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

MAP4K4 (O95819) - Overview - Molecular Target Synopsis

Protein


MAP4K4, Mitogen-activated protein kinase kinase kinase kinase 4
Enzyme Classification 2.7.11.1
UniProt O95819

Also Known as M4K4_HUMAN, MAP4K4, HGK, KIAA0687, NIK

Serine/threonine kinase that may play a role in the response to environmental stress and cytokines such as TNF-alpha. Appears to act upstream of the JUN N-terminal pathway. Phosphorylates SMAD1 on Thr-322. Interacts with the SH3 domain of the adapter proteins Nck (By similarity). Interacts (via its CNH regulatory domain) with ATL1 (via the N-terminal region). Interacts with RAP2A (GTP-bound form preferentially).

5W5Q
MAP4K4 IN COMPLEX WITH INHIBITOR COMPOUND 12 (N3-METHYL-10-(3-METHYL- 3-(5-METHYLOXAZOL-2-YL)BUT-1-YN-1-YL)-6,7-DIHYDRO-5H-5,7- METHANOBENZO[C]IMIDAZO[1,2-A]AZEPINE-2,3-DICARBOXAMIDE)
RCSB/PDB
Inspect Structure
See all 3D Structures for MAP4K4

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: MAP4K4 is active in the following subcellular-locations: cytoplasm.
GO terms: MAP4K4 is active in the following subcellular-locations: cytoplasm, focal adhesion.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project MAP4K4 has gain in 1 cell-lines, loss in 0 cell-lines and no signal in 1004 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: LOXIMVI, NCI_H522, RXF_393

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Hep G2, HEY, TYK-nu

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: HSMM, NHLF, HMEC

(see details)

RNA Interference


MAP4K4 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: SKGT4, HCH1. (see details)

3D Structures


For MAP4K4 there are:
17 structures (34 chains) solved
16 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


MAP4K4 has been screened with 765 compounds (1238 bioactivities), 70 compounds have bioactivities that show binding affinity of <= 500nM (82 bioactivities). (see details)