Target intelligence / Profile preview

Dual specificity mitogen-activated protein kinase kinase 3 (MAP2K3 (also commonly called MKK3))

Target
MAP2K3 (also commonly called MKK3)
Molecular classification
Enzyme, Kinase, Dual specificity protein kinase, Mitogen-activated protein kinase kinase family
01

Overview

Dual specificity mitogen-activated protein kinase kinase 3 (MAP2K3, also known as MKK3) is a serine/threonine and tyrosine kinase that functions as an upstream activator in the MAP kinase signaling cascade, especially the p38 MAPK pathway. It is activated by various stress signals, cytokines, and mitogens, and in turn phosphorylates and activates p38 MAPKs, which mediate diverse cellular processes such as inflammation, cell proliferation, differentiation, apoptosis, and response to environmental stress. MAP2K3 has gained attention as a molecular target in cancer therapy due to its role in promoting tumor cell survival and proliferation, particularly in tumors with mutant p53. It is also involved in cardiovascular and inflammatory responses. While not yet a common direct therapeutic target, it remains under active research for its roles in disease and potential for targeted intervention in oncology and other areas.

Other names
MAP kinase kinase 3MAPK/ERK kinase 3MAPKK 3MEK3MKK3PRKMK3SAPK kinase 2SAPKK-2SAPKK2SKK2Stress-activated protein kinase kinase 2
02

Mechanism of action

Competitive inhibition of kinase activity RNA interference (siRNA or shRNA knockdown) leading to reduced protein levels and downstream signaling

03

Biological functions

Signal transductionPhosphorylation of p38 MAPK family (p38α/β/γ/δ)Cellular response to stress and mitogenic stimuliRegulation of cell proliferation, differentiation, apoptosis, migration, invasion
04

Disease associations

Cancer (tumor progression, invasion, therapeutic resistance)InflammationCardiovascular disease (vascular endothelial function, cardiac muscle contraction)Other (response to infection, cell stress)
05

Safety considerations

Targeting MAP2K3 could affect normal cellular stress responses, possibly causing off-target toxicities or impairing normal cell survival, especially under stress conditions.As a kinase, inhibition may have unintended effects on related protein kinase pathways.
06

Interacting drugs

No specific, approved drugs directly targeting MAP2K3 are widely documented. However, experimental inhibitors and RNA interference approaches have been used in preclinical models.

1 more in the full profile.

07

Biomarkers

Phosphorylation status of p38 MAPK (downstream of MAP2K3)Expression levels of MAP2K3 mRNA or protein in tumor samples

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