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

MAP3K1 (Q13233) - Overview - Molecular Target Synopsis

Protein


MAP3K1, Mitogen-activated protein kinase kinase kinase 1
Enzyme Classification 2.7.11.25
UniProt Q13233

Also Known as M3K1_HUMAN, MAP3K1, MAPKKK1, MEKK, MEKK1

Component of a protein kinase signal transduction cascade (PubMed:9808624). Activates the ERK and JNK kinase pathways by phosphorylation of MAP2K1 and MAP2K4 (PubMed:9808624). May phosphorylate the MAPK8/JNK1 kinase (PubMed:17761173). Activates CHUK and IKBKB, the central protein kinases of the NF-kappa-B pathway (PubMed:9808624). Binds both upstream activators and downstream substrates in multimolecular complexes through its N-terminus (PubMed:9808624). Oligomerizes after binding MAP2K4 or TRAF2 (PubMed:9808624). Interacts with AXIN1 (PubMed:12223491, PubMed:15262978). Interacts (via the kinase catalytic domain) with STK38 (PubMed:17906693). Interacts with GRIPAP1 (PubMed:17761173).

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
1512ENSG00000095015ENST00000399503ENSP00000382423Q13233-1

Sub-cellular localization


GO terms: MAP3K1 is active in the following subcellular-locations: cytoplasm, cytosol.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project MAP3K1 has gain in 2 cell-lines, loss in 3 cell-lines and no signal in 1000 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: T47D, RPMI_8226, M14

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: WSU-FSCCL, CHP-212, Toledo

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, CD20-positive B cell, CD14-positive monocyte

(see details)

RNA Interference


MAP3K1 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: MDAMB453, A427. (see details)

3D Structures


At greater than 35% identity similarity to MAP3K1 there are:
18 structures (40 chains) solved
18 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


MAP3K1 has been screened with 145 compounds (158 bioactivities), 4 compounds have bioactivities that show binding affinity of <= 500nM (4 bioactivities). (see details)