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Literature summary for 2.7.11.25 extracted from

  • Oetjen, E.; Blume, R.; Cierny, I.; Schlag, C.; Kutschenko, A.; Kraetzner, R.; Stein, R.; Knepel, W.
    Inhibition of MafA transcriptional activity and human insulin gene transcription by interleukin-1beta and mitogen-activated protein kinase kinase kinase in pancreatic islet beta cells (2007), Diabetologia, 50, 1678-1687.
    View publication on PubMed

Application

Application Comment Organism
medicine IL-1beta through MEKK1 inhibits human insulin gene transcription and does so, at least in part, by decreasing MafA transcriptional activity at the RIPE3b control element. Since inappropriate insulin biosynthesis contributes to beta cell dysfunction, inhibition of MEKK1 may decelerate or prevent progression from a prediabetic state to diabetes mellitus synthetic construct

Cloned(Commentary)

Cloned (Comment) Organism
expression vector for the catalytic domain of MEKK1 expressed in a beta cell line or in primary pancreatic islets from transgenic mice synthetic construct

Inhibitors

Inhibitors Comment Organism Structure
SB203580 does not relieve the inhibitory effect of MEKK1 on insulin gene transcription, although it effectively decreases phosphorylation of JNK, SAPK/p38 or ERK, respectively synthetic construct
SP600125 does not relieve the inhibitory effect of MEKK1 on insulin gene transcription, although it effectively decreases phosphorylation of JNK, SAPK/p38 or ERK, respectively synthetic construct
U0126 does not relieve the inhibitory effect of MEKK1 on insulin gene transcription, although it effectively decreases phosphorylation of JNK, SAPK/p38 or ERK, respectively synthetic construct

Organism

Organism UniProt Comment Textmining
synthetic construct
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining

Synonyms

Synonyms Comment Organism
MEKK1
-
synthetic construct
mitogen-activated protein kinase kinase kinase 1
-
synthetic construct