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

DYRK1B (Q9Y463) - Overview - Molecular Target Synopsis

Protein


DYRK1B, Dual specificity tyrosine-phosphorylation-regulated kinase 1B
Enzyme Classification 2.7.12.1
UniProt Q9Y463

Also Known as DYR1B_HUMAN, DYRK1B, MIRK

Dual-specificity kinase which possesses both serine/threonine and tyrosine kinase activities. Enhances the transcriptional activity of TCF1/HNF1A and FOXO1. Inhibits epithelial cell migration. Mediates colon carcinoma cell survival in mitogen-poor environments. Inhibits the SHH and WNT1 pathways, thereby enhancing adipogenesis. In addition, promotes expression of the gluconeogenic enzyme glucose-6-phosphatase (G6PC). Dimer. Interacts with DCOHM, MAP2K3/MKK3, RANBP9 and TCF1/HNF1A. Part of a complex consisting of RANBP9, RAN, DYRK1B and COPS5. Interacts with DCAF7.

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: DYRK1B is active in the following subcellular-locations: nucleus.
GO terms: DYRK1B is active in the following subcellular-locations: nucleus.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project DYRK1B has gain in 15 cell-lines, loss in 1 cell-lines and no signal in 989 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: OVCAR_3, MCF7, A549

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: NIH:OVCAR-3, DMS 53, PANC-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, HUVEC, A549

(see details)

RNA Interference


DYRK1B was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: OAW42, OE19. (see details)

3D Structures


At greater than 75% identity similarity to DYRK1B 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

DYRK1B 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


DYRK1B has been screened with 747 compounds (1217 bioactivities), 127 compounds have bioactivities that show binding affinity of <= 500nM (172 bioactivities). (see details)