Novel AhR agonist with enhanced antipsoriatic activity
Sep. 12, 2023
Aryl hydrocarbon receptor (AhR) is a ligand-dependent transcription factor that maintains skin homeostasis in healthy skin and is expressed in keratinocytes, fibroblasts, mastocytes and melanocytes. In inflammatory skin disorders such as psoriasis, AhR deficit leads to marked skin inflammation, abnormal barrier function and increased cytokine release. Researchers from Sichuan University have reported the discovery and optimization of a new series of 2-thioxoimidazolidin-4-one derivatives acting as AhR agonists that led to the identification of [I] as the lead compound, which showed an EC50 value of 0.015 µM against AhR.