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

MAP2K5 (Q13163) - Overview - Molecular Target Synopsis

Protein


MAP2K5, Dual specificity mitogen-activated protein kinase kinase 5
Enzyme Classification 2.7.12.2
UniProt Q13163

Also Known as MP2K5_HUMAN, MAP2K5, MEK5, MKK5, PRKMK5

Acts as a scaffold for the formation of a ternary MAP3K2/MAP3K3-MAP3K5-MAPK7 signaling complex. Activation of this pathway appears to play a critical role in protecting cells from stress-induced apoptosis, neuronal survival and cardiac development and angiogenesis. Interacts with PARD6A, MAP3K3 and MAPK7. Forms a complex with SQSTM1 and PRKCZ or PRKCI (By similarity). Interacts with Yersinia yopJ.

4IC7
CRYSTAL STRUCTURE OF THE ERK5 KINASE DOMAIN IN COMPLEX WITH AN MKK5 BINDING FRAGMENT
RCSB/PDB
Inspect Structure
See all 3D Structures for MAP2K5

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


GO terms: MAP2K5 is active in the following subcellular-locations: cytoplasm, cytosol, nucleus, spindle.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project MAP2K5 has gain in 1 cell-lines, loss in 1 cell-lines and no signal in 1003 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: NCI_H226, HL_60, MCF7

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: WSU-FSCCL, A-673, H322T

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: GM12878, NHLF, SK-N-SH

(see details)

RNA Interference


MAP2K5 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: MCF12A, HCH1. (see details)

3D Structures


For MAP2K5 there are:
3 structures (5 chains) solved
0 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


MAP2K5 has been screened with 121 compounds (148 bioactivities), 32 compounds have bioactivities that show binding affinity of <= 500nM (32 bioactivities). (see details)