Target intelligence / Profile preview

Serine/threonine-protein kinase ATR (ATR)

Target
ATR
Molecular classification
Enzyme, Protein Kinase, Serine/threonine-protein kinase, PIKK family
01

Overview

Serine/threonine-protein kinase ATR is a member of the PIKK family and plays a crucial role in the DNA damage response. It acts as a sensor of DNA damage, particularly single-stranded DNA, and activates cell cycle checkpoints by phosphorylating key downstream targets like CHK1, RAD17/RAD9 complex members, and BRCA1. ATR forms a complex with ATRIP, which is essential for its recruitment and activation at sites of DNA damage. ATR is involved in responses to various forms of genotoxic stress, including ionizing radiation, UV radiation, and stalled replication forks. ATR inhibitors are under development as cancer therapeutics.

Other names
Ataxia telangiectasia and Rad3-related proteinFRAP-related protein 1 (FRP1)Ataxia telangiectasia Rad3 relatedFRP1
02

Mechanism of action

ATR kinase inhibitors prevent DNA damage repair and cell cycle arrest in cancer cells.

03

Biological functions

DNA damage responseCell cycle checkpoint controlGenome stabilityDNA repair
04

Disease associations

CancerInfectious Diseases
05

Safety considerations

Increased sensitivity to UV/ionizing radiationLoss of checkpoint controlPremature aging phenotypes (in mice models)

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