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Glucocorticoid receptor agonists and antagonists act on the nuclear receptor activated by cortisol. The glucocorticoid receptor (GR) is a ligand-activated transcription factor that controls genes for metabolism, stress responses and inflammation. Cloning of the human GR complementary DNA in 1985 placed it in the steroid hormone receptor family. A 2002 crystal structure of its ligand-binding domain with dexamethasone revealed a new dimer interface and mode of coactivator binding. The category covers the endogenous hormone hydrocortisone (cortisol) and synthetic agonists such as dexamethasone, budesonide and fluticasone propionate. The antagonist mifepristone, by contrast, blocks both glucocorticoid and progesterone receptors. Some entries act mainly on other targets, such as the progestin levonorgestrel and GANT61, an antagonist of glioma-associated oncogene (GLI) transcription factors.
SelDeg51 is a selective PROTAC degrader targeting FKBP51 with a Kd value of 18 nM and a maximum degradation efficacy (Dmax) of 90%. It facilitates the proteasomal degradation of FKBP51 through the formation of a ternary complex with FKBP51 and VHL, effectively reactivating glucocorticoid receptor signaling. SelDeg51 is particularly relevant for research in stress-related mental disorders, chronic pain, and obesity.
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GR-14-3-3 stabilizer-1 is a molecular glue stabilizer that effectively enhances the stability of glucocorticoid receptors (GR) by preventing their interaction with 14-3-3 proteins. This compound is instrumental in research involving the modulation of GR signaling pathways, providing a valuable tool for studying glucocorticoid-related cellular responses and their implications in various disease states. Its applications extend to the development of novel therapeutic strategies targeting GR dynamics in cellular contexts.
