Abstract:
:In this study, we investigated the anticancer efficacy of pegylated liposomes containing 6BrCaQ, an hsp90 inhibitor derived from novobiocin. 6BrCaQ has been previously identified as the most potent compound in a series of quinoleic novobiocin analogs but is poorly water-soluble. We investigated, for the first time, the anti-proliferative effects of this drug in vivo in an orthotopic breast cancer model (MDA-MB-231 luc) using pegylated liposomes to allow its administration. Hsp90, hsp70 and hsp27 protein and mRNA expressions were not strongly affected after treatment meaning it did not induce a heat shock response often associated with resistance and poor prognosis. Liposomal delivery of 6BrCaQ retarded tumor growth at a low dose (1 mg/kg, injected once a week for 4 weeks). Histological analysis of tumors revealed necrosis and a lower proportion of proliferative cells in treated mice indicating that this drug has potential for breast cancer therapy when encapsulated in liposomes.
journal_name
Cancer Lettjournal_title
Cancer lettersauthors
Sauvage F,Fattal E,Al-Shaer W,Denis S,Brotin E,Denoyelle C,Blanc-Fournier C,Toussaint B,Messaoudi S,Alami M,Barratt G,Vergnaud-Gauduchon Jdoi
10.1016/j.canlet.2018.06.001subject
Has Abstractpub_date
2018-09-28 00:00:00pages
103-111eissn
0304-3835issn
1872-7980pii
S0304-3835(18)30397-5journal_volume
432pub_type
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