2. Academic Validation
  3. Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720

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

  • Bioorg Med Chem Lett. 2004 Jun 21;14(12):3351-5. doi: 10.1016/j.bmcl.2004.02.106.
Jeffrey J Hale 1,  William Neway,  Sander G Mills,  Richard Hajdu,  Carol Ann Keohane,  Mark Rosenbach,  James Milligan,  Gan-Ju Shei,  Gary Chrebet,  James Bergstrom,  Deborah Card,  Gloria C Koo,  Sam L Koprak,  Jesse J Jackson,  Hugh Rosen,  Suzanne Mandala
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. jeffrey_hale@merck.com
PMID: 15149705 DOI: 10.1016/j.bmcl.2004.02.106
Abstract

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.

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