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

TLK2 (Q86UE8) - Overview - Molecular Target Synopsis

Protein


TLK2, Serine/threonine-protein kinase tousled-like 2
Enzyme Classification 2.7.11.1
UniProt Q86UE8

Also Known as TLK2_HUMAN, TLK2

Serine/threonine-protein kinase involved in the process of chromatin assembly and probably also DNA replication, transcription, repair, and chromosome segregation. Phosphorylates the chromatin assembly factors ASF1A AND ASF1B. Phosphorylation of ASF1A prevents its proteasome-mediated degradation, thereby enhancing chromatin assembly. Negative regulator of amino acid starvation-induced autophagy. Monomer and heterodimer with TLK1. Interacts with ASF1A and ASF1B. Association with 14-3-3 proteins such as YWHAZ regulates subcellular location. May also interact with FEZ1/LZTS1 and FEZ2.

5O0Y
TLK2 KINASE DOMAIN FROM HUMAN
RCSB/PDB
Inspect Structure
See all 3D Structures for TLK2

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: TLK2 is active in the following subcellular-locations: cytoplasm, cytoskeleton, nucleus, perinuclear region.
GO terms: TLK2 is active in the following subcellular-locations: intermediate filament, nucleus, perinuclear region of cytoplasm.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project TLK2 has gain in 8 cell-lines, loss in 0 cell-lines and no signal in 997 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: NCI_H522, CAKI_1, SR

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: HUP-T3, Hs 746T, HCC2911

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, SK-N-SH, NHLF

(see details)

RNA Interference


TLK2 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: COV362, DU4475. (see details)

3D Structures


For TLK2 there are:
1 structures (1 chains) solved
1 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


TLK2 has been screened with 297 compounds (503 bioactivities), 5 compounds have bioactivities that show binding affinity of <= 500nM (10 bioactivities). (see details)