The DOI matches its Crossref record; 58 of the 58 references it cites were found in a registry or an index.
Lipid G Protein-coupled Receptor Ligand Identification Using β-Arrestin PathHunter™ Assay
Open accessAbstract
A growing number of orphan G-protein-coupled receptors (GPCRs) have been reported to be activated by lipid ligands, such as lysophosphatidic acid, sphingosine 1-phosphate (S1P), and cannabinoids, for which there are already well established receptors. These new ligand claims are controversial due to either lack of independent confirmations or conflicting reports. We used the beta-arrestin PathHunter assay system, a newly developed, generic GPCR assay format that measures beta-arrestin binding to GPCRs, to evaluate lipid receptor and ligand pairing. This assay eliminates interference from endogenous receptors on the parental cells because it measures a signal that is specifically generated by the tagged receptor and is immediately downstream of receptor activation. We screened a large number of newly "deorphaned" receptors (GPR23, GPR92, GPR55, G2A, GPR18, GPR3, GPR6, GPR12, and GPR63) and control receptors against a collection of approximately 400 lipid molecules to try to identify the receptor ligand in an unbiased fashion. GPR92 was confirmed to be a lysophosphatidic acid receptor with weaker responses to farnesyl pyrophosphate and geranylgeranyl diphosphate. The putative cannabinoid receptor GPR55 responded strongly to AM251, rimonabant, and lysophosphatidylinositol but only very weakly to endocannabinoids. G2A receptor was confirmed to be an oxidized free fatty acid receptor. In addition, we discovered that 3,3'-diindolylmethane, a dietary molecule from cruciferous vegetables, which has known anti-cancer properties, to be a CB(2) receptor partial agonist, with binding affinity around 1 microm. The anti-inflammatory effect of 3,3'-diindolylmethane in RAW264.7 cells was shown to be partially mediated by CB(2).
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Cites
1 retracted
Lysophosphatidylcholine as a Ligand for the Immunoregulatory Receptor G2A
Kabarowski, J. H. S., Zhu, K., Le, L. Q., Witte, O. N., & Xu, Y. (2001) · Science · doi:10.1126/science.1061781 · Cited by 332
RetractedBrown, A. J., Goldsworthy, S. M., Barnes, A. A., Eilert, M. M., Tcheang, L., Daniels, D., Muir, A. I., Wigglesworth, M. J., Kinghorn, I., Fraser, N. J., et al. (2003) · Journal of Biological Chemistry · doi:10.1074/jbc.m211609200 · Cited by 2,409
Oxidized LDL Regulates Macrophage Gene Expression through Ligand Activation of PPARγ
Nagy, L., Tontonoz, P., Alvarez, J. G. A., Chen, H., & Evans, R. M. (1998) · Cell · doi:10.1016/s0092-8674(00)81574-3 · Cited by 1,860
The orphan receptor GPR55 is a novel cannabinoid receptor
Ryberg, E., Larsson, N., Sjögren, S., Hjorth, S., Hermansson, N., Leonova, J., Elebring, T., Nilsson, K., Drmota, T., & Greasley, P. J. (2007) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0707460 · Cited by 1,568
The Orphan G Protein-coupled Receptor GPR40 Is Activated by Medium and Long Chain Fatty Acids
Briscoe, C. P., Tadayyon, M., Andrews, J. L., Benson, W. G., Chambers, J. K., Eilert, M. M., Ellis, C., Elshourbagy, N. A., Goetz, A. S., Minnick, D. T., et al. (2003) · Journal of Biological Chemistry · doi:10.1074/jbc.m211495200 · Cited by 1,104
GPR55 is a cannabinoid receptor that increases intracellular calcium and inhibits M current
Lauckner, J. E., Jensen, J. B., Chen, H.-Y., Lu, H.-C., Hille, B., & Mackie, K. (2008) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0711278105 · Cited by 712
Cannabinoids: potential anticancer agents
Guzmán, M. (2003) · Nature Reviews Cancer · doi:10.1038/nrc1188 · Cited by 703
Bjeldanes, L. F., Kim, J. Y., Grose, K. R., Bartholomew, J. C., & Bradfield, C. A. (1991) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.88.21.9543 · Cited by 588
Noguchi, K., Ishii, S., & Shimizu, T. (2003) · Journal of Biological Chemistry · doi:10.1074/jbc.m302648200 · Cited by 557
The cannabinoid system and immune modulation
Klein, T. W., Newton, C., Larsen, K., Lu, L., Perkins, I., Nong, L., & Friedman, H. (2003) · Journal of Leukocyte Biology · doi:10.1189/jlb.0303101 · Cited by 524
Cited by
Pertwee, R. G., Howlett, A. C., Abood, M. E., Alexander, S. P. H., Di Marzo, V., Elphick, M. R., Greasley, P. J., Hansen, H. S., Kunos, G., Mackie, K., et al. (2010) · Pharmacological Reviews · doi:10.1124/pr.110.003004 · Cited by 1,605
Omega‐3 polyunsaturated fatty acids and inflammatory processes: nutrition or pharmacology?
Calder, P. C. (2013) · British Journal of Clinical Pharmacology · doi:10.1111/j.1365-2125.2012.04374.x · Cited by 1,347
Molecular Targets of the Phytocannabinoids: A Complex Picture
Morales, P., Hurst, D. P., & Reggio, P. H. (2017) · Progress in the Chemistry of Organic Natural Products · doi:10.1007/978-3-319-45541-9_4 · Cited by 454
Receptors and Channels Targeted by Synthetic Cannabinoid Receptor Agonists and Antagonists
Pertwee, R. (2010) · Current Medicinal Chemistry · doi:10.2174/092986710790980050 · Cited by 335
Yamashita, A., Hayashi, Y., Nemoto-Sasaki, Y., Ito, M., Oka, S., Tanikawa, T., Waku, K., & Sugiura, T. (2014) · Progress in Lipid Research · doi:10.1016/j.plipres.2013.10.001 · Cited by 268
Metadata
- Authors
- Yin, H., Chu, A., Li, W., Wang, B., Shelton, F., Otero, F., Nguyen, D. G., Caldwell, J. S., & Chen, Y. A.
- Venue
- Journal of Biological Chemistry
- Publisher
- Elsevier BV
- Published
- 2009-05
- Volume
- 284
- Issue
- 18
- Pages
- 12328-12338
- ISSN
- 0021-9258 (ISSN-L)
- OpenAlex
- W2072840386
- Cited by
- 311
- References
- 58
- FWCI
- 10.92
- Type
- journal article
- Language
- en
- Open access
- hybrid
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- Yin, H., Chu, A., Li, W., Wang, B., Shelton, F., Otero, F., Nguyen, D. G., Caldwell, J. S., & Chen, Y. A. (2009). Lipid G Protein-coupled Receptor Ligand Identification Using β-Arrestin PathHunter™ Assay. Journal of Biological Chemistry. https://doi.org/10.1074/jbc.m806516200
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