Selective peroxisome proliferator-activated receptor δ isosteric selenium agonists as potent anti-atherogenic agents in vivo

Jungwook Chin; Jun Young Hong; Jaehwan Lee; Hoosang Hwang; Hyunsil Ko; Hyukjae Choi; Dongyup Hahn; Jaeyoung Ko; Sang-Jip Nam; Jungae Tak; Jungyeob Ham; Heonjoong Kang

doi:10.1016/j.bmcl.2010.10.103

Selective peroxisome proliferator-activated receptor δ isosteric selenium agonists as potent anti-atherogenic agents in vivo

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7239-42. doi: 10.1016/j.bmcl.2010.10.103. Epub 2010 Oct 26.

Authors

Jungwook Chin¹, Jun Young Hong, Jaehwan Lee, Hoosang Hwang, Hyunsil Ko, Hyukjae Choi, Dongyup Hahn, Jaeyoung Ko, Sang-Jip Nam, Jungae Tak, Jungyeob Ham, Heonjoong Kang

Affiliation

¹ Center for Marine Natural Products and Drug Discovery, School of Earth and Environmental Sciences, Seoul National University, Seoul, Republic of Korea.

PMID: 21074432
DOI: 10.1016/j.bmcl.2010.10.103

Abstract

We report the synthesis and in vivo activity of a novel anti-atherogenic agent, isosteric selenium PPARδ-selective ligand. This ligand did not cause significant body or liver weight changes and did not have obvious adverse effects on intestinal polyp formation. Our overall results clearly demonstrate that PPARδ is a viable drug candidate for targeting and treating atherosclerosis.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Apolipoproteins E / genetics
Apolipoproteins E / metabolism
Atherosclerosis / drug therapy
Fluorescence Resonance Energy Transfer
Ligands
Mice
Mice, Knockout
PPAR delta / agonists*
PPAR delta / metabolism
Selenium / chemistry*
Thiazoles / chemistry

Substances

Apolipoproteins E
Ligands
PPAR delta
Thiazoles
Selenium