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

MAP3K2 (Q9Y2U5) - Overview - Molecular Target Synopsis

Protein


MAP3K2, Mitogen-activated protein kinase kinase kinase 2
Enzyme Classification 2.7.11.25
UniProt Q9Y2U5

Also Known as M3K2_HUMAN, MAP3K2, MAPKKK2, MEKK2

Component of a protein kinase signal transduction cascade. Regulates the JNK and ERK5 pathways by phosphorylating and activating MAP2K5 and MAP2K7 (By similarity). Plays a role in caveolae kiss-and-run dynamics. Interacts with PKN2; the interaction activates PKN2 kinase activity in a MAP3K2-independent kinase activity (By similarity). Self-associates. Binds both upstream activators and downstream substrates in multimolecular complexes. Interacts (via the kinase catalytic domain) with STK38. Interacts with XIAP/BIRC4.

5HQ8
10 RESIDUE FRAGMENT OF
MEKK2 PEPTIDE
IN THE STRUCTURE OF
CO-CRYSTAL STRUCTURE OF HUMAN SMYD3 WITH A MEKK2 PEPTIDE AT 2.13A
RCSB/PDB
Inspect Structure
See all 3D Structures for MAP3K2

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
619ENSG00000169967ENST00000409947, ENST00000344908ENSP00000387246, ENSP00000343463Q9Y2U5-1
54ENSG00000169967ENST00000409179ENSP00000386313

Sub-cellular localization


UniProt: MAP3K2 is active in the following subcellular-locations: cytoplasm, nucleus.
GO terms: MAP3K2 is active in the following subcellular-locations: cytoplasm, cytosol, nucleoplasm.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project MAP3K2 has gain in 1 cell-lines, loss in 0 cell-lines and no signal in 1004 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: RXF_393, SK_OV_3, MCF7

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Detroit 562, NCI-H2196, VMRC-LCD

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: MCF-7, HFDPC, SK-N-SH

(see details)

RNA Interference


MAP3K2 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: MDAMB157, HUO3N1. (see details)

3D Structures


For MAP3K2 there are:
4 structures (6 chains) solved
0 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


MAP3K2 has been screened with 121 compounds (128 bioactivities), 19 compounds have bioactivities that show binding affinity of <= 500nM (22 bioactivities). (see details)