Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDR00148

Target Information
NameDual specificity mitogen-activated protein kinase kinase 1    
Type of targetSuccessful target    
SynonymsERK activator kinase 1    
MAP kinase kinase 1    
MAPK/ERK kinase 1    
MAPKK 1    
MEK1    
Mitogen-activated protein kinase kinase 1    
DiseaseBreast cancer
[ICD9: 174, 175   ICD10: C50]
[1]
Prostate cancer
[ICD9: 185   ICD10: C61]
[2]
BioChemical ClassTransferases transferring phosphorus-containing groups    
EC NumberEC 2.7.1.-
PathwayAcute myeloid leukemia
B cell receptor signaling pathway
Bladder cancer
Chemokine signaling pathway
Chronic myeloid leukemia
Colorectal cancer
Endometrial cancer
ErbB signaling pathway
Fc epsilon RI signaling pathway
Focal adhesion
Gap junction
Glioma
GnRH signaling pathway
Insulin signaling pathway
Long-term depression
Long-term potentiation
MAPK signaling pathway
Melanogenesis
Melanoma
Natural killer cell mediated cytotoxicity
Non-small cell lung cancer
Pancreatic cancer
Pathways in cancer
Prostate cancer
Regulation of actin cytoskeleton
Renal cell carcinoma
T cell receptor signaling pathway
Thyroid cancer
Toll-like receptor signaling pathway
VEGF signaling pathway
Vascular smooth muscle contraction
UniProt IDQ02750
PDB Structure1S9J; 2P55; 3EQB; 3EQC; 3EQD; 3EQF; 3EQG; 3EQH.    
FunctionCatalyzes the concomitant phosphorylation of a threonine and a tyrosine residue in a thr-glu-tyr sequence located in map kinases. Activates erk1 and erk2 map kinases.    
SequenceMPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKV GELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARKLIHLEIKPAIRNQIIRELQVLHE CNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYL REKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHY SVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSY GMDSRPPMAIFELLDYIVNEPPPKLPSGVFSLEFQDFVNKCLIKNPAERADLKQLMVHAF IKRSDAEEVDFAGWLCSTIGLNQPSTPTHAAGV
Related US Patent6,319,955
Target ValidationClick to Find Target Validation Information.    
Inhibitor4,5,6,7-tetrabromobenzotriazole[3]
4,5-Dibromo-1H-pyrrole-2-carboxylic acid amide[4]
5-phenylamino-4-cyano-3-hydroxy-isothiazole[5]
ALDISIN[4]
AZD-0530[6]
DEBROMOHYMENIALDISINE[4]
K-252a[7]
OROIDIN[4]
PD-98059[4]
REVERSINE[8]
U-0126[9]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Role of extracellular signal-regulated kinase pathway in RRR-alpha-tocopheryl succinate-induced differentiation of human MDA-MB-435 breast cancer cells. Mol Carcinog. 2002 Apr;33(4):228-36. To Reference
Ref 2NF-kappa B activates prostate-specific antigen expression and is upregulated in androgen-independent prostate cancer. Mol Cell Biol. 2002 Apr;22(8):2862-70. To Reference
Ref 3J 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 4J Med Chem. 2002 Jan 17;45(2):529-32.Aldisine alkaloids from the Philippine sponge Stylissa massa are potent inhibitors of mitogen-activated protein kinase kinase-1 (MEK-1). To Reference
Ref 5Bioorg Med Chem Lett. 2006 Aug 1;16(15):3975-80. Epub 2006 May 24.Discovery of 3-hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles as potent MEK1 inhibitors. To Reference
Ref 6J Med Chem. 2006 Nov 2;49(22):6465-88.N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor. 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 8Proc Natl Acad Sci U S A. 2007 Jun 19;104(25):10482-7. Epub 2007 Jun 12.Reversine increases the plasticity of lineage-committed mammalian cells. To Reference
Ref 9Bioorg Med Chem. 2010 Nov 15;18(22):8054-60. Epub 2010 Oct 19.Structure-activity relationships of benzimidazole-based selective inhibitors of the mitogen activated kinase-5 signaling pathway. To Reference



 

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