Gadwala Saranya, Ghosh Chaitali
Neurovascular Research, Department of Biomedical Engineering, Lerner Research Institute, Cleveland Clinic, Cleveland, OH 44195, USA.
Department of Biomedical Engineering and Molecular Medicine, Cleveland Clinic Lerner College of Medicine of Case Western Reserve University, Cleveland, OH 44195, USA.
Int J Mol Sci. 2025 Apr 29;26(9):4213. doi: 10.3390/ijms26094213.
Hormone-dependent phosphorylation of steroid receptors is a mechanism for modulating glucocorticoid receptor (GR) transcriptional responses. Evidence indicates that GR phosphorylation can influence receptor transcriptional activation in a gene-specific manner, which could have positive or negative impacts, where the relative level of phosphorylation is an important determinant of overall GR function. This review provides insights into the regulatory mechanism of GR phosphorylation in the brain, cellular and molecular specificity affecting neurovascular function, and the impact of GR phosphorylation in neurological disorders. Furthermore, the role of various endogenous and exogenous factors and sex-dependent associations with GR functional changes due to phosphorylation and other interlinking mechanisms are considered. Finally, we highlight the potential therapeutic approaches which have been evaluated, while challenging GR phosphorylation and the overall influence on the activity of GR in brain disorders.
类固醇受体的激素依赖性磷酸化是调节糖皮质激素受体(GR)转录反应的一种机制。有证据表明,GR磷酸化能够以基因特异性方式影响受体转录激活,这可能产生正面或负面影响,其中磷酸化的相对水平是GR整体功能的重要决定因素。本综述深入探讨了大脑中GR磷酸化的调控机制、影响神经血管功能的细胞和分子特异性,以及GR磷酸化在神经疾病中的影响。此外,还考虑了各种内源性和外源性因素的作用以及因磷酸化和其他相互关联机制导致的GR功能变化的性别依赖性关联。最后,我们强调了已评估的潜在治疗方法,同时对GR磷酸化提出挑战以及其对脑部疾病中GR活性的整体影响。