Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein–protein interaction profile

摘要: Glucocorticoids are commonly used antiinflammatory agents whose use is limited by side effects. We have developed a series of glucocorticoid receptor (GR) ligands that retain the strong activity conventional glucocorticoids with reduced present compound, LGD5552, binds efficiently and strongly represses inflammatory gene expression. LGD5552 bound to GR activates expression somewhat differently than glucocorticoids. It some genes an efficacy similar However, other glucocorticoid-activated not regulated LGD5552. These differences may be because more efficient binding corepressor in presence compared agonists. This class nonsteroidal, GR-dependent drugs offer safer alternative steroidal treatment disease.