Biochem Biophys Res Commun. 2017 Jul 8. pii: S0006-291X(17)31380-3. doi: 10.1016/j.bbrc.2017.07.038.
[Epub ahead of print]
Abstract
Interest in lipoamino acids as endogenous modulators of G-protein coupled receptors has escalated due to their involvement in a variety of physiologic processes. In particular, a role for these amino acid conjugates has emerged in the endocannabinoid system. The study presented herein investigated the effects of N-arachidonoyl glycine (NAGly) on a candidate endocannabinoid receptor, GPR55. Our novel findings reveal that NAGly induces concentration dependent increases in calcium mobilization and mitogen-activated protein kinase activities in HAGPR55/CHO cells. These increases were attenuated by the selective GPR55 antagonist ML193 (N-[4-[[(3,4-Dimethyl-5-isoxazolyl)amino]sulfonyl]phenyl]-6,8-dimethyl-2-(2-pyridinyl)-4-quinolinecarboxamide), supporting receptor mediated signaling. To our knowledge this is the first report identifying GPR55 as a target of the endogenous lipoamino acid, NAGly.
Copyright © 2017. Published by Elsevier Inc.
KEYWORDS:
Bafilomycin A1 (PubChem CID 6436223); Calcium; GPR55; Inositol-3-phosphate receptor; ML193, (N-[4-[[(3,4-Dimethyl-5-isoxazolyl)amino]sulfonyl]phenyl]-6,8-dimethyl-2-(2-pyridinyl)-4-quinolinecarboxamide) (PubChem CID1261822); Mitogen activated protein kinase; N-arachidonyl glycine; N-arachidonyl glycine (PubChem CID 5283389); Xestopongin C (PubChem CID 9846431); ryanodine (PubChem CID 11317883)
- PMID: 28698140
- DOI: 10.1016/j.bbrc.2017.07.038
