PARP7: an Emerging Therapeutic Target-Insights into Biological Functions and Advances in Small-Molecule Inhibitor Development

Abstract

PARP7 is a critically important member of the PARP family. Current research indicates that PARP7 is associated with various diseases, including viral infections, cancers, and stroke. Consequently, pharmacological modulation of PARP7 enzymatic activity has emerged as a crucial strategy for treating numerous diseases. Notably, the selective PARP7 inhibitor RBN-2397 for tumor treatment has entered Phase II trials, highlighting the translational potential of targeting this enzyme. This perspective summarizes the biological functions of PARP7 and its roles in various diseases. Furthermore, to advance the study of PARP7 inhibitors, we analyze the mechanisms of action and design strategies of existing PARP7 inhibitors as reported in current papers and patents. Additionally, we share our experiences in designing PARP7 inhibitors and present our insights regarding the opportunities and challenges in this pioneering research field.