关键词: DNA-binding domain N-terminal domain glucocorticoid receptor glucocorticoids ligand-binding domain nuclear receptor structure

Mesh : Humans Glucocorticoids / pharmacology metabolism Receptors, Glucocorticoid / metabolism Transcription Factors

来  源:   DOI:10.3390/cells12121636   PDF(Pubmed)

Abstract:
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.
摘要:
糖皮质激素受体α(GRα)是核受体超家族的成员,并充当糖皮质激素(GC)响应性转录因子。GR可以阻止炎症并杀死癌细胞,从而解释了糖皮质激素在临床上的广泛使用。然而,副作用和治疗阻力限制了GR的治疗潜力,强调解决GR所有针对具体情况的行动机制的重要性。幸运的是,对GR结构的理解,构象,不同GR控制的生物途径中的化学计量现在逐渐增加。这些信息对于缩小GR功能的知识差距至关重要。在这次审查中,我们关注GR的各个领域和作用机制,从结构的角度来看。
公众号