天然产物作为核受体和代谢传感器 LXR、FXR 和 RXR 的调节剂。

Natural products as modulators of the nuclear receptors and metabolic sensors LXR, FXR and RXR.

机构信息

University of Vienna, Department of Pharmacognosy, Althanstrasse 14, 1090 Vienna, Austria.

出版信息

Biotechnol Adv. 2018 Nov 1;36(6):1657-1698. doi: 10.1016/j.biotechadv.2018.03.003. Epub 2018 Mar 13.

DOI:10.1016/j.biotechadv.2018.03.003

Abstract

Nuclear receptors (NRs) represent attractive targets for the treatment of metabolic syndrome-related diseases. In addition, natural products are an interesting pool of potential ligands since they have been refined under evolutionary pressure to interact with proteins or other biological targets. This review aims to briefly summarize current basic knowledge regarding the liver X (LXR) and farnesoid X receptors (FXR) that form permissive heterodimers with retinoid X receptors (RXR). Natural product-based ligands for these receptors are summarized and the potential of LXR, FXR and RXR as targets in precision medicine is discussed.

摘要

核受体 (NRs) 是治疗代谢综合征相关疾病的有吸引力的靶标。此外，天然产物是一个有趣的潜在配体库，因为它们在进化压力下经过了精炼，以与蛋白质或其他生物靶标相互作用。本综述旨在简要总结目前关于肝 X (LXR) 和法尼醇 X 受体 (FXR) 的基本知识，它们与视黄醇 X 受体 (RXR) 形成允许的异二聚体。总结了这些受体的基于天然产物的配体，并讨论了 LXR、FXR 和 RXR 作为精准医学靶点的潜力。