Glucocorticoid receptor modulator, CpdA, is a cell-permeable aziridine precursor that acts as a non-steroidal, GR (glucocorticoid receptor)-activating ligand with a binding affinity that is 4-fold higher than that of dexamethasone (sc-29059). Glucocorticoid Receptor Modulator, CpdA, induces GR nuclear translocation and selectively activates GR-mediated transrepression of the NF-κB-dependent production of pro-inflammatory cytokines. Unlike DEX, CpdA exhibits no effect on GRE- (glucocorticoid response element) driven gene expression.
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PMID: # 25389358 Malaise, O. et al. 2015. Rheumatology (Oxford). 54: 1087-92.
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