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International Journal of Molecular Sciences, ISSN 1422-0067, 07/2019, Volume 20, Issue 13, p. 3232
A decrease in heart rate (HR) is a well-established first-dose effect of sphingosine-1-phosphate subtype 1 receptor (S1P1R) modulators. For compounds with a... 
S1P1 receptor modulators | pharmacokinetics | first-dose effect
Journal Article
European Journal of Medicinal Chemistry, ISSN 0223-5234, 10/2014, Volume 85, pp. 1 - 15
We have discovered a series of triazole/oxazole-containing 2-substituted 2-aminopropane-1,3-diol derivatives as potent and selective S1P agonists (prodrugs)... 
Immunomodulator | Prodrug | S1P1 agonist | Pharmacophore | Lymphocyte
Journal Article
Biochemical and Biophysical Research Communications, ISSN 0006-291X, 09/2017, Volume 490, Issue 4, pp. 1274 - 1281
Enhanced turnover of subchondral trabecular bone is a hallmark of rheumatoid arthritis (RA) and it results from an imbalance between bone resorption and bone... 
SN50 | Temporomandibular joint | Fas | S1P1 | Osteoclast | S1P | Index Medicus
Journal Article
ACS Medicinal Chemistry Letters, ISSN 1948-5875, 03/2016, Volume 7, Issue 3, pp. 283 - 288
Clinical validation of S1P receptor modulation therapy was achieved with the approval of fingolimod (Gilenya, 1) as the first oral therapy for relapsing... 
GPCR | S1P1 | biased signaling | S1P3
Journal Article
Biological and Pharmaceutical Bulletin, ISSN 0918-6158, 2018
Psoriasis is a chronic inflammatory skin disease characterized by red, scaly and raised plaques. Thus far, T-cell infiltration is one of the most prominent... 
Psoriasis | sphingolipid sphingosine-1-phosphate | animal model | Syl930 | S1P1 modulator
Journal Article
International Immunology, ISSN 0953-8178, 2014, Volume 26, Issue 5, pp. 245 - 255
Journal Article
Molecular Immunology, ISSN 0161-5890, 11/2008, Volume 46, Issue 1, pp. 166 - 171
The CXC chemokine receptor 4 (CXCR4) and its ligand stromal derived factor 1 (SDF-1) regulate egress and homing of hematopoietic stem cells. Activation of... 
Homing | SDF-1 | CXCR4 | HSC | S1P1 | Migration
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 03/2017, Volume 27, Issue 6, pp. 1371 - 1378
Previously published S1P receptor modulator benzyl ether derivatives have shown potential as being viable therapeutics for the treatment of neurodegenerative... 
Sphingosine kinase | Enzymatic processing | Phosphoramidate | ProTide | S1P1 receptor agonist | Benzyl ether derivative | Index Medicus
Journal Article
Oncotarget, ISSN 1949-2553, 2017, Volume 8, Issue 62, pp. 104704 - 104705
Journal Article
ACS medicinal chemistry letters, ISSN 1948-5875, 12/2014, Volume 5, Issue 12, pp. 1334 - 1339
S1P1 is a validated target for treatment of autoimmune disease, and functional antagonists with superior safety and pharmacokinetic properties are being sought... 
Journal Article
Histochemistry and cell biology, ISSN 0948-6143, 2/2009, Volume 131, Issue 2, pp. 239 - 249
Sphingosine-1-phosphate (S1P) receptor subtype 1 (S1P 1 ), a G-protein coupled receptor (GPCR), regulates many biological activities of endothelial cells... 
S1P | S1P1 | Endothelial cells
Journal Article
Journal of Neuroimmunology, ISSN 0165-5728, 11/2017, Volume 312, pp. 49 - 58
Journal Article
ACS Medicinal Chemistry Letters, ISSN 1948-5875, 02/2011, Volume 2, Issue 2, pp. 107 - 112
The optimization of a series of thiazolopyridine S1P1 agonists with limited activity at the S1P3 receptor is reported. These efforts resulted in the discovery... 
Sphingosine-1-phosphate receptor | S1P | inflammation | multiple sclerosis | lymphocyte
Journal Article
Drug Design, Development and Therapy, ISSN 1177-8881, 12/2016, Volume 11, pp. 123 - 131
Stipo Jurcevic,1 Pierre-Eric Juif,2 Colleen Hamid,3 Roseanna Greenlaw,3 Daniele D'Ambrosio,2 Jasper Dingemanse2 1Department of Biomedical Sciences, University... 
lymphocyte subsets | S1P1 receptor | CD45RA/CCR7 | multiple dose | ponesimod
Journal Article
Bioorganic and Medicinal Chemistry Letters, ISSN 0960-894X, 01/2012, Volume 22, Issue 1, pp. 628 - 633
An SAR campaign designed to increase polarity in the 'tail' region of benzothiazole 1 resulted in two series of structurally novel 5-and 6-substituted S1P... 
Lymphocyte reduction | G-protein coupled receptor | S1P1 | Physicochemical properties
Journal Article
ORGANIC PROCESS RESEARCH & DEVELOPMENT, ISSN 1083-6160, 02/2017, Volume 21, Issue 2, pp. 200 - 207
Journal Article
ACS Medicinal Chemistry Letters, ISSN 1948-5875, 02/2011, Volume 2, Issue 2, pp. 102 - 106
Optimization of a benzofuranyl S1P1 agonist lead compound (3) led to the discovery of... 
S1P1 | agonist | Sphingosine-1-phosphate receptor | inflammation | lymphocyte
Journal Article
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