5-HTR1E血清素受体的发现、结构和功能。
The discovery, structure, and function of 5-HTR1E serotonin receptor.
发表日期:2023 Sep 18
作者:
Vinay Kumar Sharma, Y Peng Loh
来源:
Protein & Cell
摘要:
血清素(5-羟色胺,5-HT)是一种独特的神经递质,可以通过激活13种不同的受体来调节各种生物过程。这些血清素受体根据其结构和功能分为七个不同的类。由于这些受体在各种组织和细胞类型中共同表达,并且共享相同的配体(5-HT),研究人员一直难以确定每个血清素受体的特定信号通路和生理作用。尽管有关这些受体的功能多样性的证据不断涌现,但仍有很多工作要做。5-HTR1E是属于G蛋白偶联受体(GPCRs)的5-HT1受体家族的成员。虽然自其发现以来已有三十年,但5-HTR1E仍然是最少被研究的血清素受体。与另一家族成员(5-HTR1F)非常相似且在小鼠或大鼠中不存在,这使得5-HTR1E成为一个难以研究的靶点。尽管存在这些挑战,但有关5-HTR1E在神经保护和癌症等疾病中的作用的最新发现已激发了许多研究人员对详细探索该受体的兴趣。在这里,我们提供了自1989年发现以来,关于5-HTR1E的第一篇评论。我们详细介绍了这个重要的血清素受体的结构和功能特点,并提出了在开发5-HTR1E作为药物靶点中未来的方向。视频摘要。© 2023. BioMed Central Ltd., Springer Nature的一部分。
Serotonin (5-hydroxytryptamine, 5-HT) is a unique neurotransmitter which can regulate various biological processes by activating thirteen different receptors. These serotonin receptors are divided into seven different classes based on their structure and functions. Since these receptors co-express in various tissue and cell types and share the same ligand (5-HT), it has been a challenge for the researchers to define specific pathway and separate physiological role for each of these serotonin receptors. Though the evidence of operational diversity of these receptors is continuously emerging, much work remains to be done. 5-HTR1E is a member of 5-HT1 receptor family which belongs to G-protein coupled receptors (GPCRs). Even after three decades since its discovery, 5-HTR1E remains the least explored serotonin receptor. Very high similarity with another family member (5-HTR1F) and its non-existence in mice or rats makes 5-HTR1E a difficult target to study. Despite these challenges, recent findings on the role of 5-HTR1E in neuroprotection and diseases such as cancer, have excited many researchers to explore this receptor in detail. Here, we provide the first review of 5-HTR1E, since its discovery in 1989 to 2023. We highlight the structural and functional characteristics of this important serotonin receptor in detail and propose future directions in developing 5-HTR1E as a drug target. Video Abstract.© 2023. BioMed Central Ltd., part of Springer Nature.