• 中文
    • English
  • English 
    • 中文
    • English
  • Login
View Item 
  •   DSpace Home
  • 生命科学学院
  • 生命科学-已发表论文
  • View Item
  •   DSpace Home
  • 生命科学学院
  • 生命科学-已发表论文
  • View Item
JavaScript is disabled for your browser. Some features of this site may not work without it.

Revealing a natural marine product as a novel agonist for retinoic acid receptors with a unique binding mode and inhibitory effects on cancer cells

Thumbnail
Full Text
Revealing a natural marine product as a novel agonist for retinoic acid receptors with a unique binding mode and inhibitory effects on cancer cells.htm (391bytes)
Date
2012-08-15
Author
Wang, Shanshan
Wang, Zhao
Lin, Shengchen
Zheng, Weili
Wang, Rui
Jin, Shikai
Chen, Jinan
Jin, Lihua
Li, Yong
李勇
Collections
  • 生命科学-已发表论文 [5901]
Show full item record
Abstract
Retinoids display anti-tumour activity on various cancer cells and therefore have been used as important therapeutic agents. However, adverse side effects and RA (retinoic acid) resistance limit further development and clinical application of retinoid-based therapeutic agents. We report in the present paper the identification of a natural marine product that activates RARs (RA receptors) with a chemical structure distinct from retinoids by high-throughput compound library screening. Luffariellolide was uncovered as a novel RAR agonist by inducing co-activator binding to these receptors in vitro, further inhibiting cell growth and regulating RAR target genes in various cancer cells. Structural and molecular studies unravelled a unique binding mode of this natural ligand to RARs with an unexpected covalent modification on the RAR. Functional characterization further revealed that luffariellolide displays chemotherapeutic potentials for overcoming RA resistance in colon cancer cells, suggesting that luffariellolide may represent a unique template for designing novel non-retinoid compounds with advantages over current RA drugs.
Citation
BIOCHEMICAL JOURNAL,2012,446:79-87
URI
http://dx.doi.org/10.1042/BJ20120726
WOS:000307626300008
https://dspace.xmu.edu.cn/handle/2288/14950

copyright © 2002-2016  Duraspace  Theme by @mire  厦门大学图书馆  
About | Policies
 

 

Browse

All of DSpaceCommunities & CollectionsBy Issue DateAuthorsTitlesSubjectsThis CollectionBy Issue DateAuthorsTitlesSubjects

My Account

LoginRegister

copyright © 2002-2016  Duraspace  Theme by @mire  厦门大学图书馆  
About | Policies