Abstract：
Photo-switchable nuclear receptor modulators (\"photohormones\") enable spatial and temporal control over transcription factor activity and are valuable precision tools for biological studies. We have developed a new photohormone chemotype by incorporating a light-switchable motif in the scaffold of a cinalukast-derived PPARα ligand and tuned light-controlled activity by systematic structural variation. An optimized photohormone exhibited PPARα agonism in its light-induced (Z)-configuration and strong selectivity over related lipid-activated transcription factors representing a valuable addition to the collection of light-controlled tools to study nuclear receptor activity.
摘要：
光可切换核受体调节剂（“光激素”）可实现对转录因子活性的空间和时间控制，是生物学研究的宝贵精密工具。我们通过在卡鲁司特衍生的PPARα配体的支架中掺入光切换基序，并通过系统的结构变化调节了光控活性，从而开发了一种新的光激素化学型。优化的光激素在其光诱导的（Z）构型中表现出PPARα激动作用，并且对相关的脂质激活的转录因子具有很强的选择性，这是对研究核受体活性的光控工具集合的有价值的补充。
