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

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 dr...

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Autores principales: Valabrega, Giorgio, Scotto, Giulia, Tuninetti, Valentina, Pani, Arianna, Scaglione, Francesco
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Review
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8073512/
https://www.ncbi.nlm.nih.gov/pubmed/33921561
http://dx.doi.org/10.3390/ijms22084203
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author Valabrega, Giorgio
Scotto, Giulia
Tuninetti, Valentina
Pani, Arianna
Scaglione, Francesco
author_facet Valabrega, Giorgio
Scotto, Giulia
Tuninetti, Valentina
Pani, Arianna
Scaglione, Francesco
author_sort Valabrega, Giorgio
collection PubMed
description 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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spelling pubmed-80735122021-04-27 Differences in PARP Inhibitors for the Treatment of Ovarian Cancer: Mechanisms of Action, Pharmacology, Safety, and Efficacy Valabrega, Giorgio Scotto, Giulia Tuninetti, Valentina Pani, Arianna Scaglione, Francesco Int J Mol Sci Review 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. MDPI 2021-04-19 /pmc/articles/PMC8073512/ /pubmed/33921561 http://dx.doi.org/10.3390/ijms22084203 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Valabrega, Giorgio
Scotto, Giulia
Tuninetti, Valentina
Pani, Arianna
Scaglione, Francesco
Differences in PARP Inhibitors for the Treatment of Ovarian Cancer: Mechanisms of Action, Pharmacology, Safety, and Efficacy
title Differences in PARP Inhibitors for the Treatment of Ovarian Cancer: Mechanisms of Action, Pharmacology, Safety, and Efficacy
title_full Differences in PARP Inhibitors for the Treatment of Ovarian Cancer: Mechanisms of Action, Pharmacology, Safety, and Efficacy
title_fullStr Differences in PARP Inhibitors for the Treatment of Ovarian Cancer: Mechanisms of Action, Pharmacology, Safety, and Efficacy
title_full_unstemmed Differences in PARP Inhibitors for the Treatment of Ovarian Cancer: Mechanisms of Action, Pharmacology, Safety, and Efficacy
title_short Differences in PARP Inhibitors for the Treatment of Ovarian Cancer: Mechanisms of Action, Pharmacology, Safety, and Efficacy
title_sort differences in parp inhibitors for the treatment of ovarian cancer: mechanisms of action, pharmacology, safety, and efficacy
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8073512/
https://www.ncbi.nlm.nih.gov/pubmed/33921561
http://dx.doi.org/10.3390/ijms22084203
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