Glucocorticoids exert pleiotropic effects on all tissues to regulate cellular and metabolic homeostasis. Synthetic forms are used therapeutically in a wide range of conditions for their anti-inflammatory benefits, at the cost of dose and duration-dependent side effects. Significant variability occurs between tissues, disease states, and individuals with regard to both the beneficial and deleterious effects. The glucocorticoid receptor (GR) is the site of action for these hormones and a vast body of work has been conducted understanding its function. Traditionally, it was thought that the anti-inflammatory benefits of glucocorticoids were mediated by transrepression of pro-inflammatory transcription factors, while the adverse metabolic effects resulted from direct transactivation. This canonical understanding of the GR function has been brought into question over the past 2 decades with advances in the resolution of scientific techniques, and the discovery of multiple isoforms of the receptor present in most tissues. Here we review the structure and function of the GR, the nature of the receptor isoforms, and the contribution of the receptor to glucocorticoid sensitivity, or resistance in health and disease.

中文翻译：

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糖皮质激素受体：亚型、功能和对糖皮质激素敏感性的贡献。


糖皮质激素对所有组织发挥多效性作用，以调节细胞和代谢稳态。合成形式因其抗炎作用而被广泛用于治疗，但代价是剂量和持续时间依赖性的副作用。组织、疾病状态和个体之间在有益和有害影响方面都存在显着差异。糖皮质激素受体 （GR） 是这些激素的作用部位，已经进行了大量工作来了解其功能。传统上，人们认为糖皮质激素的抗炎作用是由促炎转录因子的反式抑制介导的，而不良代谢作用是由直接反式激活引起的。在过去的 2 年里，随着科学技术分辨率的进步，以及发现大多数组织中存在的受体的多种亚型，这种对 GR 功能的规范理解受到了质疑。在这里，我们回顾了 GR 的结构和功能、受体亚型的性质以及受体对糖皮质激素敏感性或健康和疾病耐药性的贡献。