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Literature summary for 2.7.11.24 extracted from

  • Hope, H.R.; Anderson, G.D.; Burnette, B.L.; Compton, R.P.; Devraj, R.V.; Hirsch, J.L.; Keith, R.H.; Li, X.; Mbalaviele, G.; Messing, D.M.; Saabye, M.J.; Schindler, J.F.; Selness, S.R.; Stillwell, L.I.; Webb, E.G.; Zhang, J.; Monahan, J.B.
    Anti-inflammatory properties of a novel N-phenyl pyridinone inhibitor of p38 mitogen-activated protein kinase: preclinical-to-clinical translation (2009), J. Pharmacol. Exp. Ther., 331, 882-895.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
mitogen-activated protein kinase kinase 6 MKK6 Homo sapiens

Application

Application Comment Organism
medicine p38 MAP kinase inhibition constitutes a promising therapeutic strategy for treatment of chronic inflammatory diseases, based upon its potential to inhibit key pathways driving the inflammatory and destructive processes in these debilitating diseases Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
3-(3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl)-N,4-dimethylbenzamide PH-797804, ATP-competitive, readily reversible inhibitor of the alpha isoform of human p38 MAP kinase Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + a protein Homo sapiens
-
ADP + a phosphoprotein
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
phosphoprotein
-
Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
monocyte
-
Homo sapiens
-
rheumatoid arthritis synovial fibroblast RASF Homo sapiens
-
synovial tissue
-
Homo sapiens
-
U-937 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + a protein
-
Homo sapiens ADP + a phosphoprotein
-
?
ATP + GST-c-Jun substrate in kinase activity assay Homo sapiens ADP + phosphorylated GST-c-Jun
-
?
ATP + protein EGFRP epidermal growth factor receptor peptide, substrate in kinase activity assay Homo sapiens ADP + phosphorylated protein EGFRP
-
?

Synonyms

Synonyms Comment Organism
p38 mitogen-activated protein kinase
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
kinase activity assay Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
kinase activity assay Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000058
-
3-(3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl)-N,4-dimethylbenzamide
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000026
-
-
Homo sapiens 3-(3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl)-N,4-dimethylbenzamide

General Information

General Information Comment Organism
physiological function signal transduction through the p38 mitogen-activated protein kinase pathway is central to the transcriptional and translational control of cytokine and inflammatory mediator production Homo sapiens