Kasuga Jun-ichi, Ishida Seiichi, Yamasaki Daisuke, Makishima Makoto, Doi Takefumi, Hashimoto Yuichi, Miyachi Hiroyuki
Institute of Molecular and Cellular Biosciences, The University of Tokyo, Tokyo 113-0032, Japan.
Bioorg Med Chem Lett. 2009 Dec 1;19(23):6595-9. doi: 10.1016/j.bmcl.2009.10.021. Epub 2009 Oct 8.
We designed and synthesized novel PPARdelta antagonists based on the crystal structure of the PPARdelta full agonist TIPP-204 bound to the PPARdelta ligand-binding domain, in combination with our nuclear receptor helix 12 folding modification hypothesis. Representative compound 3a exhibits PPARdelta-preferential antagonistic activity.
我们基于与PPARδ配体结合域结合的PPARδ完全激动剂TIPP-204的晶体结构，并结合我们的核受体螺旋12折叠修饰假说，设计并合成了新型PPARδ拮抗剂。代表性化合物3a表现出PPARδ优先拮抗活性。
