Discovery of a Brain-Penetrant S1P3-Sparing Direct Agonist of the S1P1 and S1P5 Receptors Efficacious at Low Oral Dose-Reference-Cited by-同舟云学术

Discovery of a Brain-Penetrant S1P3-Sparing Direct Agonist of the S1P1 and S1P5 Receptors Efficacious at Low Oral Dose

Published:2011-09-09 Issue:19 Volume:54 Page:6724-6733
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Demont Emmanuel H.,Arpino Sandra,Bit Rino A.,Campbell Colin A.,Deeks Nigel,Desai Sapna,Dowell Simon J.,Gaskin Pam,Gray James R. J.,Harrison Lee A.,Haynes Andrea,Heightman Tom D.¹,Holmes Duncan S.,Humphreys Philip G.,Kumar Umesh,Morse Mary A.,Osborne Greg J.,Panchal Terry,Philpott Karen L.¹,Taylor Simon,Watson Robert,Willis Robert,Witherington Jason

Affiliation:

1. Neurology Center of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/jm200609t

Reference35 articles.

1. Current perspectives on FTY720

2. Phosphorylation of the Immunomodulatory Drug FTY720 by Sphingosine Kinases

3. Novel Immunomodulator FTY720 Is Phosphorylated in Rats and Humans To Form a Single Stereoisomer. Identification, Chemical Proof, and Biological Characterization of the Biologically Active Species and Its Enantiomer

4. Lymphocyte egress from thymus and peripheral lymphoid organs is dependent on S1P receptor 1

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

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