Department of Pharmacological Sciences , Icahn School of Medicine at Mount Sinai , New York , New York 10029 , United States.
ACS Chem Neurosci. 2019 Apr 17;10(4):1884-1891. doi: 10.1021/acschemneuro.8b00559. Epub 2019 Feb 21.
Neuropeptides are chemical messengers that act to regulate a number of physiological processes, including feeding, reward, pain, and memory, among others. PEN is one of the most abundant hypothalamic neuropeptides; however, until recently, its target receptor remained unknown. In this Review, we summarize recent developments in research focusing on PEN and its receptor GPR83. We describe the studies leading to the deorphanization of GPR83 as the receptor for PEN. We also describe the signaling mediated by the PEN-GPR83 system, as well as the physiological roles in which PEN-GPR83 has been implicated. As studies have suggested a role for the PEN-GPR83 system in food intake and body weight regulation, as well as in drug addiction and reward disorders, a thorough understanding of this novel neuropeptide-receptor system will help identify novel therapeutic targets to treat pathophysiological conditions involving PEN-GPR83.
神经肽是一种化学信使，可调节包括进食、奖励、疼痛和记忆等多种生理过程。PEN 是最丰富的下丘脑神经肽之一；然而，直到最近，其靶受体仍然未知。在这篇综述中，我们总结了最近关于 PEN 和其受体 GPR83 的研究进展。我们描述了将 GPR83 作为 PEN 的受体进行去孤儿化的研究。我们还描述了 PEN-GPR83 系统介导的信号转导，以及 PEN-GPR83 所涉及的生理作用。由于研究表明 PEN-GPR83 系统在摄食和体重调节、药物成瘾和奖励障碍中起作用，因此深入了解这一新型神经肽-受体系统将有助于确定治疗涉及 PEN-GPR83 的病理生理状况的新的治疗靶点。
