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

MAP2K2 (P36507) - Overview - Molecular Target Synopsis

Protein


MAP2K2, Dual specificity mitogen-activated protein kinase kinase 2
Enzyme Classification 2.7.12.2
UniProt P36507

Also Known as MP2K2_HUMAN, MAP2K2, MEK2, MKK2, PRKMK2

Catalyzes the concomitant phosphorylation of a threonine and a tyrosine residue in a Thr-Glu-Tyr sequence located in MAP kinases. Activates the ERK1 and ERK2 MAP kinases. Interacts with MORG1 (By similarity). Interacts with SGK1 (PubMed:19447520). Interacts with KSR1 (PubMed:10409742).

4H3Q
12 RESIDUE FRAGMENT OF
DUAL SPECIFICITY MITOGEN-ACTIVATED PROTEIN KINASE KINASE 2
IN THE STRUCTURE OF
CRYSTAL STRUCTURE OF HUMAN ERK2 COMPLEXED WITH A MAPK DOCKING PEPTIDE
RCSB/PDB
Inspect Structure
See all 3D Structures for MAP2K2

Isoforms / Transcripts (Protein Coding)


Drugs


MAP2K2 is targeted by Approved Drugs Trametinib, Cobimetinib. (see details)
Trametinib
Cobimetinib

Sub-cellular localization


Gene Copy Number Variation


In COSMIC - Cell Lines Project MAP2K2 has gain in 0 cell-lines, loss in 2 cell-lines and no signal in 1002 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SK_MEL_5, HS578T, SK_OV_3

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: SUM 1315M02, SK23, SK-MEL-24

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, HMEC

(see details)

RNA Interference


MAP2K2 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: H2228, NY. (see details)

3D Structures


For MAP2K2 there are:
3 structures (4 chains) solved
1 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


MAP2K2 has been screened with 433 compounds (574 bioactivities), 37 compounds have bioactivities that show binding affinity of <= 500nM (59 bioactivities). (see details)