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- W3043809093 endingPage "112570" @default.
- W3043809093 startingPage "112570" @default.
- W3043809093 abstract "Poly(ADP-ribose) Polymerase 1 (PARP1), one of the most investigated 18 membered PARP family enzymes, is involved in a variety of cellular functions including DNA damage repair, gene transcription and cell apoptosis. PARP1 can form a PARP1(ADP-ribose) polymers, then bind to the DNA damage gap to recruit DNA repair proteins, and repair the break to maintain genomic stability. PARP1 is highly expressed in tumor cells, so the inhibition of PARP1 can block DNA repair, promote tumor cell apoptosis, and exert antitumor activity. To date, four PARP1 inhibitors namely olaparib, rucaparib, niraparib and talazoparib, have been approved by Food and Drug Administration (FDA) for treating ovarian cancer and breast cancer with BRCA1/2 mutation. These drugs have showed super advantages over conventional chemotherapeutic drugs with low hematological toxicity and slowly developed drug resistance. In this article, we summarize and analyze the structure features of PARP1, the biological functions and antitumor mechanisms of PARP1 inhibitors. Importantly, we suggest that establishing a new structure-activity relationship of developed PARP1 inhibitors via substructural searching and the matched molecular pair analysis would accelerate the process in finding more potent and safer PARP1 inhibitors." @default.
- W3043809093 created "2020-07-23" @default.
- W3043809093 creator A5006718110 @default.
- W3043809093 creator A5007215884 @default.
- W3043809093 creator A5045093595 @default.
- W3043809093 creator A5048643825 @default.
- W3043809093 creator A5052364380 @default.
- W3043809093 creator A5052949240 @default.
- W3043809093 creator A5052974453 @default.
- W3043809093 creator A5083809384 @default.
- W3043809093 date "2020-10-01" @default.
- W3043809093 modified "2023-10-16" @default.
- W3043809093 title "The ups and downs of Poly(ADP-ribose) Polymerase-1 inhibitors in cancer therapy–Current progress and future direction" @default.
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