Cited by 93PARP inhibition in cancer therapyBRCA gene mutations in cancerOvarian cancer diagnosis and treatment

Differences in PARP Inhibitors for the Treatment of Ovarian Cancer: Mechanisms of Action, Pharmacology, Safety, and Efficacy

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Valabrega, Giorgio, Scotto, Giulia, Tuninetti, Valentina, Pani, Arianna, Scaglione, Francesco·2021·International Journal of Molecular Sciences

Abstract

Poly(ADP-ribose) polymerases (PARP) are proteins responsible for DNA damage detection and signal transduction. PARP inhibitors (PARPi) are able to interact with the binding site for PARP cofactor (NAD+) and trapping PARP on the DNA. In this way, they inhibit single-strand DNA damage repair. These drugs have been approved in recent years for the treatment of ovarian cancer. Although they share some similarities, from the point of view of the chemical structure and pharmacodynamic, pharmacokinetic properties, these drugs also have some substantial differences. These differences may underlie the different safety profiles and activity of PARPi.

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  • Functional analyses, alongside molecular assays, are required to confirm the predicted response of women with ovarian cancer to PARP inhibitors such as olaparib, niraparib and rucaparib.

    “Functional analyses, alongside molecular assays, are required to confirm the predicted response of women with ovarian cancer to PARPis such as the FDA-approved drugs olaparib, niraparib and rucaparib (Dickson et al., 2021; Lee et al., 2021; Valabrega et al., 2021).”

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Authors
Valabrega, G., Scotto, G., Tuninetti, V., Pani, A., & Scaglione, F.
Affiliations
  • Candiolo Cancer Institute (IT)
  • University of Milan (IT)
Corresponding author
Valabrega, Giorgio
Venue
International Journal of Molecular Sciences
Publisher
MDPI AG
Published
2021-04-19
Volume
22
Issue
8
Pages
4203
ISSN
1422-0067 (ISSN-L)
OpenAlex
W3156758253
Cited by
93
References
83
Citations by year
2026: 9 · 2025: 14 · 2024: 19 · 2023: 21 · 2022: 24 · 2021: 6
FWCI
2.12
Type
journal article
Language
en
Open access
Locations
  • International Journal of Molecular Sciences (publishedVersion, cc-by)
  • PubMed Central (publishedVersion, cc-by)
  • PubMed (publishedVersion)
  • Institutional Research Information System University of Turin (University of Turin) (submittedVersion, other-oa)
  • Archivio Istituzionale della Ricerca (Universita Degli Studi Di Milano) (submittedVersion, other-oa)
  • DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
Funders
GlaxoSmithKline
Topics
  • Health Sciences › Medicine › Oncology › PARP inhibition in cancer therapy
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › BRCA gene mutations in cancer
  • Health Sciences › Medicine › Reproductive Medicine › Ovarian cancer diagnosis and treatment
Keywords
PARP inhibitors, ovarian cancer, poly(ADP-ribose) polymerase, NAD+ binding, pharmacokinetics, pharmacodynamics, drug safety, drug efficacy
MeSH terms
Poly(ADP-ribose) Polymerase Inhibitors, Female, Humans, Ovarian Neoplasms, Phthalazines, Piperazines

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