Power R F, Conneely O M, O'Malley B W
Department of Cell Biology, Baylor College of Medicine, Houston, TX 77030.
Trends Pharmacol Sci. 1992 Aug;13(8):318-23. doi: 10.1016/0165-6147(92)90099-r.
For many years the prevailing view of how steroid hormone receptors exert their effects on gene transcription has been that these intracellular receptor proteins, upon association with their specific cognate ligands, undergo a transformation to a state where they are capable of interacting with chromatin and regulating the transcription of specific genes. It has become implicit dogma in the field of biochemical endocrinology that receptor activation is absolutely dependent upon this ligand-binding event. However, recent studies described here by Bert O'Malley and colleagues have shown that certain members of the steroid hormone receptor superfamily can be activated in a totally ligand-independent manner by a cell membrane receptor agonist, the neurotransmitter dopamine.
多年来，关于类固醇激素受体如何对基因转录发挥作用的主流观点一直是，这些细胞内受体蛋白在与它们特定的同源配体结合后，会发生转变，进入一种能够与染色质相互作用并调节特定基因转录的状态。在生化内分泌学领域，受体激活绝对依赖于这种配体结合事件已成为不言而喻的教条。然而，伯特·奥马利及其同事在此描述的最新研究表明，类固醇激素受体超家族的某些成员可以被细胞膜受体激动剂——神经递质多巴胺以完全不依赖配体的方式激活。
