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PARP inhibitor

Model of the inhibitor olaparib (dark gray) occupying the NAD+-binding site of PARP1. From PDB: 5DS3​.

PARP inhibitors are a group of pharmacological inhibitors of the enzyme poly ADP ribose polymerase (PARP).

They are developed for multiple indications, including the treatment of heritable cancers.[1] Several forms of cancer are more dependent on PARP than regular cells, making PARP (PARP1, PARP2 etc.) an attractive target for cancer therapy.[2][3][4][5] PARP inhibitors appear to improve progression-free survival in women with recurrent platinum-sensitive ovarian cancer, as evidenced mainly by olaparib added to conventional treatment.[6]

In addition to their use in cancer therapy, PARP inhibitors are considered a potential treatment for acute life-threatening diseases, such as stroke and myocardial infarction, as well as for long-term neurodegenerative diseases.[7]

  1. ^ Blankenhorn D (2009-06-25). "PARP inhibitors working against inherited cancers | ZDNet Healthcare". ZDNet Healthcare owned by CBS Interactive Inc. ZDNet. Archived from the original on 2009-06-28. Retrieved 2019-12-05.
  2. ^ Pam Stephan. "PARP Inhibitor and DNA Polymerase Repair - PARP Inhibitor". About.com Health.
  3. ^ "Development of PARP Inhibitors: An Unfinished Story". cancernetwork.com. ONCOLOGY Vol 24 No 1. 24 (1). 15 January 2010.
  4. ^ "PARP Inhibitors – More Widely Effective than First Thought". drugdiscoveryopinion.com.
  5. ^ "PARP inhibitors: Halting cancer by halting DNA repair". Cancer Research UK. 24 September 2020.
  6. ^ Tattersall, Abigail; Ryan, Neil; Wiggans, Alison J.; Rogozińska, Ewelina; Morrison, Jo (2022-02-16). "Poly(ADP-ribose) polymerase (PARP) inhibitors for the treatment of ovarian cancer". The Cochrane Database of Systematic Reviews. 2022 (2): CD007929. doi:10.1002/14651858.CD007929.pub4. PMC 8848772. PMID 35170751.
  7. ^ Graziani G, Szabó C (July 2005). "Clinical perspectives of PARP inhibitors". Pharmacological Research. 52 (1): 109–18. doi:10.1016/j.phrs.2005.02.013. PMID 15911339.

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