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

MDM4 (O15151) - Overview - Molecular Target Synopsis

Protein


MDM4, Protein Mdm4
UniProt O15151

Also Known as MDM4_HUMAN, MDM4, MDMX

Inhibits p53/TP53- and TP73/p73-mediated cell cycle arrest and apoptosis by binding its transcriptional activation domain. Inhibits degradation of MDM2. Can reverse MDM2-targeted degradation of TP53 while maintaining suppression of TP53 transactivation and apoptotic functions. Interacts with MDM2, TP53, TP73 and USP2. Found in a trimeric complex with USP2, MDM2 and MDM4. Interacts (phosphorylated) with YWHAG; negatively regulates MDM4 activity toward TP53.

5VK1
CRYSTAL STRUCTURE OF HUMAN MDM4 IN COMPLEX WITH A 12-MER LYSINE- CYSTEINE SIDE CHAIN DITHIOCARBAMATE STAPLED PEPTIDE INHIBITOR PMI
RCSB/PDB
Inspect Structure
See all 3D Structures for MDM4

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: MDM4 is active in the following subcellular-locations: nucleus.
GO terms: MDM4 is active in the following subcellular-locations: nucleoplasm, nucleus.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project MDM4 has gain in 4 cell-lines, loss in 0 cell-lines and no signal in 1001 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: MCF7, SK_MEL_5, CCRF_CEM

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: WSU-FSCCL, MHH-ES-1, MHH-PREB-1

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, K562, MCF-7

(see details)

3D Structures


For MDM4 there are:
24 structures (49 chains) solved
6 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


MDM4 has been screened with 409 compounds (463 bioactivities), 38 compounds have bioactivities that show binding affinity of <= 500nM (40 bioactivities). (see details)