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C169969Level 5

Etidaligide

**Semantic type:** Pharmacologic Substance

**Definition:** A preparation of cell-permeant, short double-stranded DNA fragment that mimics double-strand breaks (DSBs) and linked to a cholesterol molecule, with potential antineoplastic activity. Upon administration of etidaligide, the cholesterol moiety enables tumoral and nuclear uptake of the DNA fragment, which mimics DNA DSBs. Inside the tumor cells, the DNA fragment triggers false DNA break signals, and binds to and activates DNA repair proteins including both poly (ADP-ribose) polymerase (PARP) and DNA-dependent protein kinase (DNA-PK). This prevents the recruitment of these repair proteins at the actual damage site and inhibits various DNA DSB repair pathways including homologous recombination (HR) and non-homologous end joining (NHEJ). This promotes genetic instability and enhances the accumulation of single and double strand DNA breaks, ultimately leading to apoptosis.

**Synonyms:** - AsiDNA - DNA Repair Inhibiting Oligonucleotide - DNA Repair Inhibiting Oligonucleotide AsiDNA - DSBs Mimic - ETIDALIGIDE - Oligonucleotide-mimicking Double-stranded DNA Breaks

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