Touitou I, Maudelonde T
INSERM U 148, Montpellier.
Rev Prat. 1994 May 15;44(10):1294-7.
Steroid receptors belong to a superfamily of hydrosoluble nuclear proteins which regulate transcription of a number of genes. In the absence of hormone, they are bound to proteins which maintain the receptors in an inactive state but prepared for binding with the hormone. In the presence of the hormone, the receptor is activated, which is reflected by modification of its physico-chemical constants and dissociation of associated proteins. This hormone-receptor complex forms a homodimer and binds to DNA at the regulatory regions of the genes involved, which is termed "hormone response element". The receptors are constituted of 5 to 6 domains, each responsible for one or several functions. The hormone binding domain (region E) and DNA binding domain (region C) are the most highly conserved. Progress in the comprehension of the mechanism of action of these receptors has led to the development of antihormones which are important in the treatment of hormone-dependent cancer. With progress in molecular biology, it is now possible to detect mutants of the receptors or their absence in syndromes involving hormonal resistance.
类固醇受体属于水溶性核蛋白超家族,可调节许多基因的转录。在没有激素的情况下,它们与蛋白质结合,这些蛋白质使受体保持无活性状态,但已准备好与激素结合。在有激素存在时,受体被激活,这表现为其物理化学常数的改变以及相关蛋白质的解离。这种激素 - 受体复合物形成同源二聚体,并与所涉及基因的调控区域的DNA结合,这被称为“激素反应元件”。受体由5至6个结构域组成,每个结构域负责一种或几种功能。激素结合结构域(E区)和DNA结合结构域(C区)是最高度保守的。对这些受体作用机制理解的进展导致了抗激素的开发,抗激素在激素依赖性癌症的治疗中很重要。随着分子生物学的进展,现在有可能在涉及激素抵抗的综合征中检测到受体的突变体或其缺失情况。