Modulators of the Sphingosine 1-phosphate receptor 1
The Sphingosine 1-phosphate receptor (S1P-R) signaling system has proven to be of biological and medical importance in autoimmune settings. S1P1-R is a validated drug target for multiple sclerosis (MS) for which FTY720 (Fingolimod), a S1P1,3–5-R pan-agonist, was recently approved as the first orally...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2013-12, Vol.23 (23), p.6377-6389 |
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| container_issue | 23 |
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| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 23 |
| creator | Urbano, Mariangela Guerrero, Miguel Rosen, Hugh Roberts, Edward |
| description | The Sphingosine 1-phosphate receptor (S1P-R) signaling system has proven to be of biological and medical importance in autoimmune settings. S1P1-R is a validated drug target for multiple sclerosis (MS) for which FTY720 (Fingolimod), a S1P1,3–5-R pan-agonist, was recently approved as the first orally active drug for the treatment of relapsing-remitting MS. Transient bradycardia and long half-life are the FTY720 critical pitfalls. This review provides the latest advances on next-generation S1P1-R modulators from 2012 up to date, with an overview of the chemical structures, structure–activity relationships, and relevant biological and clinical properties. |
| doi_str_mv | 10.1016/j.bmcl.2013.09.058 |
| format | Article |
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S1P1-R is a validated drug target for multiple sclerosis (MS) for which FTY720 (Fingolimod), a S1P1,3–5-R pan-agonist, was recently approved as the first orally active drug for the treatment of relapsing-remitting MS. Transient bradycardia and long half-life are the FTY720 critical pitfalls. 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| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2013-12, Vol.23 (23), p.6377-6389 |
| issn | 0960-894X 1464-3405 |
| language | eng |
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| source | MEDLINE; ScienceDirect Journals (5 years ago - present) |
| subjects | Animals Autoimmune diseases Bradycardia drug therapy drugs FTY720 half life Humans Immunosuppressive Agents - chemistry Immunosuppressive Agents - pharmacology Receptors, Lysosphingolipid - chemistry Receptors, Lysosphingolipid - metabolism S1P1-R agonists S1P1-R antagonists sclerosis Signal Transduction sphingosine Structure-Activity Relationship structure-activity relationships |
| title | Modulators of the Sphingosine 1-phosphate receptor 1 |
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