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Literature summary for 2.7.11.24 extracted from

  • Daouti, S.; Wang, H.; Li, W.H.; Higgins, B.; Kolinsky, K.; Packman, K.; Specian, A.; Kong, N.; Huby, N.; Wen, Y.; Xiang, Q.; Podlaski, F.J.; He, Y.; Fotouhi, N.; Heimbrook, D.; Niu, H.
    Characterization of a novel mitogen-activated protein kinase kinase 1/2 inhibitor with a unique mechanism of action for cancer therapy (2009), Cancer Res., 69, 1924-1932.
    View publication on PubMed
Search for more literature for 2.7.11.24

Activating Compound

Activating Compound Comment Organism Structure
additional information activated by phosphorylation Homo sapiens

Application

Application Comment Organism
medicine RO4927350 represents a novel therapeutic modality in cancers with aberrant MAPK pathway activation Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
-
 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2S,3S)-2-[(R)-4-[4-(2-hydroxy-ethoxy)-phenyl]-2,5-dioxo-imidazolidin-1-yl]-3-phenyl-N-(4-propionyl-thiazol-2-yl)-butyramide RO4927350 Homo sapiens
FR180204 ERK inhibitor, 5-(2-phenyl-pyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-ylamine Homo sapiens
U0126 MEK inhibitor 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
DU-145 cell
-
 Homo sapiens
-
HT-29 cell
-
 Homo sapiens
-
LOX cell
-
 Homo sapiens
-
MCF-7 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 + FITC-Aca-Ala-Ala-Ala-Thr-Gly-Pro-Leu-Ser-Pro-Gly-Pro-Phe-Ala-NH2 FITC-labeled ERK substrate peptide Homo sapiens ADP + phosphorylated FITC-Aca-Ala-Ala-Ala-Thr-Gly-Pro-Leu-Ser-Pro-Gly-Pro-Phe-Ala-NH2
-
 ?

Synonyms

Synonyms Comment Organism
ERK1/2
-
 Homo sapiens
MAP kinase
-
 Homo sapiens
MEK1/2
-
 Homo sapiens
mitogen-activated kinase
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 kinase assay Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7
-
 kinase assay Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000023
-
 MEK1 Homo sapiens (2S,3S)-2-[(R)-4-[4-(2-hydroxy-ethoxy)-phenyl]-2,5-dioxo-imidazolidin-1-yl]-3-phenyl-N-(4-propionyl-thiazol-2-yl)-butyramide

General Information

General Information Comment Organism
physiological function the MAPK pathway, via the Ras/Raf/MEK/ERK signal cascade, is responsible for transmitting and amplifying mitogenic signals from the cell surface to the nucleus where activated transcription factors regulate gene expression and determine cell fate Homo sapiens