Department of Pathology, University of Iowa Hospitals and Clinics, RCP 6233, 200 Hawkins Drive, Iowa City, IA 52242, USA.
Mol Cell Endocrinol. 2011 Mar 1;334(1-2):39-48. doi: 10.1016/j.mce.2010.06.016. Epub 2010 Jul 6.
Nuclear hormone receptors (NHRs) are transcription factors that work in concert with co-activators and co-repressors to regulate gene expression. Some examples of ligands for NHRs include endogenous compounds such as bile acids, retinoids, steroid hormones, thyroid hormone, and vitamin D. This review describes the evolution of liver X receptors α and β (NR1H3 and 1H2, respectively), farnesoid X receptor (NR1H4), vitamin D receptor (NR1I1), pregnane X receptor (NR1I2), and constitutive androstane receptor (NR1I3). These NHRs participate in complex, overlapping transcriptional regulation networks involving cholesterol homeostasis and energy metabolism. Some of these receptors, particularly PXR and CAR, are promiscuous with respect to the structurally wide range of ligands that act as agonists. A combination of functional and computational analyses has shed light on the evolutionary changes of NR1H and NR1I receptors across vertebrates, and how these receptors may have diverged from ancestral receptors that first appeared in invertebrates.
核激素受体（NHRs）是转录因子，与共激活因子和共抑制因子协同作用，调节基因表达。NHRs 的一些配体包括内源性化合物，如胆汁酸、视黄酸、甾体激素、甲状腺激素和维生素 D。本文综述了肝 X 受体 α 和 β（分别为 NR1H3 和 1H2）、法尼醇 X 受体（NR1H4）、维生素 D 受体（NR1I1）、孕烷 X 受体（NR1I2）和组成型雄烷受体（NR1I3）的进化。这些 NHRs 参与涉及胆固醇稳态和能量代谢的复杂、重叠的转录调控网络。这些受体中的一些，特别是 PXR 和 CAR，对作为激动剂的结构广泛的配体具有混杂性。功能和计算分析的结合揭示了脊椎动物中 NR1H 和 NR1I 受体的进化变化，以及这些受体如何从最初出现在无脊椎动物中的祖先受体中分化出来。
