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

MAP3K12 (Q12852) - Overview - Molecular Target Synopsis

Protein


MAP3K12, Mitogen-activated protein kinase kinase kinase 12
Enzyme Classification 2.7.11.25
UniProt Q12852

Also Known as M3K12_HUMAN, MAP3K12, ZPK

Part of a non-canonical MAPK signaling pathway (PubMed:28111074). Activated by APOE, enhances the AP-1-mediated transcription of APP, via a MAP kinase signal transduction pathway composed of MAP2K7 and MAPK1/ERK2 and MAPK3/ERK1 (PubMed:28111074). May be an activator of the JNK/SAPK pathway. Homodimer (By similarity). Interacts with MBIP (PubMed:10801814).

5VO1
DLK IN COMPLEX WITH COMPOUND 10 (5-(1-ISOPROPYL-5-(3-(OXETAN-3-YL)-3- AZABICYCLO[3.1.0]HEXAN-6-YL)-1H-PYRAZOL-3-YL)-3-(TRIFLUOROMETHYL) PYRIDIN-2-AMINE)
RCSB/PDB
Inspect Structure
See all 3D Structures for MAP3K12

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: MAP3K12 is active in the following subcellular-locations: cell membrane, cytoplasm.
GO terms: MAP3K12 is active in the following subcellular-locations: cytoplasm, cytosol, growth cone, membrane, plasma membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project MAP3K12 has gain in 2 cell-lines, loss in 1 cell-lines and no signal in 1002 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: NCI_H522, HOP_92, MALME_3M

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: MDA-MB-134-VI, SK-N-FI, SNU-398

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, IMR-90, NHLF

(see details)

RNA Interference


MAP3K12 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: CAL120, LM7. (see details)

3D Structures


For MAP3K12 there are:
6 structures (6 chains) solved
5 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


MAP3K12 has been screened with 731 compounds (843 bioactivities), 595 compounds have bioactivities that show binding affinity of <= 500nM (691 bioactivities). (see details)