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Glycosylation enhances the anti-migratory activities of isomalyngamide A analogs.

Abstract：

:Three, new, fully synthetic glycosylated isomalyngamide A analogs 4-6 were prepared and evaluated for their anti-migratory activities in human breast cancer cells. The results of the study show that two glycosylated derivatives 4 and 5, containing mannose and galactose appendages, suppress metastatic events (e.g., migration, invasion and adhesion) in human breast adenocarcinoma MDA-MB-231 cells at "nontoxic" concentration levels. In contrast, derivative 6 that contains a lactose moiety, displays a less potent activity. The findings show that monosaccharide rather than disaccharide appendages to the isomalyngamide A backbone more greatly influence cell migration and invasive ability. Evidence has been gained for a mechanism for inhibition of metastatic activities in MDA-MB-231 cells by 4 and 5, involving inactivation of the expression of p-FAK and paxillin through the integrin-mediated antimetastatic pathway.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

More SV,Chang TT,Chiao YP,Jao SC,Lu CK,Li WS

doi

10.1016/j.ejmech.2013.03.044

subject

Has Abstract

pub_date

2013-06-01 00:00:00

pages

169-78

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(13)00204-3

journal_volume

64

pub_type

杂志文章

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