PARG inhibitor PDD00031704 Inactive Small Molecule (Tool Compound)
- Name Allan Jordan ; Kate Smith
- Institute Cancer Research Technology Ltd
Tool name: PARG inhibitor PDD00031704 Inactive Small Molecule (Tool Compound)
Alternate names: Poly(ADP-ribose) glycohydrolase
Molecular formula: C24H28N6O4S2
Tool type: Small molecules
Tool sub-type: Inhibitor
Description: 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.
Research area: Cancer ; Fluorescent Cell Imaging
- For Research Use Only