Abstract：
Nuclear receptors (NR) collectively regulate several biological functions in various organs. While NRs can be characterized by activation of the transcription of their signature genes, they also have other diverse roles. Although most NRs are directly activated by ligand binding, which induces cascades of events leading to gene transcription, some NRs are also phosphorylated. Despite extensive investigations, primarily focusing on unique phosphorylation of amino acid residues in different NRs, the role of phosphorylation in the biological activity of NRs in vivo has not been firmly established. Recent studies on the phosphorylation of conserved phosphorylation motifs within the DNA- and ligand-binding domains confirmed has indicated the physiologically relevance of NR phosphorylation. This review focuses on estrogen and androgen receptors, and highlights the concept of phosphorylation as a drug target.
摘要：
核受体（NR）共同调节各种器官中的几种生物学功能。虽然NRs可以通过激活其标签基因的转录来表征，他们还有其他不同的角色。尽管大多数NRs是通过配体结合直接激活的，诱导导致基因转录的事件级联，一些NRs也被磷酸化。尽管进行了广泛的调查，主要关注不同NRs中氨基酸残基的独特磷酸化，磷酸化在NRs体内生物活性中的作用尚未得到证实。最近对DNA和配体结合域内保守磷酸化基序磷酸化的研究证实了NR磷酸化的生理相关性。本文就雌激素和雄激素受体,并强调了磷酸化作为药物靶标的概念。
