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

MAP3K11 (Q16584) - Overview - Molecular Target Synopsis

Protein


MAP3K11, Mitogen-activated protein kinase kinase kinase 11
Enzyme Classification 2.7.11.25
UniProt Q16584

Also Known as M3K11_HUMAN, MAP3K11, MLK3, PTK1, SPRK

Activates the JUN N-terminal pathway. Required for serum-stimulated cell proliferation and for mitogen and cytokine activation of MAPK14 (p38), MAPK3 (ERK) and MAPK8 (JNK1) through phosphorylation and activation of MAP2K4/MKK4 and MAP2K7/MKK7. Plays a role in mitogen-stimulated phosphorylation and activation of BRAF, but does not phosphorylate BRAF directly. Influences microtubule organization during the cell cycle. Homodimer; undergoes dimerization during activation (PubMed:9829970). Interacts with MAP2K4/MKK4 (By similarity). Interacts with MAP2K7/MKK7 (PubMed:9003778). Found in a complex with SH3RF1, RAC1, MAP2K7/MKK7, MAPK8IP1/JIP1 and MAPK8/JNK1.

6CQ7
THE SH3 DOMAIN OF MLK3 IN COMPLEX WITH POLY-PROLINE PEPTIDE DERIVED FROM HTT
RCSB/PDB
Inspect Structure
See all 3D Structures for MAP3K11

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: MAP3K11 is active in the following subcellular-locations: centrosome, cytoplasm, cytoskeleton, microtubule organizing center.
GO terms: MAP3K11 is active in the following subcellular-locations: centrosome, cytoplasm, membrane, microtubule.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project MAP3K11 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: UACC_257, RXF_393, M14

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: COLO 853, SK23, Detroit 562

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, A549

(see details)

RNA Interference


MAP3K11 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: SKGT4, H1299. (see details)

3D Structures


For MAP3K11 there are:
4 structures (7 chains) solved
1 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


MAP3K11 has been screened with 257 compounds (352 bioactivities), 47 compounds have bioactivities that show binding affinity of <= 500nM (78 bioactivities). (see details)