Target intelligence / Profile preview

DNA Repair Process Inhibition (DDRi)

Target
DDRi
Molecular classification
Enzyme, Kinase, Polymerase, Ligase, Glycosylase
01

Overview

DNA repair process inhibition refers to the targeted disruption of cellular mechanisms responsible for detecting and repairing DNA damage. These processes are essential for maintaining genomic stability, and their inhibition is a key strategy in cancer therapy, as many tumors rely on specific DNA repair pathways to survive the high levels of genomic stress they experience. Inhibition involves targeting critical components within various DDR pathways using small molecule drugs—either alone or synergistically with traditional cytotoxic therapies—to maximize tumor cell death while minimizing harm to normal tissues.

Other names
DNA Damage Response InhibitionDDR Inhibition
02

Mechanism of action

Small molecule inhibitors block key proteins involved in DNA repair pathways, preventing the repair of DNA damage and leading to cell death. Inhibition can target specific enzymes such as PARP, DNA-PK, CHK1/CHK2, or Pol beta, disrupting processes like single-strand break repair, NHEJ, cell cycle checkpoints, or BER respectively.

03

Biological functions

Cell cycleApoptosisCell deathDNA repairGenomic stability
04

Disease associations

CancerDrug resistance
05

Safety considerations

MyelosuppressionResistance development via upregulation of alternative repair pathwaysOff-target effectsSecondary malignancies
06

Interacting drugs

Olaparib

4 more in the full profile.

07

Biomarkers

BRCA1/2 mutationsHRD (Homologous Recombination Deficiency)ATM mutationsATR mutationsPD-L1 expression

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