Progress in the research of PARP inhibitors and their mechanisms of action
WANG Ying-ying
LIU Wen-jing
NING Yao
JI Min
CAI Jin
Abstract：Poly (ADP-ribose) polymerase (PARP) acts as essential DNA repair enzyme in the base excision repair pathway.PARP involves in many cellular processes including DNA damage response,maintaining the integrity of the genome and apoptosis regulation.PARP inhibitors inhibit PARP activity that selectively kills cancer cells by targeting homologous recombination repair defects.In recent years,the research on PARP inhibitors has become the hot target in cancer therapy.Olaparib,a PARP inhibitor,is the first drug that has been come to market so far,two drugs rucaparib and niraparib have been approved.In this paper,based on the structure and mechanism of PARP-1,the major structure types and recent progress of PARP-1 inhibitors were reviewed.This paper also introduced current clinical PARP inhibitors and looked forward to the development prospect of PARP inhibitors and the problems to be solved.
Keywords：PARP-1inhibitorsDNA repairantitumorresearch progress
Publication Date：2018-02-15
Online Publishing Date：2026-08-14(First online date of this platform, not the publication date of the document)
Pages：8( 306-313 )