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 / G. Valabrega, G. Scotto, V. Tuninetti, A. Pani, F. Scaglione. - In: INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES. - ISSN 1661-6596. - 22:8(2021 Apr), pp. 4203.1-4203.16. [10.3390/ijms22084203]

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

A. Pani
Penultimo
;
F. Scaglione
Ultimo
2021

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.
Efficacy; Niraparib; Olaparib; Ovarian cancer; Rucaparib; Safety; Female; Humans; Ovarian Neoplasms; Phthalazines; Piperazines; Poly(ADP-ribose) Polymerase Inhibitors
Settore BIO/14 - Farmacologia
apr-2021
Article (author)
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/903696
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