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Screening Methods to Identify New Drugs for Atherosclerosis and Type II Diabetes

Technology Benefits

Potential increase in efficacy due to increased specificityPotential reduction in side effects

Technology Application

In 2012, 29.1 million Americans have diabetes (9.3% of population, up from 7% in 2002). In 2010, 79 million Americans age 20 and older had pre-diabetes. In 2012 this number grew to 86 million. According to the American Diabetes Association the total economic cost of diabetes back in 2002 was estimated at $132 billion. In 2013 this total grew to $245 billion.

Detailed Technology Description

Researchers from UC San Diego have patented a new method that identifies a novel molecular mechanism by which ligands regulate the transcriptional activities of nuclear receptors. This mechanism provides the basis for screening assays to identify novel ligands that repress inflammation by regulating nuclear receptor proteins like PPAR-g. Such compounds would potentially represent improvements over existing drugs used to treat type II diabetes which exhibit significant side effects.

Supplementary Information

Patent Number: US8241863B2
Application Number: US2007886057A
Inventor: Pascual, Gabriel | Glass, Christopher K. | Rosenfeld, Michael G.
Priority Date: 10 Mar 2005
Priority Number: US8241863B2
Application Date: 10 Sep 2007
Publication Date: 14 Aug 2012
IPC Current: G01N003353
US Class: 4350078
Assignee Applicant: The Regents of the University of California
Title: Identification of an evolutionarily conserved pathway mediating transrepression of inflammatory response genes by nuclear receptors
Usefulness: Identification of an evolutionarily conserved pathway mediating transrepression of inflammatory response genes by nuclear receptors
Summary: The method (M1) is useful for screening for a compound that regulates SUMOylation of a nuclear receptor protein, or inflammation by activating SUMOylation of a nuclear receptor protein associated with inflammation. The method (M2) is useful for repressing inflammation. The method (M4) is useful for inhibiting an immune response or inflammatory response by SUMOylating a nuclear receptor protein, where the inflammatory response inhibited is atherosclerosis or diabetes such as type II diabetes. The nuclear receptor protein is useful for inhibiting an immune response or inflammatory response, or inhibiting expression of inflammatory genes, by SUMOylating a nuclear receptor protein. The method (M5) is useful for treating an immune system diseases e.g. type II diabetes (all claimed).
Novelty: Screening compound that regulates SUMOylation of peroxisome proliferator-activated receptor gamma, comprises contacting compound to receptor protein, and detecting SUMOylation of receptor protein

Industry

Biomedical

Sub Category

Medical Composition

Application No.

8241863

Others

State Of Development

This patented technology is available for licensing in the US.

Tech ID/UC Case

22735/2005-149-0

Related Cases

2005-149-0

*Abstract

One class of drugs developed to treat diabetes is the thiazolidinediones, which include rosiglitazone (Avandia®), troglitazone (Rezulin®), and pioglitazone (ACTOS®).  These insulin-sensitizing drugs have been shown to lower blood glucose levels in target tissues (muscle and fat) by modulating PPAR-g, a nuclear receptor involved in fat cell development and glucose homeostasis.  Activators of PPAR-g have been shown to suppress the expression of inflammatory genes that play a role in impaired insulin signaling.  However, thiazolidinediones have also been shown to exhibit serious side effects, including edema, anemia, and liver injury.

*IP Issue Date

Aug 14, 2012

*Principal Investigator

Name: Christopher Glass

Department:

Name: Gabriel Pascual

Department:

Name: Michael Rosenfeld

Department:

Country/Region

USA