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

CLK2 (P49760) - Overview - Molecular Target Synopsis

Protein


CLK2, Dual specificity protein kinase CLK2
Enzyme Classification 2.7.12.1
UniProt P49760

Also Known as CLK2_HUMAN, CLK2

Dual specificity kinase acting on both serine/threonine and tyrosine-containing substrates. Phosphorylates serine- and arginine-rich (SR) proteins of the spliceosomal complex. May be a constituent of a network of regulatory mechanisms that enable SR proteins to control RNA splicing and can cause redistribution of SR proteins from speckles to a diffuse nucleoplasmic distribution. Acts as a suppressor of hepatic gluconeogenesis and glucose output by repressing PPARGC1A transcriptional activity on gluconeogenic genes via its phosphorylation. Phosphorylates PPP2R5B thereby stimulating the assembly of PP2A phosphatase with the PPP2R5B-AKT1 complex leading to dephosphorylation of AKT1. Phosphorylates: PTPN1, SRSF1 and SRSF3. Regulates the alternative splicing of tissue factor (F3) pre-mRNA in endothelial cells. Interacts with RBMX. Interacts with AKT1 and UBL5.

6FYI
X-RAY STRUCTURE OF CLK2-KD(130-496)/TG003 AT 2.6A
RCSB/PDB
Inspect Structure
See all 3D Structures for CLK2

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: CLK2 is active in the following subcellular-locations: nucleus, nucleus speckle.
GO terms: CLK2 is active in the following subcellular-locations: nuclear body, nuclear speck, nucleoplasm, nucleus.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project CLK2 has gain in 0 cell-lines, loss in 0 cell-lines and no signal in 0 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SR, CCRF_CEM, ACHN

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: NCI-H1882, G112, NCI-H187

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, K562, HUVEC

(see details)

RNA Interference


CLK2 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: HCC1954, H2342. (see details)

3D Structures


For CLK2 there are:
5 structures (10 chains) solved
5 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


CLK2 has been screened with 874 compounds (1562 bioactivities), 52 compounds have bioactivities that show binding affinity of <= 500nM (62 bioactivities). (see details)