Kirsz Katarzyna, Zięba Dorota A
Pracownia Biotechnologii i Genomiki, Katedra Hodowli Trzody Chlewnej i Małych Przeżuwaczy Wydziału Hodowli i Biologii Zwierząt UR w Krakowie.
Postepy Hig Med Dosw (Online). 2012 Apr 16;66:196-203. doi: 10.5604/17322693.991448.
Neuromedin U (NMU) is a structurally highly conserved neuropeptide and has been paired with the G-protein-coupled receptors (GPCRs) NMUR1 and NMUR2, which were formerly classified in the orphan receptor family. Activation of the G protein Gq/11 subunit causes a pertussis toxin (PTX)-insensitive activation of both phospholipase C and mitogen-activated protein kinase (MAP), and activation of the Go subunit causes a PTX-sensitive inhibition of adenyl cyclase. Additionally, NMU selectively inhibits L-type high-voltage-gated Ca2+ channels in mouse hippocampus, as well as low-voltage-activated T-type Ca2+ channels in mouse dorsal root ganglia (DRG). NMU peptide and its receptors are predominantly expressed in the gastrointestinal tract and specific structures within the brain, reflecting its major role in the regulation of energy homeostasis. A novel neuropeptide, neuromedin S (NMS), is structurally related to NMU. They share a C-terminal core structure and both have been implicated in the regulation of food intake, as well as the circadian rhythms. The acute anorectic and weight-reducing effects of NMU and NMS are mediated by NMUR2. This suggests that NMUR2-selective agonists may be useful for the treatment of obesity.
神经介素U（NMU）是一种结构上高度保守的神经肽，与G蛋白偶联受体（GPCRs）NMUR1和NMUR2相结合，这两种受体以前被归类于孤儿受体家族。G蛋白Gq/11亚基的激活会导致磷脂酶C和丝裂原活化蛋白激酶（MAP）的百日咳毒素（PTX）不敏感激活，而Go亚基的激活会导致PTX敏感的腺苷酸环化酶抑制。此外，NMU选择性抑制小鼠海马体中的L型高电压门控Ca2+通道，以及小鼠背根神经节（DRG）中的低电压激活T型Ca2+通道。NMU肽及其受体主要在胃肠道和脑内的特定结构中表达，这反映了其在能量稳态调节中的主要作用。一种新的神经肽，神经介素S（NMS），在结构上与NMU相关。它们共享一个C端核心结构，并且都与食物摄入调节以及昼夜节律有关。NMU和NMS的急性厌食和减肥作用是由NMUR2介导的。这表明NMUR2选择性激动剂可能对肥胖症的治疗有用。
