VIB Center for Medical Biotechnology, VIB, 9052 Ghent, Belgium.
Department of Biomolecular Medicine, Ghent University, 9000 Ghent, Belgium.
Cells. 2023 Jun 15;12(12):1636. doi: 10.3390/cells12121636.
The glucocorticoid receptor α (GRα) is a member of the nuclear receptor superfamily and functions as a glucocorticoid (GC)-responsive transcription factor. GR can halt inflammation and kill off cancer cells, thus explaining the widespread use of glucocorticoids in the clinic. However, side effects and therapy resistance limit GR's therapeutic potential, emphasizing the importance of resolving all of GR's context-specific action mechanisms. Fortunately, the understanding of GR structure, conformation, and stoichiometry in the different GR-controlled biological pathways is now gradually increasing. This information will be crucial to close knowledge gaps on GR function. In this review, we focus on the various domains and mechanisms of action of GR, all from a structural perspective.
糖皮质激素受体 α（GRα）是核受体超家族的一员，作为糖皮质激素（GC）反应性转录因子发挥作用。GR 可以阻止炎症并杀死癌细胞，这解释了糖皮质激素在临床上的广泛应用。然而，副作用和治疗抵抗限制了 GR 的治疗潜力，这强调了确定所有 GR 特定于上下文的作用机制的重要性。幸运的是，现在人们对不同 GR 控制的生物途径中 GR 的结构、构象和化学计量的理解逐渐增加。这些信息对于缩小对 GR 功能的认识差距至关重要。在这篇综述中，我们从结构角度重点关注了 GR 的各种结构域和作用机制。
