skip to main content
Language:
Search Limited to: Search Limited to: Resource type Show Results with: Show Results with: Index

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]

Full text available

Citations Cited by
  • 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 . The optimized structure represents a highly S1P -selective and efficacious agonist: S1P /S1P , S1P /S1P , S1P /S1P > 10,000-fold, S1P /S1P > 600-fold, while EC (S1P ) <0.2 nM. In vivo experiments are consistent with S1P 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 . The optimized structure represents a highly S1P -selective and efficacious agonist: S1P /S1P , S1P /S1P , S1P /S1P > 10,000-fold, S1P /S1P > 600-fold, while EC (S1P ) <0.2 nM. In vivo experiments are consistent with S1P 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 ; E-ISSN: 1464-3405 ; DOI: 10.1016/j.bmcl.2006.04.064
  • Subjects: Sphingosine-1-Phosphate ; S1p ; Immunosuppressant ; Lymphocyte-Lowering ; Agonist ; Heteropentalene ; Medicine ; Chemistry ; Anatomy & Physiology
  • Language: English

Searching Remote Databases, Please Wait