如何调节FXR活性治疗代谢综合征

Janne Prawitt , Sandrine Caron , Bart Staels
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引用次数: 13

摘要

代谢综合征(MS)是一个在世界范围内普遍存在的公共卫生问题。除了生活方式干预外,开发针对多发性硬化症及其并发症(如心血管疾病(CVD)和2型糖尿病(T2D))的有效疗法是未来几十年的主要挑战。核受体farnesoid X受体(FXR)是一个潜在的药理学靶点,因为它具有广谱的功能,并且可能通过所谓的选择性胆汁酸受体调节剂(SBARM)以基因特异性的方式调节其活性。这篇综述将讨论FXR的许多与MS成分重叠的调节功能,以及调节FXR活性对MS治疗的潜在益处。
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How to modulate FXR activity to treat the Metabolic Syndrome

The Metabolic Syndrome (MS) represents a public health problem which takes epidemic proportions worldwide. In addition to life-style interventions the development of effective therapies for the MS and its complications such as cardiovascular disease (CVD) and type 2 diabetes (T2D) is a major challenge of the future decades. The nuclear receptor farnesoid X receptor (FXR) is a potential pharmacological target, because of its broad spectrum of functions and the possibility of modulating its activity in a gene-specific manner by the so-called selective bile acid receptor modulators (SBARM). This review will discuss the numerous regulatory functions of FXR that overlap with components of the MS and the potential benefit of modulating FXR activity for MS therapy.

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