Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDC00222

Target Information
NameInhibitor of nuclear factor kappa-B kinase    
Type of targetDiscontinued target    
SynonymsI kappa B kinase    
IKK    
IkBK    
DiseaseAnalgesics
[ICD9: 338   ICD10: R52]
[1]
Herpes virus infection
[ICD9: 001-139, 042-075   ICD10: A00-B99, A80-A99, B00-B34]
[2]
Inflammation[1]
Inflammatory diseases[3]
Pain, unspecified
[ICD9: 338,780   ICD10: R52, G89]
[1]
Rheumatoid arthritis, unspecified
[ICD9: 710-719, 714   ICD10: M00-M25, M05-M06]
[4]
Drug(s)SAR113945Phase IIOsteoarthritis
SAR113945Phase IOsteoarthritis
MLN0415Discontined in Phase IInflammatory diseases[5]
BioChemical ClassTransferases transferring phosphorus-containing groups    
EC NumberEC 2.7.1.-
PathwayAcute myeloid leukemia
Adipocytokine signaling pathway
Apoptosis
B cell receptor signaling pathway
Chemokine signaling pathway
Chronic myeloid leukemia
Epithelial cell signaling in Helicobacter pylori
Insulin signaling pathway
MAPK signaling pathway
Pancreatic cancer
Pathways in cancer
Prostate cancer
Small cell lung cancer
T cell receptor signaling pathway
Toll-like receptor signaling pathway
Type II diabetes mellitus
UniProt IDO14920
O15111
Q14164
PDB Structure3BRT; 3BRV.    
SequenceMSWSPSLTTQTCGAWEMKERLGTGGFGNVIRWHNQETGEQIAIKQCRQELSPRNRERWCL EIQIMRRLTHPNVVAARDVPEGMQNLAPNDLPLLAMEYCQGGDLRKYLNQFENCCGLREG AILTLLSDIASALRYLHENRIIHRDLKPENIVLQQGEQRLIHKIIDLGYAKELDQGSLCT SFVGTLQYLAPELLEQQKYTVTVDYWSFGTLAFECITGFRPFLPNWQPVQWHSKVRQKSE VDIVVSEDLNGTVKFSSSLPYPNNLNSVLAERLEKWLQLMLMWHPRQRGTDPTYGPNGCF KALDDILNLKLVHILNMVTGTIHTYPVTEDESLQSLKARIQQDTGIPEEDQELLQEAGLA LIPDKPATQCISDGKLNEGHTLDMDLVFLFDNSKITYETQISPRPQPESVSCILQEPKRN LAFFQLRKVWGQVWHSIQTLKEDCNRLQQGQRAAMMNLLRNNSCLSKMKNSMASMSQQLK AKLDFFKTSIQIDLEKYSEQTEFGITSDKLLLAWREMEQAVELCGRENEVKLLVERMMAL QTDIVDLQRSPMGRKQGGTLDDLEEQARELYRRLREKPRDQRTEGDSQEMVRLLLQAIQS FEKKVRVIYTQLSKTVVCKQKALELLPKVEEVVSLMNEDEKTVVRLQEKRQKELWNLLKI ACSKVRGPVSGSPDSMNASRLSQPGQLMSQPSTASNSLPEPAKKSEELVAEAHNLCTLLE NAIQDTVREQDQSFTALDWSWLQTEEEEHSCLEQAS
Related US Patent6,649,654
Target ValidationClick to Find Target Validation Information.    
Inhibitor4-hydroxy-2-nonenal[6]
5-Bromo-6-methoxy-9H-beta-carboline[7]
Arsenite[8]
BMS-345541[4]
MLN0415[5]
PS-1145[9]
S1627[1]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Specific Inhibition of IkappaB kinase reduces hyperalgesia in inflammatory and neuropathic pain models in rats. J Neurosci. 2004 Feb 18;24(7):1637-45. To Reference
Ref 2Activation of I kappa b kinase by herpes simplex virus type 1. A novel target for anti-herpetic therapy. J Biol Chem. 2001 Aug 3;276(31):28759-66. Epub 2001 May 31. To Reference
Ref 3Interleukin-10 signaling blocks inhibitor of kappaB kinase activity and nuclear factor kappaB DNA binding. J Biol Chem. 1999 Nov 5;274(45):31868-74. To Reference
Ref 4A highly selective inhibitor of I kappa B kinase, BMS-345541, blocks both joint inflammation and destruction in collagen-induced arthritis in mice. Arthritis Rheum. 2003 Sep;48(9):2652-9. To Reference
Ref 5Takeda. Product Development Pipeline. July 31 2009. To Reference
Ref 6IkappaB kinase, a molecular target for inhibition by 4-hydroxy-2-nonenal. J Biol Chem. 2001 May 25;276(21):18223-8. Epub 2001 Mar 16. To Reference
Ref 7Bioorg Med Chem Lett. 2003 Jul 21;13(14):2419-22.Novel IKK inhibitors: beta-carbolines. To Reference
Ref 8Inhibition of NF-kappa B activation by arsenite through reaction with a critical cysteine in the activation loop of Ikappa B kinase. J Biol Chem. 2000 Nov 17;275(46):36062-6. To Reference
Ref 9Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127. To Reference



 

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