Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T55729
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| Former ID |
TTDR00352
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| Target Name |
Mitogen-activated protein kinase 11
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| Gene Name |
MAPK11
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| Synonyms |
MAP kinase p38 beta; Mitogen-activated protein kinase p38 beta; P38 Mitogen-activated protein kinase beta; P38-2; P38b; Stress-activated protein kinase-2; MAPK11
|
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| Target Type |
Clinical Trial
|
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| Disease | Psoriasis [ICD9: 696; ICD10: L40] | ||||
| Function |
Kinase involved in a signal transduction pathway that is activated by changes in the osmolarity of the extracellular environment, by cytokines, or by environmental stress. Phosphorylates preferentially transcription factor atf2.
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| BioChemical Class |
Kinase
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| Target Validation |
T55729
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| UniProt ID | |||||
| EC Number |
EC 2.7.11.24
|
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| Sequence |
MSGPRAGFYRQELNKTVWEVPQRLQGLRPVGSGAYGSVCSAYDARLRQKVAVKKLSRPFQ
SLIHARRTYRELRLLKHLKHENVIGLLDVFTPATSIEDFSEVYLVTTLMGADLNNIVKCQ ALSDEHVQFLVYQLLRGLKYIHSAGIIHRDLKPSNVAVNEDCELRILDFGLARQADEEMT GYVATRWYRAPEIMLNWMHYNQTVDIWSVGCIMAELLQGKALFPGSDYIDQLKRIMEVVG TPSPEVLAKISSEHARTYIQSLPPMPQKDLSSIFRGANPLAIDLLGRMLVLDSDQRVSAA EALAHAYFSQYHDPEDEPEAEPYDESVEAKERTLEEWKELTYQEVLSFKPPEPPKPPGSL EIEQ |
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| Drugs and Mode of Action | |||||
| Drug(s) | CI-1040 | Drug Info | Phase 2 | Discovery agent | [1], [2] |
| SB 235699 | Drug Info | Discontinued in Phase 1 | Psoriasis | [3] | |
| Inhibitor | 4,5,6,7-tetrabromo-1H-benzo[d][1,2,3]triazole | Drug Info | [4] | ||
| BISINDOLYLMALEIMIDE IX | Drug Info | [5] | |||
| CI-1040 | Drug Info | [5] | |||
| GF-109203 | Drug Info | [5] | |||
| KN-62 | Drug Info | [5] | |||
| KT-5720 | Drug Info | [5] | |||
| L-779450 | Drug Info | [6] | |||
| ML-3163 | Drug Info | [7] | |||
| ML-3375 | Drug Info | [8] | |||
| ML-3403 | Drug Info | [8] | |||
| RO-316233 | Drug Info | [5] | |||
| RWJ-68354 | Drug Info | [9] | |||
| SB 235699 | Drug Info | [10] | |||
| STAUROSPORINONE | Drug Info | [5] | |||
| Vertex 745 (VX745) | Drug Info | [10] | |||
| VK-19911 | Drug Info | [11] | |||
| Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
| TEP | EXP Info | ||||
| Pathways | |||||
| KEGG Pathway | MAPK signaling pathway | ||||
| Rap1 signaling pathway | |||||
| FoxO signaling pathway | |||||
| Sphingolipid signaling pathway | |||||
| Adrenergic signaling in cardiomyocytes | |||||
| VEGF signaling pathway | |||||
| Osteoclast differentiation | |||||
| Signaling pathways regulating pluripotency of stem cells | |||||
| Platelet activation | |||||
| Toll-like receptor signaling pathway | |||||
| NOD-like receptor signaling pathway | |||||
| RIG-I-like receptor signaling pathway | |||||
| T cell receptor signaling pathway | |||||
| Fc epsilon RI signaling pathway | |||||
| TNF signaling pathway | |||||
| Leukocyte transendothelial migration | |||||
| Neurotrophin signaling pathway | |||||
| Retrograde endocannabinoid signaling | |||||
| Dopaminergic synapse | |||||
| Inflammatory mediator regulation of TRP channels | |||||
| GnRH signaling pathway | |||||
| Progesterone-mediated oocyte maturation | |||||
| Prolactin signaling pathway | |||||
| Amyotrophic lateral sclerosis (ALS) | |||||
| Epithelial cell signaling in Helicobacter pylori infection | |||||
| Shigellosis | |||||
| Salmonella infection | |||||
| Pertussis | |||||
| Leishmaniasis | |||||
| Chagas disease (American trypanosomiasis) | |||||
| Toxoplasmosis | |||||
| Tuberculosis | |||||
