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Method for screening of therapeutic agent for hyperlipemia

Foreign code F170009183
File No. A261-11WO
Posted date Sep 12, 2017
Country United States of America
Application number 201013511028
Gazette No. 20120244539
Gazette No. 9090932
Date of filing Nov 25, 2010
Gazette Date Sep 27, 2012
Gazette Date Jul 28, 2015
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 (US9090932)
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 GM3 synthase specific inhibitor having a blood lipid level lowering activity that specifically inhibits GM3 synthase expression, which comprises: contacting a test substance with a cell selected from the group consisting of an adipocyte and a hepatocyte, wherein the cell expresses GM3 synthase;
selecting a test substance that specifically decreases the expression level of GM3 synthase as compared to a control;
administering the selected test substance to a non-human apoE-deficient animal; and
determining a Chylomicron (CM) level, a Very Low Density Lipoprotein (VLDL) level or a Low Density Lipoprotein (LDL) level in blood in the non-human apoE-deficient animal and selecting a test substance having a blood lipid level lowering activity that specifically inhibits GM3 synthase expression and reduces the CM, VLDL or LCL level in blood by 10% or more as compared to a control.
[claim2]
2. The screening method according to claim 1, which further comprises selecting a test substance that reduces a blood cholesterol level and/or a blood triglyceride level.
[claim3]
3. The method according to claim 1, wherein the non-human animal has a higher blood lipid level than normal level.
[claim4]
4. The method according to claim 1, wherein the non-human animal is a mouse.
  • Inventor, and Inventor/Applicant
  • INOKUCHI JINICHI
  • NAGAFUKU MASAKAZU
  • HAYAMIZU HIROTAKA
  • JAPAN SCIENCE AND TECHNOLOGY AGENCY
IPC(International Patent Classification)
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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