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Discovering alkylamide derivatives of bexarotene as new therapeutic agents against triple-negative breast cancer.

Abstract：

:Triple-negative breast cancer (TNBC) has been reported to be correlated with high expression of proliferation markers as well as constitutive activation of metastasis-relevant signaling pathways. For many years, breast cancer researchers have been investigating specific and effective methods to treat or to control the development of TNBC, but promising therapeutic options remain elusive. In this study, we have demonstrated that alkylamide derivatives of bexarotene DK-1-150 and DK-1-166 induce apoptotic cell death in TNBC cell lines without causing cytotoxicity in the normal mammary epithelial cell line. Furthermore, the bexarotene derivatives also showed significant effects in inhibiting TNBC cell proliferation and migration, modulating cancer stem cell markers expressions, as well as limiting the epithelial-mesenchymal transition (EMT) activities of TNBC cell lines in terms of downregulating EMT marker and blocking nuclear translocation of β-catenin. Therefore, we propose the alkylamide derivatives of bexarotene as potential candidates for novel anticancer therapeutics against TNBC.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Chen L,Long C,Nguyen J,Kumar D,Lee J

doi

10.1016/j.bmcl.2017.12.033

subject

Has Abstract

pub_date

2018-02-01 00:00:00

pages

420-424

issue

3

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(17)31193-9

journal_volume

28

pub_type

杂志文章

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