Beyond Bile Acids: Targeting Farnesoid X Receptor (FXR) with Natural and Synthetic Ligands

被引：47

作者：

Carotti, Andrea ^{[1
]}

Marinozzi, Maura ^{[1
]}

Custodi, Chiara ^{[1
]}

Cerra, Bruno ^{[1
]}

Pellicciari, Roberto ^{[1
,2
]}

Gioiello, Antimo ^{[1
]}

Macchiarulo, Antonio ^{[1
]}

机构：

[1] Univ Perugia, Dipartimento Sci Farmaceut, I-06123 Perugia, Italy

[2] TES Pharma Srl, I-06073 Corciano, Perugia, Italy

来源：

CURRENT TOPICS IN MEDICINAL CHEMISTRY | 2014年 / 14卷 / 19期

关键词：

Bile acid homeostasis; Farnesoid X receptor; Natural ligands; Nuclear receptors; Synthetic ligands; SPONGE THEONELLA-SWINHOEI; CHOLESTEROL-RAISING FACTOR; ORPHAN NUCLEAR RECEPTOR; SALT EXPORT PUMP; MARINE SPONGE; BIOLOGICAL EVALUATION; ACTIVATED RECEPTOR; SULFATED POLYHYDROXYSTEROIDS; SCHISANDRA-GLAUCESCENS; CELL-PROLIFERATION;

D O I：

10.2174/1568026614666141112094058

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The modulation of FXR receptor remains an attractive area in drug discovery to develop novel therapeutic opportunities for liver and metabolic disorders. Despite the large variety of FXR ligands reported so far, only a very restricted number of agonists have entered in clinical settings. In this review article we provide the reader with an overview on the different classes of natural and synthetic ligands that have been developed by academic groups and pharmaceutical companies to target FXR. We discuss their structure-activity relationships, analyzing the binding modes that some of these compounds adopt to interact with the receptor.

引用

页码：2129 / 2142

页数：14

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