The poly(ADP-ribose) polymerases (PARPs) form a family of enzymes with roles in DNA repair and apoptosis. BGP-15 is a PARP inhibitor and insulin sensitizer. In perfused heart, it blocks self-ADP-ribosylation of nuclear PARP (Ki = 57 μM) and mono-ADP-ribosylation of GRP78, resulting in decreased levels of reactive oxygen species, lipid peroxidation, and single-strand DNA breaks. BGP-15 acts as a co-inducer of heat shock protein 72, augmenting expression induced by heat shock factor 1 in adipocytes and skeletal muscles and improving insulin sensitivity.
