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

Dyrk1a (Q63470) - Overview - Molecular Target Synopsis

Protein


Dyrk1a, Dual specificity tyrosine-phosphorylation-regulated kinase 1A
Enzyme Classification 2.7.12.2
UniProt Q63470

Also Known as DYR1A_RAT, Dyrk1a, Dyrk

Dual-specificity kinase which possesses both serine/threonine and tyrosine kinase activities. May play a role in a signaling pathway regulating nuclear functions of cell proliferation. Modulates alternative splicing by phosphorylating the splice factor SRSF6 (By similarity). Exhibits a substrate preference for proline at position P+1 and arginine at position P-3. Has pro-survival function and negatively regulates the apoptotic process. Promotes cell survival upon genotoxic stress through phosphorylation of SIRT1. This in turn inhibits TP53 activity and apoptosis. Interacts with RANBP9. Interacts with RAD54L2/ARIP4. Interacts with CRY2 (By similarity). Interacts with WDR68 (By similarity). Interacts with SRSF6 (PubMed:22767602). Interacts with SIRT1.

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
763Q63470-1
754Q63470-2

Sub-cellular localization


UniProt: Dyrk1a is active in the following subcellular-locations: nucleus speckle.
GO terms: Dyrk1a is active in the following subcellular-locations: axon, cytoplasm, cytoskeleton, dendrite, nuclear speck, nucleus, ribonucleoprotein complex.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project Dyrk1a has gain in 0 cell-lines, loss in 0 cell-lines and no signal in 0 cell-lines. (see details)

RNA Interference


Dyrk1a was reported in the following RNAI studies:

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


Screening and Chemistry


Dyrk1a has been screened with 494 compounds (520 bioactivities), 87 compounds have bioactivities that show binding affinity of <= 500nM (101 bioactivities). (see details)