| Literature DB >> 24900337 |
Konstantin Chegaev1, Chiara Riganti2, Loretta Lazzarato1, Barbara Rolando1, Stefano Guglielmo1, Ivana Campia2, Roberta Fruttero1, Amalia Bosia2, Alberto Gasco1.
Abstract
Products 4 and 5, obtained by conjugation of doxorubicin with nitric oxide (NO) donor nitrooxy and phenylsulfonyl furoxan moieties, respectively, accumulate in doxorubicin-resistant human colon cancer cells (HT29-dx), inducing high cytotoxicity. This behavior parallels the ability of the compounds to generate NO, detected as nitrite, in these cells. Preliminary immunoblotting studies suggest that the mechanism that underlies the cytotoxic effect could involve inhibition of cellular drug efflux due to nitration of tyrosine residues of the MRP3 protein pump.Entities:
Keywords: Multidrug resistance; P-glycoprotein; doxorubicin; nitric oxide
Year: 2011 PMID: 24900337 PMCID: PMC4018161 DOI: 10.1021/ml100302t
Source DB: PubMed Journal: ACS Med Chem Lett ISSN: 1948-5875 Impact factor: 4.345