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.
No
English
Efficacy; Niraparib; Olaparib; Ovarian cancer; Rucaparib; Safety; Female; Humans; Ovarian Neoplasms; Phthalazines; Piperazines; Poly(ADP-ribose) Polymerase Inhibitors
Settore BIO/14 - Farmacologia
Review essay
Esperti anonimi
Ricerca applicata
Pubblicazione scientifica
apr-2021
MDPI
22
8
4203
1
16
16
Pubblicato
Periodico con rilevanza internazionale
scopus
orcid
pubmed
crossref
wos
Aderisco
info:eu-repo/semantics/article
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]
open
Prodotti della ricerca::01 - Articolo su periodico
5
262
Article (author)
no
G. Valabrega, G. Scotto, V. Tuninetti, A. Pani, F. Scaglione
File in questo prodotto:
File Dimensione Formato  
ijms-22-04203.pdf

accesso aperto

Tipologia: Publisher's version/PDF
Dimensione 692.76 kB
Formato Adobe PDF
692.76 kB Adobe PDF Visualizza/Apri
Pubblicazioni consigliate

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/903696
Citazioni
  • ???jsp.display-item.citation.pmc??? 21
  • Scopus 52
  • ???jsp.display-item.citation.isi??? 48
social impact