Xu Tian-Rui, Yang Yang, Ward Richard, Gao Linghuan, Liu Ying
Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming, Yunnan 650500, China.
Cell Signal. 2013 Dec;25(12):2413-23. doi: 10.1016/j.cellsig.2013.07.025. Epub 2013 Aug 1.
The orexin peptides (orexin A, orexin B) and their receptors (orexin receptor type 1, orexin receptor type 2) are involved in multiple physiological processes such as the regulation of sleep/wakefulness state, energy homeostasis and reward seeking. A result of this has been the development of small-molecule orexin receptor antagonists as novel therapies for the treatment of insomnia and drug addiction. Increased levels of signaling via the orexin peptide/receptor system may protect against obesity, while somewhat unexpectedly, orexins acting at orexin receptors induce dramatic apoptosis resulting in the significant reduction of cell growth in various cancer cell lines. Meanwhile, the orexin peptide/receptor system is also involved in cardiovascular modulation, neuroendocrine and reproduction regulation. This review summarizes the latest developments in deciphering the biology of orexin signaling as well as efforts to manipulate orexin signaling pharmacologically.
食欲素肽（食欲素A、食欲素B）及其受体（1型食欲素受体、2型食欲素受体）参与多种生理过程，如睡眠/觉醒状态调节、能量稳态和奖赏寻求。由此产生的一个成果是，小分子食欲素受体拮抗剂已被开发为治疗失眠和药物成瘾的新型疗法。通过食欲素肽/受体系统增加的信号传导水平可能预防肥胖，而有些出乎意料的是，作用于食欲素受体的食欲素会诱导显著的细胞凋亡，导致各种癌细胞系中的细胞生长显著减少。同时，食欲素肽/受体系统也参与心血管调节、神经内分泌和生殖调节。本综述总结了解析食欲素信号生物学的最新进展以及通过药理学手段调控食欲素信号的研究成果。
