PARP16 is a momo-ADP ribotransferase belonging to the members of the poly(ADP-ribose) poiyerases (PARPs) family, unlike other family members, it is an anchored transmembrane protein located in the endoplasmic reticulum. During the unfolding protein reaction of the endoplasmic reticulum, the two pressure sensors PERK and IRE1α of the endoplasmic reticulum will be activated, and PARP16 plays an important role in this process.Through their single ADP-ribosylation and activating biological activity, PARP16 can regulate cancer, cardiovascular diseases and cystic fibrosis, which make it become a great potential drug target for major human diseases such as cancer and cardiovascular disease. This article mainly describes the structures and function of PARP16, related diseases mediated, and small molecule inhibitors.