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

DSTYK (Q6XUX3) - Overview - Molecular Target Synopsis

Protein


DSTYK, Dual serine/threonine and tyrosine protein kinase
Enzyme Classification 2.7.12.1
UniProt Q6XUX3

Also Known as DUSTY_HUMAN, DSTYK, KIAA0472, RIP5, RIPK5, SGK496

Acts as a positive regulator of ERK phosphorylation downstream of fibroblast growth factor-receptor activation (PubMed:23862974, PubMed:28157540). Involved in the regulation of both caspase-dependent apoptosis and caspase-independent cell death (PubMed:15178406). In the skin, it plays a predominant role in suppressing caspase-dependent apoptosis in response to UV stress in a range of dermal cell types (PubMed:28157540).

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: DSTYK is active in the following subcellular-locations: apical cell membrane, basolateral cell membrane, cell junction, cell membrane, cytoplasm.
GO terms: DSTYK is active in the following subcellular-locations: apical plasma membrane, basolateral plasma membrane, cell junction, cytoplasm.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project DSTYK has gain in 2 cell-lines, loss in 0 cell-lines and no signal in 1003 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SK_MEL_5, M14, SK_MEL_28

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: SK-MEL-1, C32, COLO-783

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: NHLF, BJ, AG445

(see details)

RNA Interference


DSTYK was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: MDAMB453, SKBR3. (see details)

3D Structures


At greater than 35% identity similarity to DSTYK there are:
5 structures (9 chains) solved
5 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


DSTYK has been screened with 81 compounds (81 bioactivities), 6 compounds have bioactivities that show binding affinity of <= 500nM (6 bioactivities). (see details)