Yissum - Research Development Company of the Hebrew University

Efficient Chemical Preparation of Highly Stable and Fully Active Human Seleno-Insulin Analogue

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

Summary of the technology

Efficient Chemical Preparation of Highly Stable and Fully Active Human Seleno-Insulin Analogue
Project ID : 6-2018-4657

Yissum - Research Development Company of the Hebrew University

Description of the technology

Keywords

Selenocysteine, peptides, stability, activity, insulin

Current development stage

TRL3 - hypothesis testing and intial POC demonstrated in limited # of in-vitro models

Application

Insulin is the most important and widely used of drugs for patients with diabetes mellitus. The chemical synthesis of insulin analogs is very attractive as it allows incorporation of unnatural moieties, which would have further effect (higher) on insulin activity and stability. Efficient preparation of insulin analogs is still time consuming and limited with low yields. Here we found a better way to prepare fully active highly stable human insulin analogs based on the reactivity of selenocysteine in enhancing protein folding.

Our Innovation

Our synthesis approach requires incorporation of selenocysteine residues in the insulin hormone, which allows efficient preparation insulin based on the recombination method between chain A and chain B.

  • The new human insulin analog is far more stable than human insulin under all tested conditions, yet it is fully active.
  • crystal structure by X-ray diffraction was solved.
  • An isolated yield of ~30%, which is higher than previous preparation and in shorter time.
  • Does not require orthogonal protecting groups as usually required.

Technology

Chemical synthesis of insulin and analogs is a long-standing goal in insulin research. We use our expertise in peptide and protein chemistry and selenium chemistry to solve this long standing challenge. By simple substitutions in the peptide sequence of insulin, we were able to increase the yield of combination between chain A and chain B, to give fully active and highly stable insulin analog.

Figure 1 Activity of Seleno-insulin

Opportunity

Long lasting insulin analogs will be an important drug in the market for patients with diabetes mellitus. Many pharmaceutical companies would consider new insulin analogs with properties similar to what we discovered. Lantus (glargine), sold by Sanofi-Aventis's biotechnology with sales reaching 2.45 Billion EUR per year, yet the patent was expired 2015, and now it is sold by other companies including Eli Lilly under the brand name Basaglar.

Project manager

Ariela Markel
VP, Business Development, Healthcare

Project researchers

Norman Metanis
HUJI, Faculty of Science
The Institute of Chemistry

Related keywords

  • Clean Industrial Technologies
  • Biological Sciences
  • Other (uncategorised)
  • Medical Health related
  • Life Science & Biotechnology

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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