Title:
METHODS FOR EVALUATING AND SCREENING S1P1 RECEPTOR AGONISTS
Document Type and Number:
WIPO Patent Application WO/2015/025871
Kind Code:
A1
Abstract:
It was discovered that the main effect (immunosuppressive activity) of S1P1 receptor agonists correlates with the selectivity for cells expressing a combination of S1P1 receptors and Gαi2 or Gαi3, and that the side effect (cardiotoxicity) of S1P1 receptor agonists correlates with the selectivity for cells expressing a combination of S1P1 receptors and Gαi1.
Inventors:
NINOMIYA TOMOHISA (JP)
YOSHIDA SATOSHI (JP)
YOSHIDA SATOSHI (JP)
Application Number:
PCT/JP2014/071737
Publication Date:
February 26, 2015
Filing Date:
August 20, 2014
Export Citation:
Assignee:
MEIJI SEIKA PHARMA CO LTD (JP)
International Classes:
G01N33/50; A61K31/397; A61K45/00; A61P37/06; A61P43/00; G01N33/15; C07K14/705
Domestic Patent References:
| WO2013094761A1 | 2013-06-27 | |||
| WO2013094761A1 | 2013-06-27 |
Foreign References:
| JP2010524886A | 2010-07-22 | |||
| EP1826197A1 | 2007-08-29 |
Other References:
KENJI CHIBA: "A New Therapeutic Approach for Autoimmune Diseases by the Sphingosine 1-Phosphate Receptor Modulator, Fingolimod (FTY720", JOURNAL OF THE PHARMACEUTICAL SOCIETY OF JAPAN, vol. 129, no. 6, 2009, pages 655 - 665, XP055318091
ZHI L ET AL.: "FTY720 blocks egress of T cells in part by abrogation of their adhesion on the lymph node sinus", J IMMUNOL, vol. 187, no. 5, pages 2244 - 2251, XP055318088
GERGELY P ET AL.: "The selective sphingosine 1-phosphate receptor modulator BAF312 redirects lymphocyte distribution and has species-specific effects on heart rate", BR J PHARMACOL, vol. 167, no. 5, November 2012 (2012-11-01), pages 1035 - 1047, XP002718009
HILL JJ ET AL.: "Inhibition of a Gi- activated potassium channel (GIRK1/4) by the Gq-coupled m1 muscarinic acetylcholine receptor", J BIOL CHEM, vol. 276, no. 8, 23 February 2001 (2001-02-23), pages 5505 - 5510, XP055318087
PHAM TH ET AL.: "S1P1 receptor signaling overrides retention mediated by G alpha i-coupled receptors to promote T cell egress", IMMUNITY, vol. 28, no. 1, January 2008 (2008-01-01), pages 122 - 133, XP055318085
BROWN AJ: "Functional coupling of mammalian receptors to the yeast mating pathway using novel yeast/mammalian G protein alpha-subunit chimeras", YEAST, vol. 16, no. 1, 15 January 2000 (2000-01-15), pages 11 - 22, XP055286795
SATOSHI YOSHIDA ET AL.: "Galphai2/Galphai3 Biased-S1P1 Receptor Agonist no Sosei: Juyotai Karyu Signal Sentaku ni yoru Shindokusei Keigen", ABSTRACTS OF SYMPOSIUM ON MEDICINAL CHEMISTRY, vol. 31 ST, 1 November 2013 (2013-11-01), pages 168, XP008183188
SATOSHI YOSHIDA ET AL.: "Novel S1P1 receptor agonists with unique intracellular signaling", 246TH NATIONAL MEETING OF THE AMERICAN - CHEMICAL-SOCIETY(ACS, vol. 246, 8 September 2013 (2013-09-08), pages 65, XP009192567
SCIENCE, vol. 296, 2002, pages 346 - 349
JOURNAL OF THE AMERICAN SOCIETY OF NEPHROLOGY, vol. 13, no. 4, 2002, pages 1073 - 1083
JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 279, no. 14, 2004, pages 13839 - 13848
MOLECULAR PHARMACOLOGY, vol. 58, 2000, pages 449 - 454
BRITISH JOURNAL OF PHARMACOLOGY, vol. 167, 2012, pages 1035 - 1047
JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 276, no. 8, 2001, pages 5505 - 5510
NATURE CHEMICAL BIOLOGY, vol. 8, 2012, pages 622 - 630
INVEST OPHTHALMOL VIS SCI., vol. 46, no. 6, June 2005 (2005-06-01), pages 1927 - 33
LIFE SCIENCE, vol. 74, no. 4, 12 December 2003 (2003-12-12), pages 489 - 508
See also references of EP 3037818A4
ZHI L ET AL.: "FTY720 blocks egress of T cells in part by abrogation of their adhesion on the lymph node sinus", J IMMUNOL, vol. 187, no. 5, pages 2244 - 2251, XP055318088
GERGELY P ET AL.: "The selective sphingosine 1-phosphate receptor modulator BAF312 redirects lymphocyte distribution and has species-specific effects on heart rate", BR J PHARMACOL, vol. 167, no. 5, November 2012 (2012-11-01), pages 1035 - 1047, XP002718009
HILL JJ ET AL.: "Inhibition of a Gi- activated potassium channel (GIRK1/4) by the Gq-coupled m1 muscarinic acetylcholine receptor", J BIOL CHEM, vol. 276, no. 8, 23 February 2001 (2001-02-23), pages 5505 - 5510, XP055318087
PHAM TH ET AL.: "S1P1 receptor signaling overrides retention mediated by G alpha i-coupled receptors to promote T cell egress", IMMUNITY, vol. 28, no. 1, January 2008 (2008-01-01), pages 122 - 133, XP055318085
BROWN AJ: "Functional coupling of mammalian receptors to the yeast mating pathway using novel yeast/mammalian G protein alpha-subunit chimeras", YEAST, vol. 16, no. 1, 15 January 2000 (2000-01-15), pages 11 - 22, XP055286795
SATOSHI YOSHIDA ET AL.: "Galphai2/Galphai3 Biased-S1P1 Receptor Agonist no Sosei: Juyotai Karyu Signal Sentaku ni yoru Shindokusei Keigen", ABSTRACTS OF SYMPOSIUM ON MEDICINAL CHEMISTRY, vol. 31 ST, 1 November 2013 (2013-11-01), pages 168, XP008183188
SATOSHI YOSHIDA ET AL.: "Novel S1P1 receptor agonists with unique intracellular signaling", 246TH NATIONAL MEETING OF THE AMERICAN - CHEMICAL-SOCIETY(ACS, vol. 246, 8 September 2013 (2013-09-08), pages 65, XP009192567
SCIENCE, vol. 296, 2002, pages 346 - 349
JOURNAL OF THE AMERICAN SOCIETY OF NEPHROLOGY, vol. 13, no. 4, 2002, pages 1073 - 1083
JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 279, no. 14, 2004, pages 13839 - 13848
MOLECULAR PHARMACOLOGY, vol. 58, 2000, pages 449 - 454
BRITISH JOURNAL OF PHARMACOLOGY, vol. 167, 2012, pages 1035 - 1047
JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 276, no. 8, 2001, pages 5505 - 5510
NATURE CHEMICAL BIOLOGY, vol. 8, 2012, pages 622 - 630
INVEST OPHTHALMOL VIS SCI., vol. 46, no. 6, June 2005 (2005-06-01), pages 1927 - 33
LIFE SCIENCE, vol. 74, no. 4, 12 December 2003 (2003-12-12), pages 489 - 508
See also references of EP 3037818A4
Attorney, Agent or Firm:
CENTCREST IP ATTORNEYS (JP)
Patent business corporation cent Crest international patent firm (JP)
Patent business corporation cent Crest international patent firm (JP)
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