Journal
ACS CHEMICAL NEUROSCIENCE
Volume 10, Issue 1, Pages 716-727Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acschemneuro.8b00505
Keywords
Lysolipids; glycolipids; G-protein coupled receptor 55; homology model; structure-activity relationship; cannabinoid receptor related receptor
Funding
- Integrated Lipidology Program of RIKEN
- AMED-CREST Grant [JP18gm0910006]
- Ministry of Education, Culture, Sports, Science and Technology of Japan [16H06290, 16K08259, 17K14970]
- Mizutani Foundation for Glycoscience
- Grants-in-Aid for Scientific Research [16H06290, 16K08259, 17K14970] Funding Source: KAKEN
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G protein-coupled receptor 55 (GPR55) is highly expressed in brain and chemorepulsion peripheral nervous system. Originally deorphanized as a cannabinoid receptor, recently GPRS5 has been described as a lysophospholipid-responsive receptor, specifically toward lysophosphatidylinositol and lysophosphatidyl-beta-n-glucoside (LysoPtdGlc). To characterize lysolipid-GPR55 interaction, synthetic access to LysoPtdGlc and selected analogues was established utilizing a phosphorus(III)-based chemical approach. The biological activity of each synthetic lipid was assessed using a GPR55-dependent chemotropism assay in primary sensory neurons. Combined with molecular dynamics simulations the potential ligand entry port and binding pocket specifics are discussed. These results highlight the preference for gluco- over inositol- and galacto-configured headgroups.
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