Trapp T, Holsboer F
Clinical Institute, Max Planck Institute of Psychiatry, Munich, Germany.
Trends Pharmacol Sci. 1996 Apr;17(4):145-9. doi: 10.1016/0165-6147(96)81590-2.
Gene regulation by steroids is mediated by the binding of the endogenous or pharmacological ligand to the corresponding nuclear receptor. Ligand-activated steroid receptors usually regulate the expression of responsive genes by binding to common response elements on DNA as homodimers. However, recent findings indicate that mineralocorticoid and glucocorticoid receptors are able to interact by forming heterodimers. In tissues coexpressing both of these corticosteroid receptors, heterodimerization between them may be a hitherto unrecognized modality for the transcriptional regulation of corticosteroid-responsive genes. In this review, Thorsten Trapp and Florian Holsboer discuss the potential impact of this heterodimerization on corticosteriod physiology and pharmacology.
类固醇的基因调控是通过内源性或药理配体与相应核受体的结合来介导的。配体激活的类固醇受体通常作为同二聚体与DNA上的共同反应元件结合，从而调节反应性基因的表达。然而，最近的研究结果表明，盐皮质激素受体和糖皮质激素受体能够通过形成异二聚体相互作用。在同时表达这两种皮质类固醇受体的组织中，它们之间的异二聚化可能是一种迄今未被认识的皮质类固醇反应性基因转录调控方式。在这篇综述中，托尔斯滕·特拉普和弗洛里安·霍尔茨博尔讨论了这种异二聚化对皮质类固醇生理学和药理学的潜在影响。
