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糖皮质激素(glucocorticoid,GC)具有重要的生理和药理作用,其作用主要通过GC受体(glucocorticoid receptor,GR)的介导而发挥。作为配体依赖性的转录调节因子,GR的活性除了受GC调节外,还受磷酸化的调节。GR分子,特别是在它的N端区存在多个磷酸化位点,能以激素依赖性或者非依赖性的方式被细胞特异性的激酶,如周期素依赖性蛋白激酶(CDKs)、糖原合成酶激酶3β(GSK3β)和丝裂原激活的蛋白激酶(MAPKs)等磷酸化。磷酸化调节GR的信号转导与转录活性等,并影响组织细胞对GC的反应性和参与疾病的发生发展。本文就GR磷酸化方面的研究进展及其生理病理意义作一综述。
Glucocorticoid (GC) has important physiological and pharmacological effects, its role mainly through the GC receptor (glucocorticoid receptor, GR) mediated play. As a ligand-dependent transcriptional regulator, the activity of GR is regulated by phosphorylation in addition to GC. The GR molecule, particularly in its N-terminal region, has multiple phosphorylation sites that can be blocked by cell-specific kinases, such as cyclin-dependent protein kinases (CDKs), glycogen in a hormone-dependent or non-dependent manner Synthase kinase 3β (GSK3β) and mitogen-activated protein kinases (MAPKs) are phosphorylated. Phosphorylation regulates the signal transduction and transcriptional activity of GR, and affects the reactivity of tissue cells to GC and participates in the occurrence and development of the disease. This article reviews the progress of GR phosphorylation and its physiological and pathological significance.