Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDR01206

Target Information
NameInhibitor of nuclear factor kappa B kinase beta subunit    
Type of targetResearch target    
SynonymsI-kappa-B kinase 2    
I-kappa-B-kinase beta    
IKK-2    
IKK-B    
IKK-beta    
IKK2    
IKKbeta    
IkBKB    
IkappaB kinase 2    
IkappaB kinase beta    
Inhibitory kappa B kinase b    
NFKBIKB    
Nuclear factor NF-kappa-B inhibitor kinase beta    
DiseaseAsthma
[ICD9: 493   ICD10: J45]
[1]
Autoimmune diseases
[ICD9: 279.4   ICD10: D84.9, M35.9]
[2]
Fibrosing alveolitis
[ICD9: 516.3   ICD10: J84.1]
[3]
Inflammation[4]
Inflammatory lung disease[1]
Rheumatoid arthritis, unspecified
[ICD9: 710-719, 714   ICD10: M00-M25, M05-M06]
[5]
Transplant failure or rejection[2]
BioChemical ClassTransferases transferring phosphorus-containing groups    
EC NumberEC 2.7.1.-
EC 2.7.1.37
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
PDB Structure3BRT; 3BRV.    
FunctionPhosphorylates inhibitors of nf-kappa-b thus leading to the dissociation of the inhibitor/nf-kappa-b complex and ultimately the degradation of the inhibitor. Also phosphorylates ncoa3 (by similarity).    
SequenceMSWSPSLTTQTCGAWEMKERLGTGGFGNVIRWHNQETGEQIAIKQCRQELSPRNRERWCL EIQIMRRLTHPNVVAARDVPEGMQNLAPNDLPLLAMEYCQGGDLRKYLNQFENCCGLREG AILTLLSDIASALRYLHENRIIHRDLKPENIVLQQGEQRLIHKIIDLGYAKELDQGSLCT SFVGTLQYLAPELLEQQKYTVTVDYWSFGTLAFECITGFRPFLPNWQPVQWHSKVRQKSE VDIVVSEDLNGTVKFSSSLPYPNNLNSVLAERLEKWLQLMLMWHPRQRGTDPTYGPNGCF KALDDILNLKLVHILNMVTGTIHTYPVTEDESLQSLKARIQQDTGIPEEDQELLQEAGLA LIPDKPATQCISDGKLNEGHTLDMDLVFLFDNSKITYETQISPRPQPESVSCILQEPKRN LAFFQLRKVWGQVWHSIQTLKEDCNRLQQGQRAAMMNLLRNNSCLSKMKNSMASMSQQLK AKLDFFKTSIQIDLEKYSEQTEFGITSDKLLLAWREMEQAVELCGRENEVKLLVERMMAL QTDIVDLQRSPMGRKQGGTLDDLEEQARELYRRLREKPRDQRTEGDSQEMVRLLLQAIQS FEKKVRVIYTQLSKTVVCKQKALELLPKVEEVVSLMNEDEKTVVRLQEKRQKELWNLLKI ACSKVRGPVSGSPDSMNASRLSQPGQLMSQPSTASNSLPEPAKKSEELVAEAHNLCTLLE NAIQDTVREQDQSFTALDWSWLQTEEEEHSCLEQAS
Target ValidationClick to Find Target Validation Information.    
Inhibitor2-amino-5-phenylthiophene-3-carboxamide[6]
2-amino-quinoline-3-carboxylic acid amide[6]
3-amino-5- (4-chlorophenyl)thiophene-2-carboxamide[6]
3-amino-benzo[b]thiophene-2-carboxylic acid amide[6]
4-amino-biphenyl-3-carboxylic acid amide[6]
5-Bromo-6-methoxy-9H-beta-carboline[7]
5-amino-2-p-tolyl-oxazole-4-carboxylic acid amide[6]
5-amino-2-phenyl-oxazole-4-carboxylic acid amide[6]
6-phenyl-thieno[3,2-d]pyrimidin-4-ylamine[6]
PF-228[8]
Parthenolide[4]
SC-514[9]
Staurosporine[10]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1IkappaB kinase is a critical regulator of chemokine expression and lung inflammation in respiratory syncytial virus infection. J Virol. 2004 Mar;78(5):2232-41. To Reference
Ref 2Ikappa B kinase 2 but not NF-kappa B-inducing kinase is essential for effective DC antigen presentation in the allogeneic mixed lymphocyte reaction. Blood. 2003 Feb 1;101(3):983-91. Epub 2002 Sep 19. To Reference
Ref 3Nuclear factor-kappaB activation in alveolar macrophages requires IkappaB kinase-beta, but not nuclear factor-kappaB inducing kinase. Am J Respir Crit Care Med. 2002 Apr 1;165(7):996-1004. To Reference
Ref 4The anti-inflammatory natural product parthenolide from the medicinal herb Feverfew directly binds to and inhibits IkappaB kinase. Chem Biol. 2001 Aug;8(8):759-66. To Reference
Ref 5Heterogeneous requirement of IkappaB kinase 2 for inflammatory cytokine and matrix metalloproteinase production in rheumatoid arthritis: implications for therapy. Arthritis Rheum. 2003 Jul;48(7):1901-12. To Reference
Ref 6J Med Chem. 2006 May 18;49(10):2898-908.Evolution of the thienopyridine class of inhibitors of IkappaB kinase-beta: part I: hit-to-lead strategies. To Reference
Ref 7Bioorg Med Chem Lett. 2003 Jul 21;13(14):2419-22.Novel IKK inhibitors: beta-carbolines. To Reference
Ref 8J Biol Chem. 2007 May 18;282(20):14845-52. Epub 2007 Mar 28.Cellular characterization of a novel focal adhesion kinase inhibitor. To Reference
Ref 9Biochem J. 2007 Dec 15;408(3):297-315.The selectivity of protein kinase inhibitors: a further update. To Reference
Ref 10UCN-01: a potent abrogator of G2 checkpoint function in cancer cells with disrupted p53. J Natl Cancer Inst. 1996 Jul 17;88(14):956-65. To Reference



 

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