Styrylphenylphthalimides as Novel Transrepression-Selective Liver X Receptor (LXR) Modulators.

ABSTRACT: Anti-inflammatory effects of liver X receptor (LXR) ligands are thought to be largely due to LXR-mediated transrepression, whereas side effects are caused by activation of LXR-responsive gene expression (transactivation). Therefore, selective LXR modulators that preferentially exhibit transrepression activity should exhibit anti-inflammatory properties with fewer side effects. Here, we synthesized a series of styrylphenylphthalimide analogues and evaluated their structure-activity relationships focusing on LXRs-transactivating-agonistic/antagonistic activities and transrepressional activity. Among the compounds examined, 17l showed potent LXR-transrepressional activity with high selectivity over transactivating activity and did not show characteristic side effects of LXR-transactivating ag

SUBMITTER: Nomura S 

PROVIDER: S-EPMC4538439 | biostudies-literature | 2015 Aug

REPOSITORIES: biostudies-literature