Probing the Anticancer Mechanism of (−)‐Ainsliatrimer A through Diverted Total Synthesis and Bioorthogonal Ligation1. Issue 45 (15th September 2014)

• Record Type: Journal Article
• Authors: Li, Chao; Dong, Ting; Li, Qiang; Lei, Xiaoguang
• Is Part Of: Angewandte Chemie international edition. Volume 53:Issue 45(2014)
• Page Start: 12111
• Page End: 12115
• Publication Date: 2014-09-15
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1002/anie.201407225
• Languages: English
• ISSNs: 1433-7851

Abstract

<abstract abstract-type="main" xml:lang="en"> <title>Abstract</title> <p>Herein, we report an efficient approach for exploring the novel anticancer mechanism of (−)‐ainsliatrimer A, a structurally complex and unique trimeric sesquiterpenoid, through a combined strategy of diverted total synthesis (DTS) and bioorthogonal ligation (TQ ligation), which allowed us to visualize the subcellular localization of this natural product in live cells. Further biochemical studies facilitated by pretarget imaging revealed that PPARγ, a nucleus receptor, was a functional cellular target of ainsliatrimer A. We also confirmed that the anticancer activity of ainsliatrimer A was caused by the activation of PPARγ.</p> </abstract>