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

MAP3K3 (Q99759) - Overview - Molecular Target Synopsis

Protein


MAP3K3, Mitogen-activated protein kinase kinase kinase 3
Enzyme Classification 2.7.11.25
UniProt Q99759

Also Known as M3K3_HUMAN, MAP3K3, MAPKKK3, MEKK3

Component of a protein kinase signal transduction cascade. Mediates activation of the NF-kappa-B, AP1 and DDIT3 transcriptional regulators. Binds both upstream activators and downstream substrates in multimolecular complexes. Part of a complex with MAP2K3, RAC1 and CCM2. Interacts with MAP2K5 and SPAG9.

4Y5O
CCM2 HHD IN COMPLEX WITH MEKK3 NPB1
RCSB/PDB
Inspect Structure
See all 3D Structures for MAP3K3

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


GO terms: MAP3K3 is active in the following subcellular-locations: cytoplasm, cytosol.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project MAP3K3 has gain in 5 cell-lines, loss in 0 cell-lines and no signal in 999 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SR, MDA_MB_231, MDA_MB_435

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: MeWo, COLO 792, HT-144

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, HUVEC, NHLF

(see details)

RNA Interference


MAP3K3 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: MFM223, G292. (see details)

3D Structures


For MAP3K3 there are:
6 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


MAP3K3 has been screened with 114 compounds (121 bioactivities), 16 compounds have bioactivities that show binding affinity of <= 500nM (19 bioactivities). (see details)