Advances Towards The Discovery of GPR55 Ligands

Author(s): Paula Morales, Nadine Jagerovic

Journal Name: Current Medicinal Chemistry

Volume 23 , Issue 20 , 2016

  Journal Home
Translate in Chinese
Become EABM
Become Reviewer
Call for Editor


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.

Keywords: Agonist, Antagonist, Cannabinoid, Endocannabinoid, GPCR, GPR55, Structure.

Rights & PermissionsPrintExport Cite as

Article Details

Year: 2016
Page: [2087 - 2100]
Pages: 14
DOI: 10.2174/0929867323666160425113836
Price: $65

Article Metrics

PDF: 123