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.

Differences in parp inhibitors for the treatment of ovarian cancer: Mechanisms of action, pharmacology, safety, and efficacy

Valabrega G.;Scotto G.;Tuninetti V.;
2021-01-01

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.
2021
Apr 19;22
8
4203
4218
Efficacy; Niraparib; Olaparib; Ovarian cancer; Rucaparib; Safety; Female; Humans; Ovarian Neoplasms; Phthalazines; Piperazines; Poly(ADP-ribose) Polymerase Inhibitors
Valabrega G.; Scotto G.; Tuninetti V.; Pani A.; Scaglione F.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2318/1844899
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