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

VRK1 (Q99986) - Overview - Molecular Target Synopsis

Protein


VRK1, Serine/threonine-protein kinase VRK1
Enzyme Classification 2.7.11.1
UniProt Q99986

Also Known as VRK1_HUMAN, VRK1

Serine/threonine kinase involved in Golgi disassembly during the cell cycle: following phosphorylation by PLK3 during mitosis, required to induce Golgi fragmentation. Acts by mediating phosphorylation of downstream target protein. Phosphorylates 'Thr-18' of p53/TP53 and may thereby prevent the interaction between p53/TP53 and MDM2. Phosphorylates casein and histone H3. Phosphorylates BANF1: disrupts its ability to bind DNA, reduces its binding to LEM domain-containing proteins and causes its relocalization from the nucleus to the cytoplasm. Phosphorylates ATF2 which activates its transcriptional activity.

6NPN
CRYSTAL STRUCTURE OF THE HUMAN VACCINIA-RELATED KINASE BOUND TO A N,N- DIPROPYNYL-DIHYDROPTERIDINE-3-HYDROXYINDAZOLE INHIBITOR
RCSB/PDB
Inspect Structure
See all 3D Structures for VRK1

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: VRK1 is active in the following subcellular-locations: cytoplasm, cytoskeleton, nucleus, spindle.
GO terms: VRK1 is active in the following subcellular-locations: cytoplasm, cytosol, Golgi stack, nucleolus, nucleoplasm, nucleus, spindle.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project VRK1 has gain in 7 cell-lines, loss in 4 cell-lines and no signal in 994 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: CCRF_CEM, HL_60, MOLT_4

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: TK, FaDu, KARPAS-422

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: MCF-7, HMEC, NHLF

(see details)

RNA Interference


VRK1 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: H1650, OE19. (see details)

3D Structures


For VRK1 there are:
19 structures (64 chains) solved
15 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


VRK1 has been screened with 162 compounds (169 bioactivities). (see details)