Yissum - Research Development Company of the Hebrew University

Super Active Leptin Antagonists for Treatment of Autoimmune Diseases and CKD-associated Cachexia

Posted by Yissum - Research Development Company of the Hebrew UniversityResponsive · Innovative Products and Technologies · Israel

Summary of the technology

Cluster8
A novel Recombinant leptin mutant acts as antagonist has a strong potential for pharmacologic agent for autoimmune and inflammatory diseases, cancers, and cardiovascular disease, among others. Substitution of two to four amino acid residues of leptin to alanine converts agonist to antagonist without reducing affinity toward leptin receptor.
Keywords: Leptin, antagonist, mutein, multiple sclerosis, inflammatory bowel syndrome, rheumatoid arthritis, fibrosis, cardiovascular disease, breast cancer, colon cancer, prostate cancer, ovarian cancer, obesity

Project ID : 8-2006-198

Description of the technology

Categories

Superactive High Afinity Leptin antagonist, mutein, multiple sclerosis, inflammatory bowel syndrome, rheumatoid arthritis, fibrosis, cardiovascular disease, CKD Cachexia, Osteoarthritis

Development Stage

(1) In vivo tests in animal (mouse) models, (2) Preparation of second generation of antagonists with increased affinity toward leptin receptor and longer in vivo persistence in circulation

Patent Status

Patent number application: WO2011/132189A3

Highlights

  • Advances treatment of many diseases by blocking undesired leptin effects
  • Interacts with mammalian leptin receptor with affinity identical to non-mutated leptins
  • Can be easily prepared in large quantities as recombinant protein expressed in E. coli
  • Effectiveness established in three mice models of human acute and chronic fibrosis

Our Innovation

  • Recombinant leptin mutein acts as antagonist
  • Isolated DNA molecule encoding super active leptin antagonist
  • Strong potential for pharmacologic agent for CKD (Chronic Kidney Disease) associated cachexia, autoimmune and inflammatory diseases, cancers, and cardiovascular disease, among others
  • Substitution of two to four amino acid residues of leptin to alanine converts agonist to antagonist without reducing affinity toward leptin receptor

The Opportunity

  • Addresses multiple markets for treatment of multiple disease entities, specifically, CKD associated cachexia
  • Expands various research fields stressing proteins that inhibit leptin activity

Development Milestones

  • Testing super activeleptin antagonist activity in additional in vivo models e.g., Cachexia Inflammatory Bowel Disease in mice or others
  • Preparation of leptin antagonists with more potent activity in vivo

Additional Information

Project manager

Shani Bullock
VP, Business Development, Healthcare

Project researchers

Arieh Gertler
HUJI, Faculty of Agricultural, Food and Environmental Quality Sciences
Biochemistry, Food Science and Nutrition

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About Yissum - Research Development Company of the Hebrew University

Technology Transfer Office from Israel

Yissum Research Development Company of the Hebrew University of Jerusalem Ltd. Founded in 1964 to protect and commercialize the Hebrew University’s intellectual property. Ranked among the top technology transfer companies, Yissum has registered over 8,900 patents covering 2,500 inventions; has licensed out 800 technologies and has spun-off 90 companies. Products that are based on Hebrew University technologies and were commercialized by Yissum generate today over $2 Billion in annual sales.

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