Therapeutic Targets Database
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TTD Target ID: TTDC00044

Target Information
NameMAP kinase p38    
Type of targetClinical trial target    
SynonymsERK-6    
ERK5    
ERK6    
Extracellular signal-regulated kinase 6    
MAP kinase p38 gamma    
MAPK12    
Mitogen-activated protein kinase 12    
Mitogen-activated protein kinase p38 gamma    
SAPK3    
Stress-activated protein kinase 3    
DiseaseAnalgesics
[ICD9: 338   ICD10: R52]
[1][2][3]
Cancer, unspecific
[ICD9: 140-229   ICD10: C00-C96]
[4]
Cardiovascular Disorders
[ICD9: 390-459   ICD10: I00-I99]
[4]
Coronary Artery Disease
[ICD9: 410-414, 429.2   ICD10: I20-I25]
[5][6]
Inflammatory Bowel Disease
[ICD9: 555, 556   ICD10: K50, K51]
[4]
Inflammatory Disorders, Unspecified[5][6]
Neurologic Disorders
[ICD9: 320-359   ICD10: G00-G99]
[4]
Oral Facial Pain
[ICD9: 338,780   ICD10: R52, G89]
[4]
Pain, Acute or Chronic
[ICD9: 338,780   ICD10: R52, G89]
[1][2][3]
Psoriasis and Psoriatic Disorders
[ICD9: 696   ICD10: L40]
[7][8]
Rheumatoid arthritis
[ICD9: 714   ICD10: M05-M06]
[9][10]
Drug(s)SCIO-469Phase IIa completedRheumatoid Arthritis[1][2][3]
VX-702Phase IIa completedRheumatoid Arthritis, Coronary Artery Disease[5][6]
KC706Phase II completedInflammatory Bowel Disease, Rheumatoid Arthritis, Cardiovascular Disorders, Psoriasis and Psoriatic Disorders[11]
ARRY-797Phase IIOral Facial Pain[12]
GSK-681323Phase IIRheumatoid arthritis, Chronic obstructive pulmonary disease[13][14]
SB681323Phase IIRheumatoid Arthritis, Coronary Artery Disease, Acute or Chronic Pain, Neurologic Disorders[15]
ARRY-797Phase I completedCancer/Tumors, Inflammatory Disorders[12]
SCIO-469Phase IbAcute or Chronic Pain[1][2][3]
SB681323Phase IChronic rheumatoid Arthritis[15]
VX-702Phase IInflammatory Disorders[5][6]
BIRB 796DiscontinuedPsoriasis and Psoriatic Disorders[7][8]
R1503TerminatedRheumatoid arthritis[13]
VX-745DiscontinuedRheumatoid Arthritis[9][10]
SMP-534PreclinicalDiabetic nephropathy[16]
EC NumberEC 2.7.11.24
PathwayAmyotrophic lateral sclerosis (ALS)
Epithelial cell signaling in Helicobacter pylori
Fc epsilon RI signaling pathway
GnRH signaling pathway
Leukocyte transendothelial migration
MAPK signaling pathway
T cell receptor signaling pathway
Toll-like receptor signaling pathway
VEGF signaling pathway
UniProt IDP53778
PDB Structure1CM8.    
SequenceMSSPPPARSGFYRQEVTKTAWEVRAVYRDLQPVGSGAYGAVCSAVDGRTGAKVAIKKLYR PFQSELFAKRAYRELRLLKHMRHENVIGLLDVFTPDETLDDFTDFYLVMPFMGTDLGKLM KHEKLGEDRIQFLVYQMLKGLRYIHAAGIIHRDLKPGNLAVNEDCELKILDFGLARQADS EMTGYVVTRWYRAPEVILNWMRYTQTVDIWSVGCIMAEMITGKTLFKGSDHLDQLKEIMK VTGTPPAEFVQRLQSDEAKNYMKGLPELEKKDFASILTNASPLAVNLLEKMLVLDAEQRV TAGEALAHPYFESLHDTEDEPQVQKYDDSFDDVDRTLDEWKRVTYKEVLSFKPPRQLGAR VSKETPL
Target ValidationClick to Find Target Validation Information.    
Inhibitor4,5,6,7-tetrabromobenzotriazole[17]
ARRY-797[12]
BIRB 796[7][8]
BIRB796[18]
BISINDOLYLMALEIMIDE IX[19]
CI-1040,   PD-18435,   PD-184352[19]
GF-109203[19]
GSK-681323[13][14]
Go-6976[19]
KC706[11]
KN-62[19]
KT-5720[19]
LY-294002[19]
ML-3163[20]
ML-3375[21]
ML-3403[21]
PD-98059[19]
Phosphoaminophosphonic Acid-Adenylate Ester[22]
Phosphonothreonine[23]
R1503[13]
RO-316233[19]
RWJ-68354[24]
SB-202190[19]
SB-203580[19]
SB681323[15]
SCIO-469[1][2][3]
SK&F-86002,   SK-86002[20]
SMP-534[16]
STAUROSPORINONE[19]
U-0126[19]
VK-19911[25]
VX-702[5][6]
