Pubblicazioni

Autori:

Masetto, Francesca; Chegaev, Konstantin; Gazzano, Elena; Mullappilly, Nidula; Rolando, Barbara; Arpicco, Silvia; Fruttero, Roberta; Riganti, Chiara; Donadelli, Massimo

Titolo:

MRP5 nitration by NO-releasing gemcitabine encapsulated in liposomes confers sensitivity in chemoresistant pancreatic adenocarcinoma cells

Anno:

2020

Tipologia prodotto:

Articolo in Rivista

Tipologia ANVUR:

Articolo su rivista

Lingua:

Inglese

Formato:

Elettronico

Referee:

Sì

Nome rivista:

BBA - Molecular cell research

ISSN Rivista:

0167-4889

N° Volume:

1867

Numero o Fascicolo:

118824

Intervallo pagine:

1-14

Parole chiave:

Chemoresistance; Drug delivery; Gemcitabine; MDR; Nitric oxide; Pancreatic cancer

Breve descrizione dei contenuti:

Pancreatic ductal adenocarcinoma (PDAC) is a therapy recalcitrant disease characterized by the aberrations in multiple genes that drive pathogenesis and drug chemoresistance. In this study, we synthesize a library of seven novel nitric oxide-releasing gemcitabine pro-drugs (NO-GEMs) in order to improve the effectiveness of GEM by exploiting the therapeutic effects of NO. Among these NO-GEM pro-drugs we select 5b as the most effective compound in GEM-resistant PDAC cells. After its encapsulation in liposomes for drug delivery the intracellular NO level increases and nitration associated to activity inhibition of the multidrug resistance associated protein 5 (MRP5; ABCC5) occurs. This results in GEM intracellular accumulation and enhanced apoptotic cell death in GEM-resistant PDAC cells, which express MRP5 at higher levels than GEM-sensitive cells. Our results support the development of a new anti-tumoral strategy to efficiently affect GEM-resistant PDAC cells based on the usage of NO-GEM pro-drugs.

Pagina Web:

https://doi.org/10.1016/j.bbamcr.2020.118824

Id prodotto:

115990

Handle IRIS:

11562/1024365

ultima modifica:

15 novembre 2022

Citazione bibliografica:

Masetto, Francesca; Chegaev, Konstantin; Gazzano, Elena; Mullappilly, Nidula; Rolando, Barbara; Arpicco, Silvia; Fruttero, Roberta; Riganti, Chiara; Donadelli, Massimo, MRP5 nitration by NO-releasing gemcitabine encapsulated in liposomes confers sensitivity in chemoresistant pancreatic adenocarcinoma cells «BBA - Molecular cell research» , vol. 1867 , n. 118824 , 2020 , pp. 1-14

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