Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720

JJ Hale, W Neway, SG Mills, R Hajdu… - Bioorganic & medicinal …, 2004 - Elsevier
JJ Hale, W Neway, SG Mills, R Hajdu, CA Keohane, M Rosenbach, J Milligan, GJ Shei…
Bioorganic & medicinal chemistry letters, 2004Elsevier
Alteration in lymphocyte trafficking and prevention of graft rejection in rodents observed on
exposure to FTY720 (1) or its corresponding phosphate ester 2 can be induced by the
systemic administration of potent sphingosine-1-phosphate receptor agonists exemplified by
19. The similar S1P receptor profiles of 2 and 19 coupled with their comparable potency in
vivo supports a connection between S1P receptor agonism and immunosuppressive
efficacy.
Alteration in lymphocyte trafficking and prevention of graft rejection in rodents observed on exposure to FTY720 (1) or its corresponding phosphate ester 2 can be induced by the systemic administration of potent sphingosine-1-phosphate receptor agonists exemplified by 19. The similar S1P receptor profiles of 2 and 19 coupled with their comparable potency in vivo supports a connection between S1P receptor agonism and immunosuppressive efficacy.
Elsevier