- References (2)
- Inventor Info
|Antigen/Gene or Protein Targets||Poly(ADP-ribose) glycohydrolase (PARG)|
Poly(ADP ribose) glycohydrolase (PARG) has been shown to be a critical component in the repair of single strand DNA breaks. PARG counteracts the function of the ARTD family of poly(ADP ribose) polymerases, commonly known as PARPS, by efficiently catalysing the hydrolysis of O-glycosidic linkages of ADP-ribose polymer, thereby reversing the effects of PARPs. As PARG exists as a single protein, it presents an attractive target for therapeutic intervention in cancer cells with enhanced dependence upon DNA repair.
Methylation of the sulphonamide moiety of the PARG Inhibitor PDD00017273 was found to disrupt PARG-binding interactions, rendering the compound inactive and providing useful controls to demonstrate on-target pharmacology of the active compound.
|On Target IC50||>100µM (PARG)|
|Molecular Weight (g/mol)||528.16|
|Research Area||Cancer, Epigenetics & Nuclear Signalling|
|Notes||N-methylated analogs of the PARG tool compounds are inactive.|
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