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Items: 1 to 20 of 96

1.

Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.

Nakamura T, Asano M, Sekiguchi Y, Mizuno Y, Tamaki K, Nara F, Kawase Y, Yabe Y, Nakai D, Kamiyama E, Urasaki-Kaneno Y, Shimozato T, Doi-Komuro H, Kagari T, Tomisato W, Inoue R, Nagasaki M, Yuita H, Oguchi-Oshima K, Kaneko R, Nishi T.

Eur J Med Chem. 2012 May;51:92-8. doi: 10.1016/j.ejmech.2012.02.022. Epub 2012 Feb 25.

PMID:
22405291
2.

Discovery of CS-2100, a potent, orally active and S1P3-sparing S1P1 agonist.

Nakamura T, Asano M, Sekiguchi Y, Mizuno Y, Tamaki K, Kimura T, Nara F, Kawase Y, Shimozato T, Doi H, Kagari T, Tomisato W, Inoue R, Nagasaki M, Yuita H, Oguchi-Oshima K, Kaneko R, Watanabe N, Abe Y, Nishi T.

Bioorg Med Chem Lett. 2012 Feb 15;22(4):1788-92. doi: 10.1016/j.bmcl.2011.12.019. Epub 2012 Jan 2.

PMID:
22264485
3.

Synthesis and SAR of 1,3-thiazolyl thiophene and pyridine derivatives as potent, orally active and S1P₃-sparing S1P₁ agonists.

Asano M, Nakamura T, Sekiguchi Y, Mizuno Y, Yamaguchi T, Tamaki K, Shimozato T, Doi-Komuro H, Kagari T, Tomisato W, Inoue R, Yuita H, Oguchi-Oshima K, Kaneko R, Nara F, Kawase Y, Masubuchi N, Nakayama S, Koga T, Namba E, Nasu H, Nishi T.

Bioorg Med Chem Lett. 2012 May 1;22(9):3083-8. doi: 10.1016/j.bmcl.2012.03.067. Epub 2012 Mar 23.

PMID:
22487179
4.

Discovery of a brain-penetrant S1P₃-sparing direct agonist of the S1P₁ and S1P₅ receptors efficacious at low oral dose.

Demont EH, Arpino S, Bit RA, Campbell CA, Deeks N, Desai S, Dowell SJ, Gaskin P, Gray JR, Harrison LA, Haynes A, Heightman TD, Holmes DS, Humphreys PG, Kumar U, Morse MA, Osborne GJ, Panchal T, Philpott KL, Taylor S, Watson R, Willis R, Witherington J.

J Med Chem. 2011 Oct 13;54(19):6724-33. doi: 10.1021/jm200609t. Epub 2011 Sep 9.

PMID:
21838322
5.

Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.

Nishi T, Miyazaki S, Takemoto T, Suzuki K, Iio Y, Nakajima K, Ohnuki T, Kawase Y, Nara F, Inaba S, Izumi T, Yuita H, Oshima K, Doi H, Inoue R, Tomisato W, Kagari T, Shimozato T.

ACS Med Chem Lett. 2011 Mar 2;2(5):368-72. doi: 10.1021/ml100301k. eCollection 2011 May 12.

6.

Pharmacophore-based design of novel oxadiazoles as selective sphingosine-1-phosphate (S1P) receptor agonists with in vivo efficacy.

Quattropani A, Sauer WH, Crosignani S, Dorbais J, Gerber P, Gonzalez J, Marin D, Muzerelle M, Beltran F, Nichols A, Georgi K, Schneider M, Vitte PA, Eligert V, Novo-Perez L, Hantson J, Nock S, Carboni S, de Souza AL, Arrighi JF, Boschert U, Bombrun A.

ChemMedChem. 2015 Apr;10(4):688-714. doi: 10.1002/cmdc.201402557. Epub 2015 Mar 3.

PMID:
25735812
7.

The selective sphingosine 1-phosphate receptor 1 agonist ponesimod protects against lymphocyte-mediated tissue inflammation.

Piali L, Froidevaux S, Hess P, Nayler O, Bolli MH, Schlosser E, Kohl C, Steiner B, Clozel M.

J Pharmacol Exp Ther. 2011 May;337(2):547-56. doi: 10.1124/jpet.110.176487. Epub 2011 Feb 23.

8.

Full pharmacological efficacy of a novel S1P1 agonist that does not require S1P-like headgroup interactions.

Gonzalez-Cabrera PJ, Jo E, Sanna MG, Brown S, Leaf N, Marsolais D, Schaeffer MT, Chapman J, Cameron M, Guerrero M, Roberts E, Rosen H.

