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Neuromedin U and Structural Analogs: an Overview of Their Structure, Function and Selectivity.
Current Medicinal Chemistry ( IF 4.1 ) Pub Date : 2020-11-30 , DOI: 10.2174/0929867326666190916143028
An De Prins 1 , Ann Van Eeckhaut 2 , Ilse Smolders 2 , Dirk Tourwé 1 , Steven Ballet 1
Affiliation  

The neuromedin U peptide sequence is highly conserved between various species. Neuromedin U is involved in a variety of physiological processes. It exerts its effects via two neuromedin U receptors, NMUR1 and NMUR2. These receptors are characterized by a distinct, yet complementary, tissue distribution with NMUR1 mostly found in the periphery, while NMUR2 is most abundant in the central nervous system. The capability of the neuropeptide to reduce food intake in rodents triggered the design and synthesis of a broad range of modified peptide ligands. The purpose of these ligands is to develop novel therapeutics which could be beneficial in the treatment of obesity and diabetes. Most compounds are derived either from the full-length neuromedin U sequence or are based on the truncated orthologs of this neuropeptide. Only a few non-peptidic ligands were developed. This review provides an overview on various neuromedin U analogs and mimetics that have been reported to date.



中文翻译:

Neuromedin U和结构类似物:其结构,功能和选择性概述。

Neuromedin U肽序列在各种物种之间高度保守。Neuromedin U参与多种生理过程。它通过两种神经介素U受体NMUR1和NMUR2发挥作用。这些受体的特征是与NMUR1明显不同但互补的组织分布,而NMUR1主要存在于外周,而NMUR2在中枢神经系统中含量最高。神经肽减少啮齿动物食物摄入的能力触发了多种修饰肽配体的设计和合成。这些配体的目的是开发对肥胖症和糖尿病的治疗可能有益的新型疗法。大多数化合物要么衍生自全长神经介素U序列,要么基于该神经肽的截短直向同源物。仅开发了一些非肽配体。这篇综述概述了迄今为止已报道的各种神经介素U类似物和模拟物。

更新日期:2020-11-25
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