摘要
G蛋白偶联受体55(GPR55)在1999年被确定。由于其内源性,植物提取以及作用于GPR55的合成大麻素配体,它被作为内源性大麻素系统的一个新成员。然而,细胞下游信号通路与GPR55活化的相关复杂性延缓了GPR55选择性配体的发现。几年前,高通量的制药公司和政府机构的图书馆才允许识别选择性激动剂和拮抗剂受体。此后,几个GPR55调制器支架陆陆续续被报道。与之相关联的GPR55已在多种生理和病理过程中被揭示,如其在炎症反应中的作用,神经病理性疼痛、骨生理学、糖尿病和癌症。考虑GPR55作为一种新的有潜力的治疗靶点,很明显需要新的有选择性和潜力的GPR55调节器。本文将针对当前GPR55配体结构更新的状况进行叙述。
关键词: 激动剂;拮抗剂;大麻;内源性大麻素;GPCR;GPR55;结构。
Current Medicinal Chemistry
Title:Advances Towards The Discovery of GPR55 Ligands
Volume: 23 Issue: 20
Author(s): Paula Morales and Nadine Jagerovic
Affiliation:
关键词: 激动剂;拮抗剂;大麻;内源性大麻素;GPCR;GPR55;结构。
摘要: The G-protein-coupled receptor 55 (GPR55) was identified in 1999. It was proposed as a novel member of the endocannabinoid system due to the fact that some endogenous, plant-derived and synthetic cannabinoid ligands act on GPR55. However, the complexity of the cellular downstream signaling pathways related to GPR55 activation delayed the discovery of selective GPR55 ligands. It was only a few years ago that the high throughput screening of libraries of pharmaceutical companies and governmental organizations allowed to identify selective GPR55 agonists and antagonists. Since then, several GPR55 modulator scaffolds have been reported. The relevance of GPR55 has been explored in diverse physiological and pathological processes revealing its role in inflammation, neuropathic pain, bone physiology, diabetes and cancer. Considering GPR55 as a new promising therapeutic target, there is a clear need for new selective and potent GPR55 modulators. This review will address a current structural update of GPR55 ligands.
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Cite this article as:
Paula Morales and Nadine Jagerovic , Advances Towards The Discovery of GPR55 Ligands, Current Medicinal Chemistry 2016; 23 (20) . https://dx.doi.org/10.2174/0929867323666160425113836
DOI https://dx.doi.org/10.2174/0929867323666160425113836 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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