VX-745[9][10]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Investigations of SCIO-469-like compounds for the inhibition of p38 MAP kinase. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1461-4. Epub 2009 Jan 14. To Reference
Ref 2p38alpha-selective MAP kinase inhibitor reduces tumor growth in mouse xenograft models of multiple myeloma. Anticancer Res. 2008 Nov-Dec;28(6A):3827-33. To Reference
Ref 3Analgesic effects of p38 kinase inhibitor treatment on bone fracture healing. Pain. 2009 Mar;142(1-2):116-26. Epub 2009 Jan 23. To Reference
Ref 4CenterWatch. Drugs in Clinical Trials Database. CenterWatch. 2008. To Reference
Ref 5Efficacy, pharmacodynamics, and safety of VX-702, a novel p38 MAPK inhibitor, in rheumatoid arthritis: results of two randomized, double-blind, placebo-controlled clinical studies. Arthritis Rheum. 2009 May;60(5):1232-41. To Reference
Ref 6Drug evaluation: VX-702, a MAP kinase inhibitor for rheumatoid arthritis and acute coronary syndrome. Curr Opin Investig Drugs. 2006 Nov;7(11):1020-5. To Reference
Ref 7Inhibition of p38: has the fat lady sung? Arthritis Rheum. 2009 Feb;60(2):317-20. To Reference
Ref 8Phosphorylation of Ewing's sarcoma protein (EWS) and EWS-Fli1 in response to DNA damage. Biochem J. 2009 Mar 15;418(3):625-34. To Reference
Ref 9P38 MAP kinase inhibitors as potential therapeutics for the treatment of joint degeneration and pain associated with osteoarthritis. J Inflamm (Lond). 2008 Dec 4;5:22. To Reference
Ref 10Rapid synthesis of VX-745: p38 MAP kinase inhibition in Werner syndrome cells. Bioorg Med Chem Lett. 2007 Sep 15;17(18):5107-10. Epub 2007 Jul 13. To Reference
Ref 11KC706, an Oral p38 MAP Kinase Inhibitor, Increases HDL-C. Circulation. 2007;116:II_126. To Reference
Ref 12Array BioPharma Advances p38 Inhibitor, ARRY-797, into Phase 1 Cancer Patient Trial. Array BioPharma. 2007 To Reference
Ref 13Emerging drugs for rheumatoid arthritis. Expert Opin Emerg Drugs. 2008 Mar;13(1):175-96. To Reference
Ref 14Emerging drugs in chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2009 Mar;14(1):181-94. To Reference
Ref 15P38 Mitogen-activated Protein (Map) Kinase Inhibitor (SB-681323)Study In Patients With Neuropathic Pain. GlaxoSmithKline. 2009 To Reference
Ref 16Agents in development for the treatment of diabetic nephropathy. Expert Opin Emerg Drugs. 2008 Sep;13(3):447-63. To Reference
Ref 17J 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 18J 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
Ref 19Biochem J. 2000 Oct 1;351(Pt 1):95-105.Specificity and mechanism of action of some commonly used protein kinase inhibitors. To Reference
Ref 20J Med Chem. 2002 Jun 20;45(13):2733-40.From imidazoles to pyrimidines: new inhibitors of cytokine release. To Reference
Ref 21J Med Chem. 2003 Jul 17;46(15):3230-44.Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes. To Reference
Ref 22Berman 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 23Overington 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 24Bioorg Med Chem Lett. 2003 Feb 10;13(3):347-50.Imidazopyrimidines, potent inhibitors of p38 MAP kinase. To Reference
Ref 25J Med Chem. 2003 Dec 18;46(26):5651-62.Synthesis and structure-activity relationship of aminobenzophenones. A novel class of p38 MAP kinase inhibitors with high antiinflammatory activity. To Reference



 

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