Glucocorticoid receptors: finding the middle ground.
Glucocorticoids (GCs; referred to clinically as corticosteroids) are steroid hormones with potent anti-inflammatory and immune modulatory profiles. Depending on the context, these hormones can also mediate pro-inflammatory activities, thereby serving as primers of the immune system. Their target receptor, the GC receptor (GR), is a multi-tasking transcription factor, changing its role and function depending on cellular and organismal needs. To get a clearer idea of how to improve the safety profile of GCs, recent studies have investigated the complex mechanisms underlying GR functions. One of the key findings includes both pro- and anti-inflammatory roles of GR, and a future challenge will be to understand how such paradoxical findings can be reconciled and how GR ultimately shifts the balance to a net anti-inflammatory profile. As such, there is consensus that GR deserves a second life as a drug target, with either refined classic GCs or a novel generation of nonsteroidal GR-targeting molecules, to meet the increasing clinical needs of today to treat inflammation and cancer.
Sofie J
SJ
Desmet
Karolien
K
De Bosscher
D000700:Analgesics / Q000627:therapeutic use*; D000818:Animals; D016503:Drug Delivery Systems; D005938:Glucocorticoids / Q000276:immunology*; D006801:Humans; D007249:Inflammation / Q000276:immunology / Q000473:pathology / Q000628:therapy; D009363:Neoplasm Proteins / Q000276:immunology*; D009369:Neoplasms / Q000188:drug therapy / Q000276:immunology / Q000473:pathology; D011965:Receptors, Glucocorticoid / Q000276:immunology*
D000700:Analgesics; D005938:Glucocorticoids; D009363:Neoplasm Proteins; D011965:Receptors, Glucocorticoid