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

MKNK2 (Q9HBH9) - Overview - Molecular Target Synopsis

Protein


MKNK2, MAP kinase-interacting serine/threonine-protein kinase 2
Enzyme Classification 2.7.11.1
UniProt Q9HBH9

Also Known as MKNK2_HUMAN, MKNK2, GPRK7, MNK2

Serine/threonine-protein kinase that phosphorylates SFPQ/PSF, HNRNPA1 and EIF4E. May play a role in the response to environmental stress and cytokines. Appears to regulate translation by phosphorylating EIF4E, thus increasing the affinity of this protein for the 7-methylguanosine-containing mRNA cap. Required for mediating PP2A-inhibition-induced EIF4E phosphorylation. Triggers EIF4E shuttling from cytoplasm to nucleus. Isoform 1 displays a high basal kinase activity, but isoform 2 exhibits a very low kinase activity. Acts as a mediator of the suppressive effects of IFNgamma on hematopoiesis. Negative regulator for signals that control generation of arsenic trioxide As(2)O(3)-dependent apoptosis and anti-leukemic responses. Involved in anti-apoptotic signaling in response to serum withdrawal. Monomer. Interacts with the C-terminal regions of EIF4G1 and EIF4G2; this interaction is promoted when MAPK pathways are repressed but repressed upon ERK proteins activation. Also binds to dephosphorylated MAPK3/ERK1 and MAPK1/ERK2. Isoform 1 interaction with phosphorylated MAPK3/ERK1 and MAPK1/ERK2 protects it from dephosphorylation and inactivation. Isoform 2 interacts with ESR2 and EIF4E in the nucleus.

6CJH
CO-CRYSTAL STRUCTURE OF MNK2 IN COMPLEX WITH AN INHIBITOR
RCSB/PDB
Inspect Structure
See all 3D Structures for MKNK2

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: MKNK2 is active in the following subcellular-locations: cytoplasm, nucleus, pml body.
GO terms: MKNK2 is active in the following subcellular-locations: cytoplasm, nuclear body, nucleoplasm, nucleus, PML body.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project MKNK2 has gain in 0 cell-lines, loss in 5 cell-lines and no signal in 1000 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: IGROV1, OVCAR_3, SR

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: COR-L26, CCRF-SB, RC-K8

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, HMEC, K562

(see details)

RNA Interference


MKNK2 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: SCC90, KPD. (see details)

3D Structures


For MKNK2 there are:
11 structures (11 chains) solved
9 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


MKNK2 has been screened with 1369 compounds (2049 bioactivities), 500 compounds have bioactivities that show binding affinity of <= 500nM (528 bioactivities). (see details)