142
Novel Inhibitors of PARP1/2
University of Colorado
Small molecule
Oncology
Hit To Lead or Lead Optimization
• The inventors developed a series of novel PARPi compounds which interact with PARP1/2 and HPF1 to form ternary PARP-HPF1 inhibitor complexes.
• These novel PARPi compounds are configured to interact with HPF1 form more stable and effective inhibitors.
• The novel PARPi can inhibit PARP activity, HPF1 activity, and the activity of the PARP-HPF1 complex. The novel PARPi can be therapeutically administered to treat cancers deficient in homologous dependent DNA double strand break repair pathways, vascular disease, as well as cerebral and cardiovascular neurotoxicity.
Inhibitors of PARP: Number crunching and structure gazing, PNAS (2022)
