Institut de Génomique Fonctionnelle de Lyon, Université de Lyon, Université Lyon 1, CNRS UMR5242, Ecole Normale Supérieure de Lyon, 32-34 Avenue Tony Garnier, 69007, Lyon, France.
Laboratory of Stem Cells and Cancer, Université Libre de Bruxelles, Brussels, Belgium.
Cell Mol Life Sci. 2020 Nov;77(22):4573-4579. doi: 10.1007/s00018-020-03549-0. Epub 2020 May 24.
Estrogen related receptors (ERRα, β and γ in mammals) are orphan members of the nuclear receptor superfamily acting as transcription factors. ERRs are expressed in several tissues and cells and they display various physiological and pathological functions, controlling, amongst others and depending on the receptor, bone homeostasis, energy metabolism, embryonic stem cell pluripotency, and cancer progression. In contrast to classical nuclear receptors, the activities of the ERRs are not controlled by a natural ligand. Regulation of their activities thus rely on other means such as post-translational modification or availability of transcriptional co-regulators. In addition, regulation of their mere expression under given physiological or pathological conditions is a particularly important level of control. Here we discuss the mechanisms involved in the regulation of ERRs expression and the reported means to impact on it using pharmacological approaches.
雌激素相关受体（ERRα、β 和 γ 在哺乳动物中）是核受体超家族的孤儿成员，作为转录因子发挥作用。ERRs 在多种组织和细胞中表达，它们具有多种生理和病理功能，控制着骨稳态、能量代谢、胚胎干细胞多能性和癌症进展等功能。与经典核受体不同，ERRs 的活性不受天然配体的控制。因此，它们的活性调节依赖于其他方式，如翻译后修饰或转录共调节剂的可用性。此外，在特定的生理或病理条件下，仅仅调节它们的表达是一个特别重要的控制水平。在这里，我们讨论了调节 ERRs 表达的机制，以及使用药理学方法来影响它们的报道手段。
