Institute of Pharmaceutical Chemistry, Goethe University, Frankfurt, Max-von-Laue-Strausse 9, D-60438 Frankfurt am Main, Germany.
Future Med Chem. 2012 May;4(8):1015-36. doi: 10.4155/fmc.12.47.
The nuclear receptor farnesoid X receptor (FXR) has emerged as a highly promising target in preclinical development in recent years. A significant amount of research has been conducted and, although none has reached clinical use, many synthetic ligands of FXR have been described. This review outlines the available knowledge regarding the medicinal chemistry and SAR of these FXR ligands, and discusses the molecular interactions of the compounds with the FXR ligand-binding domain by interpreting the existing co-crystal structures.
核受体法尼醇 X 受体（FXR）近年来在临床前开发中成为一个极具前景的靶点。已经进行了大量的研究，尽管没有一种达到临床应用，但已经描述了许多 FXR 的合成配体。这篇综述概述了这些 FXR 配体的药物化学和 SAR 的现有知识，并通过解释现有的共晶结构讨论了化合物与 FXR 配体结合域的分子相互作用。
