Molecular Target Synopsis
Domains and Structures
Drugs and Clinical Candidates
Ligand Efficiency Plot
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
Germline Genetics

TLK1 (Q9UKI8) - Overview - Molecular Target Synopsis


TLK1, Serine/threonine-protein kinase tousled-like 1
Enzyme Classification
UniProt Q9UKI8

Also Known as TLK1_HUMAN, TLK1, KIAA0137

Rapidly and transiently inhibited by phosphorylation following the generation of DNA double-stranded breaks during S-phase. This is cell cycle checkpoint and ATM-pathway dependent and appears to regulate processes involved in chromatin assembly. Isoform 3 phosphorylates and enhances the stability of the t-SNARE SNAP23, augmenting its assembly with syntaxin. Isoform 3 protects the cells from the ionizing radiation by facilitating the repair of DSBs. In vitro, phosphorylates histone H3 at 'Ser-10'. Heterodimerizes with TLK2. Interacts with ASF1A and ASF1B.

Isoforms / Transcripts (Protein Coding)

Sub-cellular localization

UniProt: TLK1 is active in the following subcellular-locations: nucleus.
GO terms: TLK1 is active in the following subcellular-locations: nucleus.

GO terms

Gene Copy Number Variation

In COSMIC - Cell Lines Project TLK1 has gain in 2 cell-lines, loss in 2 cell-lines and no signal in 1001 cell-lines. (see details)

Gene Expression

In NCI60, the highest expressing cell lines are: MOLT_4, CCRF_CEM, NCI_H460

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: BICR 10, MKN-74, SK-MES-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: NHLF, MCF-7, AG445

(see details)

RNA Interference

TLK1 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: LM7, H727. (see details)

3D Structures

At greater than 75% identity similarity to TLK1 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

TLK1 has been screened with 143 compounds (186 bioactivities), 3 compounds have bioactivities that show binding affinity of <= 500nM (5 bioactivities). (see details)