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2000
Volume 21, Issue 8
  • ISSN: 1573-4072
  • E-ISSN: 1875-6646

Abstract

Cancer is a highly fatal disease that is typified by aberrant cells proliferating out of control. The properties of acquired cells, including as genomic instability and mutations, cellular death evasion, and proliferative signaling sustenance, are evidenced by the hallmarks of cancer and contribute to the establishment of malignant tumors. A protein called poly(ADP-ribose) polymerase-1 (PARP1) is essential for both cell survival and DNA damage repair, two processes that affect cellular control. Since homologous recombination deficient cells exhibit cellular death upon suppression of PARP1, the PARP protein has gained attention as a potential target for anticancer treatments. The Food and Drug Administration (FDA) has already approved a number of effective PARP1 inhibitors, including olaparib and niraparib. The final chemical has a 1,3,4-thiadiazole core in its structure. In fact, heterocyclic moieties have gained attention due to their numerous medicinal advantages, which include their capacity to combat cancer. The compounds derived from these substances have been studied as PARP1 inhibitors, with promising results. Thus, the goal of this study is to go over the importance of PARP1 in cancer as well as its role in cell regulation. It also attempts to offer a comprehensive assessment of the literature that has been published in the previous fifteen years about PARP1 inhibitors, including the different scaffolds, with an emphasis on features of the structure-activity relationship. This will provide vital information for the creation of fresh, more effective PARP1 inhibitors.

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  • Article Type:     Review Article
Keyword(s): anti-cancer; biological activities; DNA damage; FDA; Heterocyclic moieties; PARP1

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