Affiliation:
1. College of Pharmaceutical Science, Zhejiang University of Technology and Institute of Drug Development & Chemical Biology, Zhejiang University of Technology, Hangzhou 310014, China
2. School of Pharmaceutical Sciences, Gannan Medical University, Ganzhou 341000, China
Abstract
Abstract::
Poly (ADP-ribose) polymerase (PARP) acts as an essential DNA repair enzyme.
PARP inhibitors are novel small molecule targeted drugs based on the principle of "Synthetic
Lethality", which affect DNA repair process by competitively inhibiting the activity of PARP
enzyme and thereby kill cancer cells. Currently, four PARP inhibitors including olaparib, rucaparib,
niraparib, and talazoparib have been approved by FDA for cancer treatment and have
achieved great success in the treatment of ovarian cancer, breast cancer, and pancreatic cancer,
etc. This paper provides a general overview of the research progress of PARP inhibitors
including the major structure types, structure-activity relationship (SAR), and synthetic
routes, with the aim of providing ideas for the discovery and synthesis of novel PARP inhibitors.
Funder
Zhejiang Provincial Natural Science Foundation
Publisher
Bentham Science Publishers Ltd.
Subject
Pharmacology,Molecular Medicine,Drug Discovery,Biochemistry,Organic Chemistry
Cited by
8 articles.
订阅此论文施引文献
订阅此论文施引文献,注册后可以免费订阅5篇论文的施引文献,订阅后可以查看论文全部施引文献