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

MAP3K20 (Q9NYL2) - Overview - Molecular Target Synopsis

Protein


MAP3K20, Mitogen-activated protein kinase kinase kinase 20
Enzyme Classification 2.7.11.25
UniProt Q9NYL2

Also Known as M3K20_HUMAN, MAP3K20, MLTK, ZAK

Stress-activated component of a protein kinase signal transduction cascade. Regulates the JNK and p38 pathways. Part of a signaling cascade that begins with the activation of the adrenergic receptor ADRA1B and leads to the activation of MAPK14. Pro-apoptotic. Role in regulation of S and G2 cell cycle checkpoint by direct phosphorylation of CHEK2 (PubMed:10924358, PubMed:11836244, PubMed:15342622, PubMed:21224381). Involved in limb development (PubMed:26755636)., Isoform 1: Phosphorylates histone H3 at 'Ser-28' (PubMed:15684425). May have role in neoplastic cell transformation and cancer development (PubMed:15172994). Causes cell shrinkage and disruption of actin stress fibers (PubMed:11042189). Homodimer (PubMed:10924358, PubMed:26755636). Interacts with PKN1 and ZNF33A (PubMed:12535642, PubMed:12761180). Component of a signaling complex containing at least AKAP13, PKN1, MAPK14, MAP3K20 and MAP2K3. Within this complex, AKAP13 interacts directly with PKN1, which in turn recruits MAPK14, MAP2K3 and MAP3K20 (PubMed:21224381).

5X5O
CRYSTAL STRUCTURE OF ZAK IN COMPLEX WITH COMPOUND D2829
RCSB/PDB
Inspect Structure
See all 3D Structures for MAP3K20

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: MAP3K20 is active in the following subcellular-locations: cytoplasm, nucleus.
GO terms: MAP3K20 is active in the following subcellular-locations: cytoplasm, cytosol, nucleus.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project MAP3K20 has gain in 3 cell-lines, loss in 2 cell-lines and no signal in 999 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are:

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

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:

(see details)

RNA Interference


MAP3K20 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: COV504, LM7. (see details)

3D Structures


For MAP3K20 there are:
2 structures (3 chains) solved
2 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

MAP3K20 is solved in complex with the approved drug(s):

032/VEMURAFENIB (5HES_A, 5HES_B).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


MAP3K20 has been screened with 158 compounds (198 bioactivities), 11 compounds have bioactivities that show binding affinity of <= 500nM (17 bioactivities). (see details)