| Hepatitis C | |||||
| Influenza A | |||||
| Epstein-Barr virus infection | |||||
| Proteoglycans in cancer | |||||
| PANTHER Pathway | Alzheimer disease-amyloid secretase pathway | ||||
| B cell activation | |||||
| EGF receptor signaling pathway | |||||
| FGF signaling pathway | |||||
| Interferon-gamma signaling pathway | |||||
| Oxidative stress response | |||||
| TGF-beta signaling pathway | |||||
| Ras Pathway | |||||
| p53 pathway feedback loops 2 | |||||
| p38 MAPK pathway | |||||
| Pathway Interaction Database | p73 transcription factor network | ||||
| p38 MAPK signaling pathway | |||||
| Plasma membrane estrogen receptor signaling | |||||
| CD40/CD40L signaling | |||||
| Regulation of p38-alpha and p38-beta | |||||
| FAS (CD95) signaling pathway | |||||
| Thromboxane A2 receptor signaling | |||||
| Glucocorticoid receptor regulatory network | |||||
| IL2-mediated signaling events | |||||
| Rapid glucocorticoid signaling | |||||
| ATF-2 transcription factor network | |||||
| IL6-mediated signaling events | |||||
| p38 signaling mediated by MAPKAP kinases | |||||
| CXCR3-mediated signaling events | |||||
| Signaling mediated by p38-alpha and p38-beta | |||||
| Signaling events mediated by VEGFR1 and VEGFR2 | |||||
| VEGFR3 signaling in lymphatic endothelium | |||||
| Regulation of retinoblastoma protein | |||||
| PathWhiz Pathway | Intracellular Signalling Through Adenosine Receptor A2a and Adenosine | ||||
| Intracellular Signalling Through Adenosine Receptor A2b and Adenosine | |||||
| Reactome | NOD1/2 Signaling Pathway | ||||
| p38MAPK events | |||||
| ERK/MAPK targets | |||||
| Activation of PPARGC1A (PGC-1alpha) by phosphorylation | |||||
| Oxidative Stress Induced Senescence | |||||
| CDO in myogenesis | |||||
| DSCAM interactions | |||||
| VEGFA-VEGFR2 Pathway | |||||
| activated TAK1 mediates p38 MAPK activation | |||||
| Activation of the AP-1 family of transcription factors | |||||
| KSRP (KHSRP) binds and destabilizes mRNA | |||||
| WikiPathways | Toll-like receptor signaling pathway | ||||
| Insulin Signaling | |||||
| IL-4 Signaling Pathway | |||||
| MAP kinase activation in TLR cascade | |||||
| Regulation of mRNA Stability by Proteins that Bind AU-rich Elements | |||||
| Nanoparticle-mediated activation of receptor signaling | |||||
| Structural Pathway of Interleukin 1 (IL-1) | |||||
| Parkinsons Disease Pathway | |||||
| NGF signalling via TRKA from the plasma membrane | |||||
| Myogenesis | |||||
| DSCAM interactions | |||||
| Physiological and Pathological Hypertrophy of the Heart | |||||
| Regulation of toll-like receptor signaling pathway | |||||
| References | |||||
| REF 1 | ClinicalTrials.gov (NCT00033384) CI-1040 in Treating Patients With Advanced Breast, Colon, Pancreatic, or Non-Small Cell Lung Cancer. U.S. National Institutes of Health. | ||||
| REF 2 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5676). | ||||
| REF 3 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012315) | ||||
| REF 4 | J Med Chem. 2004 Dec 2;47(25):6239-47.Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole. | ||||
| REF 5 | Biochem J. 2000 Oct 1;351(Pt 1):95-105.Specificity and mechanism of action of some commonly used protein kinase inhibitors. | ||||
| REF 6 | Bioorg Med Chem Lett. 2006 Jan 15;16(2):378-81. Epub 2005 Nov 2.The identification of potent and selective imidazole-based inhibitors of B-Raf kinase. | ||||
| REF 7 | J Med Chem. 2002 Jun 20;45(13):2733-40.From imidazoles to pyrimidines: new inhibitors of cytokine release. | ||||
| REF 8 | J 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. | ||||
| REF 9 | Bioorg Med Chem Lett. 2003 Feb 10;13(3):347-50.Imidazopyrimidines, potent inhibitors of p38 MAP kinase. | ||||
| REF 10 | Pharmacological inhibitors of MAPK pathways. Trends Pharmacol Sci. 2002 Jan;23(1):40-5. | ||||
| REF 11 | J 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. | ||||
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