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Method for screening of therapeutic agent for hyperlipemia

Foreign code F170009204
File No. A261-11WO
Posted date Sep 12, 2017
Country EPO
Application number 10833235
Gazette No. 2505660
Gazette No. 2505660
Date of filing Nov 25, 2010
Gazette Date Oct 3, 2012
Gazette Date May 21, 2014
International application number JP2010070959
International publication number WO2011065389
Date of international filing Nov 25, 2010
Date of international publication Jun 3, 2011
Priority data
  • P2009-269593 (Nov 27, 2009) JP
  • 2010WO-JP70959 (Nov 25, 2010) WO
Title Method for screening of therapeutic agent for hyperlipemia
Abstract (EP2505660)
Disclosed are a highly safe treatment method for hyperlipidemia and a therapeutic agent for hyperlipidemia.
Specifically, the invention provides a novel method for screening an agent for treating hyperlipidemia, more specifically, a method for screening a substance that can inhibit the production or function of gangliosides, particularly GM3, or inhibit the activity or expression of GM3 synthase to reduce a blood lipid level.
A pharmaceutical composition, which can specifically inhibit the production of gangliosides, particularly GM3, thereby effective for hyperlipidemia treatment, and others are also provided.
Scope of claims [claim1]
1. A method for screening a substance having a blood lipid level lowering activity, which comprises: (i) contacting GM3 synthase with a substrate thereof in the presence or absence of a test substance, (ii) selecting a test substance that decreases the synthesized amount of GM3, (iii) administering the selected test substance to a non-human animal, and (iv) determining the blood lipid level in the non-human animal.
[claim2]
2. A method for screening a substance having a blood lipid level lowering activity, which comprises: (i) contacting a test substance with a cell expressing GM3 synthase, (ii) selecting a test substance that decreases the expression level of GM3 synthase, (iii) administering the selected test substance to a non-human animal, and (iv) determining the blood lipid level in the non-human animal.
[claim3]
3. The method according to claim 2, wherein the cell expressing GM3 synthase is selected from the group consisting of adipocytes, hepatocytes, vascular endothelial cells, vascular smooth muscle cells, skeletal muscle cells, epithelial cells, neurocytes, fibroblasts, monocytes and macrophages.
[claim4]
4. The method according to claim 2, wherein the cell expressing GM3 synthase is a transformant produced by genetic engineering.
[claim5]
5. The screening method according to any one of claims 1 to 4, which further comprises selecting a test substance that reduces a blood cholesterol level and/or a blood triglyceride level.
[claim6]
6. The method according to any one of claims 1 to 5, wherein the non-human animal has a higher blood lipid level than normal level.
[claim7]
7. The method according to any one of claims 1 to 6, wherein the non-human animal is a mouse.
[claim8]
8. A pharmaceutical composition effective for treatment of hyperlipidemia, comprising a substance that specifically prevents a production of a ganglioside.
[claim9]
9. The composition according to claim 8, wherein the ganglioside is GM3.
[claim10]
10. A pharmaceutical composition effective for treatment of hyperlipidemia, comprising an antibody against GM3, a GM3 synthase inhibitor, or a substance that inhibits GM3 synthase expression.
  • Applicant
  • JAPAN SCIENCE AND TECHNOLOGY AGENCY
  • Inventor
  • INOKUCHI JINICHI
  • NAGAFUKU MASAKAZU
  • HAYAMIZU HIROTAKA
IPC(International Patent Classification)
U.S. Cl./(Sub)
  • A61K045/06
  • C12Q001/48
  • C12Q001/60
  • C12Q001/61
  • S01N333/910D9
  • S01N405/10
  • S01N500/02
  • S01N800/04B
  • S01N800/32D
Specified countries (EP2505660)
Contracting States: AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
Reference ( R and D project ) CREST Clarification of the Biological Functions of Sugar Chains and the Use of this Knowledge in Applied Technologies AREA
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