prospective randomized phase I/II study. Acta Otolaryngol. 2007 Sep;127(9):938-42. To Reference
Ref 6A central role for JNK in obesity and insulin resistance. Nature. 2002 Nov 21;420(6913):333-6. To Reference
Ref 7Overington 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 8Bioorg Med Chem Lett. 2007 Feb 1;17(3):668-72. Epub 2006 Nov 2.Discovery of a new class of 4-anilinopyrimidines as potent c-Jun N-terminal kinase inhibitors: Synthesis and SAR studies. To Reference
Ref 9J Med Chem. 2004 Dec 2;47(25):6239-47.Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole. To Reference
Ref 10Biochem J. 2007 Dec 15;408(3):297-315.The selectivity of protein kinase inhibitors: a further update. To Reference
Ref 11Biochem J. 2000 Oct 1;351(Pt 1):95-105.Specificity and mechanism of action of some commonly used protein kinase inhibitors. To Reference
Ref 12Emerging drugs for Parkinson's disease. Expert Opin Emerg Drugs. 2006 Sep;11(3):403-17. To Reference
Ref 13J Med Chem. 2006 Jul 27;49(15):4455-8.Discovery of potent, highly selective, and orally bioavailable pyridine carboxamide c-Jun NH2-terminal kinase inhibitors. To Reference
Ref 14J 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 15Bioorg Med Chem. 2008 Apr 15;16(8):4715-32. Epub 2008 Feb 13.Discovery, synthesis and biological evaluation of isoquinolones as novel and highly selective JNK inhibitors (1). To Reference



 

Welcome to sign our Guestbook.

If you find any error in data or bug in web service, please kindly report it to Dr. Zhu.


Dr. Chen Yuzong
Deputy Director of Center for Computational Science and Engineering
Professor in Department of Pharmacy
National University of Singapore, Singapore


All rights reserved.

   
 
 
Computer-aided Drug Design
about BIDD |  databases |  software |  teaching |  research |  links

 

Department of Computational Science | National University of Singapore | Blk S17, 3 Science Drive 2, Singapore 117543