Development of Hybrid Phospholipid Mimics as Effective Agonists for Liver Receptor Homologue-1
Development of Hybrid Phospholipid Mimics as Effective Agonists for Liver Receptor Homologue-1
复制标题
DOI：
10.1021/acsmedchemlett.8b00361
复制
发表时间：
2018-10-01
影响因子：
4.2
通讯作者：
Jui, Nathan T.
中科院分区：
文献类型：
--
作者：
Flynn, Autumn R.;Mays, Suzanne G.;Jui, Nathan T.
The orphan nuclear receptor Liver Receptor Homologue-1 (LRH-1) is an emerging drug target for metabolic disorders. The most effective known LRH-1 HO modulators are phospholipids or synthetic hexahydropentalene compounds. While both classes have micromolar efficacy, they target different portions of the ligand binding pocket and activate LRH-1 through different mechanisms. Guided by crystallographic data, we combined aspects of both ligand classes into a single scaffold, resulting in the most potent and efficacious LRH-1 agonists to date.
