当前位置： SCI文献检索 > BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS期刊下所有文献 > Erybraedin A is a potential Src inhibitor that blocks the adhesion and viability of non-small-cell lung cancer cells.

Erybraedin A is a potential Src inhibitor that blocks the adhesion and viability of non-small-cell lung cancer cells.

Abstract：

:The adhesion of cancer cells to the extracellular matrix (ECM) is crucial for cell proliferation, survival, and metastasis. Thus, it is necessary to inhibit cell-ECM adhesion by blocking the activation of the associated signaling to control cancer. Here, we identify erybraedin A (EBA) as a potential Src inhibitor that blocks cell adhesion and viability in non-small-cell lung cancer (NSCLC). EBA significantly inhibited the adhesion of NSCLC cells to fibronectin. EBA also markedly inhibited the activation of Src and its downstream targets, including FAK and Akt. The interaction between integrin β1 or integrin β3 and Src was inhibited by EBA treatment. A docking study revealed the bindings of EBA to the ATP-binding pocket and the allosteric regulatory site of the Src kinase. Additionally, EBA markedly inhibited the viability and the colony formation of NSCLC cells and induced apoptotic cell death. These results describe novel biological properties of EBA, which can block the Src-mediated adhesion and survival of NSCLC cells, suggesting the potential of EBA as an anticancer Src inhibitor that warrants further development in advanced preclinical and clinical settings.

journal_name

Biochem Biophys Res Commun

journal_title

Biochemical and biophysical research communications

authors

Min HY,Jung Y,Park KH,Oh WK,Lee HY

doi

10.1016/j.bbrc.2018.05.137

subject

Has Abstract

pub_date

2018-07-07 00:00:00

pages

145-151

issue

1

eissn

0006-291X

issn

1090-2104

pii

S0006-291X(18)31206-3

journal_volume

502

pub_type

杂志文章

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