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

HIPK4 (Q8NE63) - Overview - Molecular Target Synopsis

Protein


HIPK4, Homeodomain-interacting protein kinase 4
Enzyme Classification 2.7.11.1
UniProt Q8NE63

Also Known as HIPK4_HUMAN, HIPK4

Protein kinase that phosphorylates human TP53 at Ser-9, and thus induces TP53 repression of BIRC5 promoter (By similarity). May act as a corepressor of transcription factors .

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
616ENSG00000160396ENST00000291823ENSP00000291823Q8NE63-1

Sub-cellular localization


UniProt: HIPK4 is active in the following subcellular-locations: cytoplasm.
GO terms: HIPK4 is active in the following subcellular-locations: cytoplasm, nucleus.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project HIPK4 has gain in 12 cell-lines, loss in 0 cell-lines and no signal in 992 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are:

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Hs 746T, NCI-H209, HCC12

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, NHLF, HSMM

(see details)

RNA Interference


HIPK4 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: TE10, NY. (see details)

3D Structures


At greater than 35% identity similarity to HIPK4 there are:
30 structures (106 chains) solved
30 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

HIPK4 is solved in complex with the approved drug(s):

2K2/MIDOSTAURIN (4NCT_A, 4NCT_B, 4NCT_C, 4NCT_D).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


HIPK4 has been screened with 484 compounds (866 bioactivities), 16 compounds have bioactivities that show binding affinity of <= 500nM (20 bioactivities). (see details)