McEwan Iain J, Nardulli Ann M
Molecular and Cellular Endocrinology, School of Medical Sciences, University of Aberdeen, Foresterhill, Aberdeen, Scotland, UK.
Nucl Recept Signal. 2009 Dec 31;7:e011. doi: 10.1621/nrs.07011.
Nuclear hormone receptors (NHRs) represent a large and diverse family of ligand-activated transcription factors involved in regulating development, metabolic homeostasis, salt balance and reproductive health. The ligands for these receptors are typically small hydrophobic molecules such as steroid hormones, thyroid hormone, vitamin D3 and fatty acid derivatives. The first NHR structural information appeared approximately 20 years ago with the solution and crystal structures of the DNA binding domains and was followed by the structure of the agonist and antagonist bound ligand binding domains of different NHR members. Interestingly, in addition to these defined structural features, it has become clear that NHRs also possess significant structural plasticity. Thus, the dynamic structure of the NHRs was the topic of a recent stimulating and informative FASEB Summer Research Conference held in Vermont.
核激素受体(NHRs)是一个庞大且多样的配体激活转录因子家族,参与调节发育、代谢稳态、盐平衡和生殖健康。这些受体的配体通常是小的疏水分子,如类固醇激素、甲状腺激素、维生素D3和脂肪酸衍生物。大约20年前,随着DNA结合域的溶液结构和晶体结构的出现,首次有了NHR的结构信息,随后不同NHR成员的激动剂和拮抗剂结合配体结合域的结构也相继被解析。有趣的是,除了这些明确的结构特征外,很明显NHRs还具有显著的结构可塑性。因此,NHRs的动态结构是最近在佛蒙特州举行的一次极具启发性和信息量的美国实验生物学联合会夏季研究会议的主题。