Gilardi Federica, Desvergne Béatrice
Center for Integrative Genomics, University of Lausanne, Genopode Building, 1015, Lausanne, Switzerland,
Subcell Biochem. 2014;70:75-102. doi: 10.1007/978-94-017-9050-5_5.
Retinoid X Receptors (RXR) were initially identified as nuclear receptors binding with stereo-selectivity the vitamin A derivative 9-cis retinoic acid, although the relevance of this molecule as endogenous activator of RXRs is still elusive. Importantly, within the nuclear receptor superfamily, RXRs occupy a peculiar place, as they are obligatory partners for a number of other nuclear receptors, thus integrating the corresponding signaling pathways. In this chapter, we describe the structural features allowing RXR to form homo- and heterodimers, and the functional consequences of this unique ability. Furthermore, we discuss the importance of studying RXR activity at a genome-wide level in order to comprehensively address the biological implications of their action that is fundamental to understand to what extent RXRs could be exploited as new therapeutic targets.
维甲酸X受体(RXR)最初被鉴定为能与维生素A衍生物9-顺式视黄酸立体选择性结合的核受体,尽管该分子作为RXR内源性激活剂的相关性仍不明确。重要的是,在核受体超家族中,RXR占据着特殊地位,因为它们是许多其他核受体的必需伴侣,从而整合相应的信号通路。在本章中,我们描述了使RXR形成同二聚体和异二聚体的结构特征,以及这种独特能力的功能后果。此外,我们讨论了在全基因组水平上研究RXR活性的重要性,以便全面探讨其作用的生物学意义,这对于理解RXR在多大程度上可被开发为新的治疗靶点至关重要。