The DOI matches its Crossref record; 1 of the 1 references it cites were found in a registry or an index.
S1P1-Selective In Vivo-Active Agonists from High- Throughput Screening: Off-the-Shelf Chemical Probes of Receptor Interactions, Signaling, and Fate
Open accessAbstract
The essential role of the sphingosine 1-phosphate (S1P) receptor S1P(1) in regulating lymphocyte trafficking was demonstrated with the S1P(1)-selective nanomolar agonist, SEW2871. Despite its lack of charged headgroup, the tetraaromatic compound SEW2871 binds and activates S1P(1) through a combination of hydrophobic and ion-dipole interactions. Both S1P and SEW2871 activated ERK, Akt, and Rac signaling pathways and induced S1P(1) internalization and recycling, unlike FTY720-phosphate, which induces receptor degradation. Agonism with receptor recycling is sufficient for alteration of lymphocyte trafficking by S1P and SEW2871. S1P(1) modeling and mutagenesis studies revealed that residues binding the S1P headgroup are required for kinase activation by both S1P and SEW2871. Therefore, SEW2871 recapitulates the action of S1P in all the signaling pathways examined and overlaps in interactions with key headgroup binding receptor residues, presumably replacing salt-bridge interactions with ion-dipole interactions.
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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
Cited by
“Inside-Out” Signaling of Sphingosine-1-Phosphate: Therapeutic Targets
Takabe, K., Paugh, S. W., Milstien, S., & Spiegel, S. (2008) · Pharmacological Reviews · doi:10.1124/pr.107.07113 · Cited by 718
Massberg, S., Schaerli, P., Knezevic-Maramica, I., Köllnberger, M., Tubo, N., Moseman, E. A., Huff, I. V., Junt, T., Wagers, A. J., Mazo, I. B., et al. (2007) · Cell · doi:10.1016/j.cell.2007.09.047 · Cited by 696
Teijaro, J. R., Walsh, K. B., Cahalan, S., Fremgen, D. M., Roberts, E., Scott, F., Martinborough, E., Peach, R., Oldstone, M. B. A., & Rosen, H. (2011) · Cell · doi:10.1016/j.cell.2011.08.015 · Cited by 688
Self-citationCrystal 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
Self-citationAn 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
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Metadata
- Authors
- Jo, E., Sanna, M. G., Gonzalez-Cabrera, P. J., Thangada, S., Tigyi, G., Osborne, D. A., Hla, T., Parrill, A. L., & Rosen, H.
- Venue
- Chemistry & Biology
- Publisher
- Elsevier BV
- Published
- 2005-06
- Volume
- 12
- Issue
- 6
- Pages
- 703-715
- ISSN
- 1074-5521 (ISSN-L)
- OpenAlex
- W1991624475
- Cited by
- 240
- References
- 1
- FWCI
- 7.61
- Type
- journal article
- Language
- en
- Open access
- bronze
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- Jo, E., Sanna, M. G., Gonzalez-Cabrera, P. J., Thangada, S., Tigyi, G., Osborne, D. A., Hla, T., Parrill, A. L., & Rosen, H. (2005). S1P1-Selective In Vivo-Active Agonists from High- Throughput Screening: Off-the-Shelf Chemical Probes of Receptor Interactions, Signaling, and Fate. Chemistry & Biology. https://doi.org/10.1016/j.chembiol.2005.04.019
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