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

MAP3K9 (P80192) - Overview - Molecular Target Synopsis

Protein


MAP3K9, Mitogen-activated protein kinase kinase kinase 9
Enzyme Classification 2.7.11.25
UniProt P80192

Also Known as M3K9_HUMAN, MAP3K9, MLK1, PRKE1

Serine/threonine kinase which acts as an essential component of the MAP kinase signal transduction pathway. Plays an important role in the cascades of cellular responses evoked by changes in the environment. Once activated, acts as an upstream activator of the MKK/JNK signal transduction cascade through the phosphorylation of MAP2K4/MKK4 and MAP2K7/MKK7 which in turn activate the JNKs. The MKK/JNK signaling pathway regulates stress response via activator protein-1 (JUN) and GATA4 transcription factors. Plays also a role in mitochondrial death signaling pathway, including the release cytochrome c, leading to apoptosis. Homodimer.

4UY9
STRUCTURE OF MLK1 KINASE DOMAIN WITH LEUCINE ZIPPER 1
RCSB/PDB
Inspect Structure
See all 3D Structures for MAP3K9

Isoforms / Transcripts (Protein Coding)


Gene Copy Number Variation


In COSMIC - Cell Lines Project MAP3K9 has gain in 5 cell-lines, loss in 0 cell-lines and no signal in 1000 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: NCI_H322M, RXF_393, T47D

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: HCC2935, NCI-H2347, NCI-H441

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: HMEC, MCF-7, NHLF

(see details)

RNA Interference


MAP3K9 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: SUM44, PL5. (see details)

3D Structures


For MAP3K9 there are:
2 structures (3 chains) solved
1 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


MAP3K9 has been screened with 442 compounds (706 bioactivities), 48 compounds have bioactivities that show binding affinity of <= 500nM (80 bioactivities). (see details)