The DOI matches its Crossref record; 24 of the 24 references it cites were found in a registry or an index.
Sphingosine 1-Phosphate Analogs as Receptor Antagonists
Open accessAbstract
Sphingosine 1-phosphate (S1P) is a lysophospholipid mediator that evokes a variety of cell and tissue responses via a set of cell surface receptors. The recent development of S1P receptor agonists, led by the immunomodulatory pro-drug FTY720, has revealed that S1P signaling is an important regulator of lymphocyte trafficking. With the twin goals of understanding structure-activity relationships of S1P ligands and developing tool compounds to explore S1P biology, we synthesized and tested numerous S1P analogs. We report herein that a subset of our aryl amide-containing compounds are antagonists at the S1P(1) and S1P(3) receptors. The lead compound in series, VPC23019, was found in broken cell and whole cell assays to behave as a competitive antagonist at the S1P(1) and S1P(3) receptors. The structure-activity relationship of this series is steep; for example, a slight modification of the lead compound resulted in VPC25239, which was one log order more potent at the S1P(3) receptor. These new chemical entities will enable further understanding of S1P signaling and provide leads for further S1P receptor antagonist development.
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Cites
Lymphocyte egress from thymus and peripheral lymphoid organs is dependent on S1P receptor 1
Matloubian, M., Lo, C. G., Cinamon, G., Lesneski, M. J., Xu, Y., Brinkmann, V., Allende, M. L., Proia, R. L., & Cyster, J. G. (2004) · Nature · doi:10.1038/nature02284 · Cited by 2,581
Alteration of Lymphocyte Trafficking by Sphingosine-1-Phosphate Receptor Agonists
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The Immune Modulator FTY720 Targets Sphingosine 1-Phosphate Receptors
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Self-citationSphingosine-1-Phosphate as a Ligand for the G Protein-Coupled Receptor EDG-1
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The immunosuppressant FTY720 down‐regulates sphingosine 1‐phosphate G protein‐coupled receptors
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Characterization of a Novel Sphingosine 1-Phosphate Receptor, Edg-8
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Self-citation
Cited by
Sphingosine 1-phosphate and cancer
Pyne, N. J., & Pyne, S. (2010) · Nature Reviews Cancer · doi:10.1038/nrc2875 · Cited by 852
“Inside-Out” Signaling of Sphingosine-1-Phosphate: Therapeutic Targets
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Crystal Structure of a Lipid G Protein–Coupled Receptor
Hanson, M. A., Roth, C. B., Jo, E., Griffith, M. T., Scott, F. L., Reinhart, G., Desale, H., Clemons, B., Cahalan, S. M., Schuerer, S. C., et al. (2012) · Science · doi:10.1126/science.1215904 · Cited by 666
An update on the biology of sphingosine 1-phosphate receptors
Blaho, V. A., & Hla, T. (2014) · Journal of Lipid Research · doi:10.1194/jlr.r046300 · Cited by 516
Targeting the sphingosine-1-phosphate axis in cancer, inflammation and beyond
Kunkel, G. T., Maceyka, M., Milstien, S., & Spiegel, S. (2013) · Nature Reviews Drug Discovery · doi:10.1038/nrd4099 · Cited by 434
Metadata
- Authors
- Davis, M. D., Clemens, J. J., Macdonald, T. L., & Lynch, K. R.
- Venue
- Journal of Biological Chemistry
- Publisher
- Elsevier BV
- Published
- 2005-03
- Volume
- 280
- Issue
- 11
- Pages
- 9833-9841
- ISSN
- 0021-9258 (ISSN-L)
- OpenAlex
- W2047174762
- Cited by
- 269
- References
- 24
- FWCI
- 5.79
- Type
- journal article
- Language
- en
- Open access
- hybrid
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