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

TLK1 (Q9UKI8) - Overview - Molecular Target Synopsis

Protein


TLK1, Serine/threonine-protein kinase tousled-like 1
Enzyme Classification 2.7.11.1
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.



UniProt
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)