Title:Neuromedin U and Structural Analogs: An Overview of their Structure, Function and Selectivity
Volume: 27
Issue: 39
关键词:
Neuromedin U,Neuromedin U受体1,Neuromedin U受体2,激动剂,拮抗剂,类似物,拟肽。
摘要: 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.