Center for Marine Natural Products and Drug Discovery, School of Earth and Environmental Sciences, Seoul National University, Seoul, Republic of Korea.
Bioorg Med Chem Lett. 2010 Dec 15;20(24):7239-42. doi: 10.1016/j.bmcl.2010.10.103. Epub 2010 Oct 26.
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.
我们报告了一种新型抗动脉粥样硬化剂——同型硒过氧化物酶体增殖物激活受体 δ（PPARδ）选择性配体的合成及体内活性。该配体不会引起明显的体重或肝脏重量变化，也不会对肠道息肉形成有明显的不良影响。我们的整体结果清楚地表明，PPARδ 是一种可行的药物靶点，可用于靶向治疗动脉粥样硬化。
