Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

MAP2K3 (P46734) - Overview - Molecular Target Synopsis

Protein


MAP2K3, Dual specificity mitogen-activated protein kinase kinase 3
Enzyme Classification 2.7.12.2
UniProt P46734

Also Known as MP2K3_HUMAN, MAP2K3, MEK3, MKK3, PRKMK3, SKK2

Dual specificity kinase. Is activated by cytokines and environmental stress in vivo. Catalyzes the concomitant phosphorylation of a threonine and a tyrosine residue in the MAP kinase p38. Part of a signaling cascade that begins with the activation of the adrenergic receptor ADRA1B and leads to the activation of MAPK14. Component of a signaling complex containing at least AKAP13, PKN1, MAPK14, ZAK and MAP2K3. Within this complex, AKAP13 interacts directly with PKN1, which in turn recruits MAPK14, MAP2K3 and ZAK (PubMed:21224381). Binds to DYRK1B/MIRK and increases its kinase activity (PubMed:11980910). Part of a complex with MAP3K3, RAC1 and CCM2 (By similarity). Interacts with ARRB1 (PubMed:16709866). Interacts with Yersinia yopJ (PubMed:16728640).

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


GO terms: MAP2K3 is active in the following subcellular-locations: cytoplasm, cytosol, membrane, nucleoplasm.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project MAP2K3 has gain in 6 cell-lines, loss in 10 cell-lines and no signal in 989 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SN12C, KM12, SK_MEL_2

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: MFM-223, JHH-7, NCI-H322T

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: SK-N-SH, NHLF, A549

(see details)

RNA Interference


MAP2K3 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: CAL120, MDAMB134VI. (see details)

3D Structures


At greater than 75% identity similarity to MAP2K3 there are:
3 structures (6 chains) solved
2 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


MAP2K3 has been screened with 146 compounds (185 bioactivities), 13 compounds have bioactivities that show binding affinity of <= 500nM (15 bioactivities). (see details)