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Title 

Methyllucidone inhibits STAT3 activity by regulating the expression of the protein tyrosine phosphatase MEG2 in DU145 prostate carcinoma cells

 

Methyllucidone의 항암 효과 관련 표적 발굴 및 기전 규명

Authors 

Yena JinYoung Hwan KimJin Young ParkYu Jin LeeH M OhS K ChoiDong Cho HanByoung-Mog Kwon

Publisher 

Elsevier

Issue Date 

2018

Citation 

Bioorganic & Medicinal Chemistry Letters

Keywords 

ApoptosisMEG2 phosphataseMethyllucidoneProstate cancerSTAT3

Abstract 

During the search for signal transducer and activator of transcription 3 (STAT3) inhibitors from natural products, methyllucidone, isolated from Lindera species (Lauraceae), was identified as a STAT3 inhibitor. Methyllucidone inhibited STAT3 phosphorylation at tyrosine 705 in a dose- and time dependent manner in DU145 prostate cancer cells and suppressed IL-6-induced STAT3 phosphorylation at Tyr-705 in LNCaP cells. Methyllucidone decreased the expression levels of STAT3 target genes, such as cyclin D1, cyclin A, Bcl-2, Mcl-1, and survivin. Methyllucidone inhibited DU145 cell growth and induced apoptosis by arresting the cell cycle at G1 phase. Notably, knockdown of the MEG2 gene by small interfering RNA suppressed the ability of methyllucidone to inhibit STAT3 activation. Methyllucidone regulates STAT3 activity by modulating MEG2 expression, and our results suggest that this compound is a novel inhibitor of the STAT3 pathway and may be a useful lead molecule for the development of a therapeutic STAT3 inhibitor

ISSN 

0960-894X

Link 

http://dx.doi.org/10.1016/j.bmcl.2018.02.012

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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