Digitalis as an immunomodulator

摘要

A chemical screen in an insect-cell-based reporter system has been used to identify the cardiac glycoside digoxin and various derivatives as inhibitors of the transcriptional activity of the retinoic-acid-related orphan nuclear receptor RORyt. Through this mechanism, these compounds block the differentiation of T_H17 cells in mice, and inhibit interleukin-17 production in vitro in human T cells. This suggests that digoxin derivatives can be used as chemical templates for RORγt-targeting therapeutics to treat inflammatory conditions and autoimmune diseases.