Mol Pharmacol. 2008 Nov;74(5):1308-18. doi: 10.1124/mol.108.049783. Epub 2008 Aug 15.

9.

ASP4058, a novel agonist for sphingosine 1-phosphate receptors 1 and 5, ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile.

Yamamoto R, Okada Y, Hirose J, Koshika T, Kawato Y, Maeda M, Saito R, Hattori K, Harada H, Nagasaka Y, Morokata T.

PLoS One. 2014 Oct 27;9(10):e110819. doi: 10.1371/journal.pone.0110819. eCollection 2014.

10.

Off the shelf but not mass produced.

Karliner JS.

Chem Biol. 2005 Jun;12(6):614-5.

11.

Efficacy and immunomodulatory actions of ONO-4641, a novel selective agonist for sphingosine 1-phosphate receptors 1 and 5, in preclinical models of multiple sclerosis.

Komiya T, Sato K, Shioya H, Inagaki Y, Hagiya H, Kozaki R, Imai M, Takada Y, Maeda T, Kurata H, Kurono M, Suzuki R, Otsuki K, Habashita H, Nakade S.

Clin Exp Immunol. 2013 Jan;171(1):54-62. doi: 10.1111/j.1365-2249.2012.04669.x.

12.

A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model.

Pan S, Mi Y, Pally C, Beerli C, Chen A, Guerini D, Hinterding K, Nuesslein-Hildesheim B, Tuntland T, Lefebvre S, Liu Y, Gao W, Chu A, Brinkmann V, Bruns C, Streiff M, Cannet C, Cooke N, Gray N.

Chem Biol. 2006 Nov;13(11):1227-34.

13.

Mapping pathways downstream of sphingosine 1-phosphate subtype 1 by differential chemical perturbation and proteomics.

Gonzalez-Cabrera PJ, Hla T, Rosen H.

J Biol Chem. 2007 Mar 9;282(10):7254-64. Epub 2007 Jan 10.

14.

Sphingosine 1-phosphate receptor type 1 regulates egress of mature T cells from mouse bone marrow.

Maeda Y, Seki N, Sato N, Sugahara K, Chiba K.

Int Immunol. 2010 Jun;22(6):515-25. doi: 10.1093/intimm/dxq036. Epub 2010 May 23.

PMID:
20497959
16.

S1P1-selective in vivo-active agonists from high-throughput screening: off-the-shelf chemical probes of receptor interactions, signaling, and fate.

Jo E, Sanna MG, Gonzalez-Cabrera PJ, Thangada S, Tigyi G, Osborne DA, Hla T, Parrill AL, Rosen H.

Chem Biol. 2005 Jun;12(6):703-15.

17.

S1P(1) receptor modulation with cyclical recovery from lymphopenia ameliorates mouse model of multiple sclerosis.

Gonzalez-Cabrera PJ, Cahalan SM, Nguyen N, Sarkisyan G, Leaf NB, Cameron MD, Kago T, Rosen H.

Mol Pharmacol. 2012 Feb;81(2):166-74. doi: 10.1124/mol.111.076109. Epub 2011 Oct 26.

18.

Sphingosine-1-phosphate receptor type-1 agonism impairs blood dendritic cell chemotaxis and skin dendritic cell migration to lymph nodes under inflammatory conditions.

Gollmann G, Neuwirt H, Tripp CH, Mueller H, Konwalinka G, Heufler C, Romani N, Tiefenthaler M.

Int Immunol. 2008 Jul;20(7):911-23. doi: 10.1093/intimm/dxn050. Epub 2008 May 20.

PMID:
18495625
19.

A potent and selective S1P(1) antagonist with efficacy in experimental autoimmune encephalomyelitis.

Quancard J, Bollbuck B, Janser P, Angst D, Berst F, Buehlmayer P, Streiff M, Beerli C, Brinkmann V, Guerini D, Smith PA, Seabrook TJ, Traebert M, Seuwen K, Hersperger R, Bruns C, Bassilana F, Bigaud M.

Chem Biol. 2012 Sep 21;19(9):1142-51. doi: 10.1016/j.chembiol.2012.07.016.

20.

Sphingosine 1-phosphate type 1 receptor agonism inhibits transendothelial migration of medullary T cells to lymphatic sinuses.

Wei SH, Rosen H, Matheu MP, Sanna MG, Wang SK, Jo E, Wong CH, Parker I, Cahalan MD.

Nat Immunol. 2005 Dec;6(12):1228-35. Epub 2005 Nov 6.

PMID:
16273098

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