U0126, Selective MKK inhibitor

Supplementary info

This supplementary information is collated from multiple sources and compiled automatically.

Activity summary

MEK1 and MEK2 also known as MAP2K1 and MAP2K2 are protein kinases with molecular weights approximately 43 kDa and 45 kDa respectively. These proteins belong to the MAPKK family and function as dual-specificity kinases phosphorylating both serine/threonine and tyrosine residues. MEK1 and MEK2 are expressed ubiquitously in human tissues indicating their widespread role in cellular processes. Their main mechanical role is to activate ERK1/2 which is important in various signal transduction pathways. As part of the MAPK/ERK cascade MEK proteins serve as a conduit for signals from the membrane to the nucleus.

Biological function summary

MEK1 and MEK2 participate in transmitting signals that regulate cell proliferation differentiation and survival. Their role in these processes involves forming part of a signaling complex that includes RAF kinases and ERK1/2. This assembly ensures precise regulation of cell cycle events and growth responses to extracellular signals. The activity of MEK proteins allows cells to modulate responses to external growth factors and stress maintaining cellular homoeostasis. Given their involvement in key biological processes MEK1 and MEK2 are essential for normal cellular function.

Pathways

MEK1 and MEK2 play significant roles in the MAPK/ERK and PI3K/Akt pathways. Their activation by upstream kinases like RAF enables downstream phosphorylation and activation of ERK1/2 key regulators of gene expression and cellular activities. The MAPK/ERK pathway interconnects with other pathways such as the PI3K/Akt pathway creating a network of signals important for cell fate decisions. Through these pathways MEK1 and MEK2 interact with a variety of proteins including PI3K and Akt linking growth factor signaling to broader cellular outcomes.

Associated diseases and disorders

MEK1 and MEK2 exhibit distinct connections to cancers and RASopathies. Aberrant activation of the MAPK/ERK pathway often through mutations in MEK1/2 contributes to oncogenesis in several cancer types including melanoma and colorectal cancer. Additionally changes in these proteins are implicated in RASopathies such as Noonan syndrome a series of genetic disorders caused by dysregulation of the RAS-MAPK pathway. In these conditions MEK proteins often show altered interactions with other proteins like RAF and RAS correlating with disease pathogenesis and progression.