Abstract 5119: P015, a highly selective PARP7&12 dual inhibitor

Key Points

• To develop and characterize a selective small-molecule inhibitor targeting PARP7 and PARP12.
• Designed small-molecule inhibitors based on structure-activity relationship studies.
• Utilized AIDRUG.WORK molecular design platform for optimization.
• Conducted in vitro enzymatic assays to measure inhibitory activity of P015 against PARP7 and PARP12.
• Calculated IC50 values from concentration-response curves.
• P015 demonstrated potent inhibitory activity against PARP7 and PARP12 with IC50 values below 10 nM.
• The findings indicate strong affinity and inhibitory potency at the enzymatic level for both enzymes.
• P015 holds promise for further investigation as a novel anti-cancer agent targeting the PARP7 and PARP12 pathway.