Title:PARP1: A Promising Target for the Development of PARP1-based Candidates for Anticancer Intervention
VOLUME: 23 ISSUE: 17
Author(s):Xiaolei Zhu, Xiaodong Ma and Yongzhou Hu
Affiliation:ZJU-ENS Joint Laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
Keywords:Anticancer, clinical trial, PARP1 inhibitors, PARPs, structure-activity relationship (SAR).
Abstract:Poly(ADP-ribose) polymerase 1 (PARP1) inhibition, increasing chemosensitization
and conferring independent antiproliferation against defective homologous recombination
cells, has provided a unique opportunity for anticancer therapeutic intervention. Therefore,
PARP1, the best characterized enzyme among PARP family, is presently serving as a
well-established target for the treatment of oncology attributed to its intimate role in DNA
repair. Nowadays, intensified medicinal chemistry efforts have led to the discovery of 12
PARP1 inhibitors that have been advanced into clinical trial. In this article, we classify these candidates as
three categories based on the chemical structure, including lactam type, pseudo ring type and untypical
PARP1 inhibitors, for a sequential overview of them. In particular, the development of some candidates will
serve the purpose for the future exploration of PARP1 inhibitors.
