Affiliation:
1. Department of Pharmaceutical Sciences and Natural Products, Central University of Punjab, Ghudda,
Bathinda 151401, India
2. Department of Pharmaceutical Sciences and Technology, Maharaja Ranjit Sigh Punjab Technical University, Bathinda
151001, India
Abstract
Background:
Cancer is the world's second largest cause of death and is responsible for an estimated 9.6 million mortalities in 2018. Poly-ADP-ribose polymerases (PARPs) are enzymes and family of proteins, involved in many cellular processes, including DNA repair, gene regulation, chromatin remodeling, and apoptosis. The first characterized and best known member of the PARP family is poly(ADP-ribose) polymerase 1 (PARP-1). PARP-1 is a major protein for DNA single-strand breaks in the BER pathway (base excision repair) (SSBs).
Objective:
The objective of this article was to compile synthetic PARP-1 inhibitors reported in the last decade
Methods:
In the present manuscript, bibliographic investigation was carried out by scrutinizing peerreviewed
articles from online/offline databases. The inclusion criteria consisted of the most relevant studies
indicating the relationship between PARP-1 and cancer in textbooks/edited books and peer-reviewed
papers from scientific databases, like SCOPUS, PUBMED, NISCAIR, and Google Scholar since 2010 to
2020. Only the studies published in English language were searched/considered. The exclusion criteria
consisted of the studies on other PARP isoforms than PARP-1. The studies thus obtained were classified
according to the heterocyclic moieties, year of publication, etc. The data compiled in this article is a systematic
review of the reported studies.
Results:
The literature reports indicated that a number of PARP-1 inhibitors reported have IC50 value in nanomolar concentration.
Conclusion:
PARP-1 is an essential target for anti-cancer drug discovery. Further, research for more effective and safe PARP-1 inhibitors is carried out and we may discover some novel PARP-1 inhibitors in the near future.
Publisher
Bentham Science Publishers Ltd.
Subject
Drug Discovery,Pharmaceutical Science,Molecular Medicine