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Highly selective and potent agonists of sphingosine-1-phosphate 1 (S1P 1) receptor

Vachal, Petr ; Toth, Leslie M. ; Hale, Jeffrey J. ; Yan, Lin ; Mills, Sander G. ; Chrebet, Gary L. ; Koehane, Carol A. ; Hajdu, Richard ; Milligan, James A. ; Rosenbach, Mark J. ; Mandala, Suzanne

Bioorganic & Medicinal Chemistry Letters, 2006, Vol.16(14), pp.3684-3687 [Peer Reviewed Journal]

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  • Title:
    Highly selective and potent agonists of sphingosine-1-phosphate 1 (S1P 1) receptor
  • Author: Vachal, Petr ; Toth, Leslie M. ; Hale, Jeffrey J. ; Yan, Lin ; Mills, Sander G. ; Chrebet, Gary L. ; Koehane, Carol A. ; Hajdu, Richard ; Milligan, James A. ; Rosenbach, Mark J. ; Mandala, Suzanne
  • Description: Novel series of sphingosine-1-phosphate (S1P) receptor agonists were developed through a systematic SAR aimed to achieve high selectivity for a single member of the S1P family of receptors, S1P 1. The optimized structure represents a highly S1P 1-selective and efficacious agonist: S1P 1/S1P 2, S1P 1/S1P 3, S1P 1/S1P 4 > 10,000-fold, S1P 1/S1P 5 > 600-fold, while EC 50 (S1P 1) <0.2 nM. In vivo experiments are consistent with S1P 1 receptor agonism alone being sufficient for achieving desired lymphocyte-lowering effect. Novel series of sphingosine-1-phosphate (S1P) receptor agonists were developed through a systematic SAR aimed to achieve high selectivity for a single member of the S1P family of receptors, S1P 1. The optimized structure represents a highly S1P 1-selective and efficacious agonist: S1P 1/S1P 2, S1P 1/S1P 3, S1P 1/S1P 4 > 10,000-fold, S1P 1/S1P 5 > 600-fold, while EC 50 (S1P 1) <0.2 nM. In vivo experiments are consistent with S1P 1 receptor agonism alone being sufficient for achieving desired lymphocyte-lowering effect.
  • Is Part Of: Bioorganic & Medicinal Chemistry Letters, 2006, Vol.16(14), pp.3684-3687
  • Identifier: ISSN: 0960-894X ; DOI: 10.1016/j.bmcl.2006.04.064
  • Subjects: Sphingosine-1-Phosphate ; S1p ; Immunosuppressant ; Lymphocyte-Lowering ; Agonist ; Heteropentalene
  • Language: English

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