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

MAPK7 (Q13164) - Overview - Molecular Target Synopsis

Protein


MAPK7, Mitogen-activated protein kinase 7
Enzyme Classification 2.7.11.24
UniProt Q13164

Also Known as MK07_HUMAN, MAPK7, BMK1, ERK5, PRKM7

Plays a role in various cellular processes such as proliferation, differentiation and cell survival. The upstream activator of MAPK7 is the MAPK kinase MAP2K5. Upon activation, it translocates to the nucleus and phosphorylates various downstream targets including MEF2C. EGF activates MAPK7 through a Ras-independent and MAP2K5-dependent pathway. May have a role in muscle cell differentiation. May be important for endothelial function and maintenance of blood vessel integrity. MAP2K5 and MAPK7 interact specifically with one another and not with MEK1/ERK1 or MEK2/ERK2 pathways. Phosphorylates SGK1 at Ser-78 and this is required for growth factor-induced cell cycle progression. Involved in the regulation of p53/TP53 by disrupting the PML-MDM2 interaction. Interacts with MAP2K5. Forms oligomers (By similarity). Interacts with MEF2A, MEF2C and MEF2D; the interaction phosphorylates the MEF2s and enhances transcriptional activity of MEF2A, MEF2C but not MEF2D (By similarity). Interacts with SGK1. Preferentially interacts with PML isoform PML-4 but shows interaction also with its other isoforms: isoform PML-1, isoform PML-2, isoform PML-3 and isoform PML-6. Interacts (via N-terminal half) with HSP90AB1-CDC37 chaperone complex in resting cells; the interaction is MAP2K5-independent and prevents MAPK7 from ubiquitination and proteasomal degradation (PubMed:23428871).

6HKM
CRYSTAL STRUCTURE OF COMPOUND 1 WITH ERK5
RCSB/PDB
Inspect Structure
See all 3D Structures for MAPK7

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: MAPK7 is active in the following subcellular-locations: cytoplasm, nucleus, pml body.
GO terms: MAPK7 is active in the following subcellular-locations: cytoplasm, cytosol, nucleoplasm, nucleus, PML body.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project MAPK7 has gain in 9 cell-lines, loss in 9 cell-lines and no signal in 987 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SN12C, HS578T, U251

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: SNU-449, SNU-182, NCI-H1155

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, A549, IMR-90

(see details)

RNA Interference


MAPK7 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: TE10, MDAMB231. (see details)

3D Structures


For MAPK7 there are:
12 structures (14 chains) solved
10 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


MAPK7 has been screened with 139 compounds (206 bioactivities), 24 compounds have bioactivities that show binding affinity of <= 500nM (28 bioactivities). (see details)