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Discovery of potent 3,5-diphenyl-1,2,4-oxadiazole sphingosine-1-phosphate-1 (S1P1) receptor agonists with exceptional selectivity against S1P2 and S1P3.
Li Z, Chen W, Hale JJ, Lynch CL, Mills SG, Hajdu R, Keohane CA, Rosenbach MJ, Milligan JA, Shei GJ, Chrebet G, Parent SA, Bergstrom J, Card D, Forrest M, Quackenbush EJ, Wickham LA, Vargas H, Evans RM, Rosen H, Mandala S. Li Z, et al. Among authors: mills sg. J Med Chem. 2005 Oct 6;48(20):6169-73. doi: 10.1021/jm0503244. J Med Chem. 2005. PMID: 16190743
Immune cell regulation and cardiovascular effects of sphingosine 1-phosphate receptor agonists in rodents are mediated via distinct receptor subtypes.
Forrest M, Sun SY, Hajdu R, Bergstrom J, Card D, Doherty G, Hale J, Keohane C, Meyers C, Milligan J, Mills S, Nomura N, Rosen H, Rosenbach M, Shei GJ, Singer II, Tian M, West S, White V, Xie J, Proia RL, Mandala S. Forrest M, et al. J Pharmacol Exp Ther. 2004 May;309(2):758-68. doi: 10.1124/jpet.103.062828. Epub 2004 Jan 27. J Pharmacol Exp Ther. 2004. PMID: 14747617
The discovery of 3-(N-alkyl)aminopropylphosphonic acids as potent S1P receptor agonists.
Hale JJ, Doherty G, Toth L, Li Z, Mills SG, Hajdu R, Ann Keohane C, Rosenbach M, Milligan J, Shei GJ, Chrebet G, Bergstrom J, Card D, Rosen H, Mandala S. Hale JJ, et al. Among authors: mills sg. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3495-9. doi: 10.1016/j.bmcl.2004.04.069. Bioorg Med Chem Lett. 2004. PMID: 15177460
Selecting against S1P3 enhances the acute cardiovascular tolerability of 3-(N-benzyl)aminopropylphosphonic acid S1P receptor agonists.
Hale JJ, Doherty G, Toth L, Mills SG, Hajdu R, Keohane CA, Rosenbach M, Milligan J, Shei GJ, Chrebet G, Bergstrom J, Card D, Forrest M, Sun SY, West S, Xie H, Nomura N, Rosen H, Mandala S. Hale JJ, et al. Among authors: mills sg. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3501-5. doi: 10.1016/j.bmcl.2004.04.070. Bioorg Med Chem Lett. 2004. PMID: 15177461
Design and synthesis of conformationally constrained 3-(N-alkylamino)propylphosphonic acids as potent agonists of sphingosine-1-phosphate (S1P) receptors.
Yan L, Hale JJ, Lynch CL, Budhu R, Gentry A, Mills SG, Hajdu R, Keohane CA, Rosenbach MJ, Milligan JA, Shei GJ, Chrebet G, Bergstrom J, Card D, Rosen H, Mandala SM. Yan L, et al. Among authors: mills sg. Bioorg Med Chem Lett. 2004 Oct 4;14(19):4861-6. doi: 10.1016/j.bmcl.2004.07.049. Bioorg Med Chem Lett. 2004. PMID: 15341940
A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists.
Hale JJ, Lynch CL, Neway W, Mills SG, Hajdu R, Keohane CA, Rosenbach MJ, Milligan JA, Shei GJ, Parent SA, Chrebet G, Bergstrom J, Card D, Ferrer M, Hodder P, Strulovici B, Rosen H, Mandala S. Hale JJ, et al. Among authors: mills sg. J Med Chem. 2004 Dec 30;47(27):6662-5. doi: 10.1021/jm0492507. J Med Chem. 2004. PMID: 15615513
2,5-Disubstituted pyrrolidine carboxylates as potent, orally active sphingosine-1-phosphate (S1P) receptor agonists.
Colandrea VJ, Legiec IE, Huo P, Yan L, Hale JJ, Mills SG, Bergstrom J, Card D, Chebret G, Hajdu R, Keohane CA, Milligan JA, Rosenbach MJ, Shei GJ, Mandala SM. Colandrea VJ, et al. Among authors: mills sg. Bioorg Med Chem Lett. 2006 Jun 1;16(11):2905-8. doi: 10.1016/j.bmcl.2006.03.038. Epub 2006 Mar 31. Bioorg Med Chem Lett. 2006. PMID: 16580205
Highly selective and potent agonists of sphingosine-1-phosphate 1 (S1P1) receptor.
Vachal P, Toth LM, Hale JJ, Yan L, Mills SG, Chrebet GL, Koehane CA, Hajdu R, Milligan JA, Rosenbach MJ, Mandala S. Vachal P, et al. Among authors: mills sg. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3684-7. doi: 10.1016/j.bmcl.2006.04.064. Epub 2006 May 6. Bioorg Med Chem Lett. 2006. PMID: 16682185
84 results