Yissum - Research Development Company of the Hebrew University

A Promising Agent for Coronavirus SARS-CoV-2 Infection therapy: Orally Available - Highly Potent Integrin avb3/avb5 Inhibitor

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

Summary of the technology

A Promising Agent for Coronavirus SARS-CoV-2 Infection therapy: Orally Available - Highly Potent Integrin avb3/avb5 Inhibitor
Project ID : 47-2020-10889

Description of the technology

Pneumonia caused by the new coronavirus SARS-CoV-2 has caused serious damage to people’s lives and health. The initial route of infection is the binding of the spike protein (S protein) of the virus to the angiotensin-converting enzyme 2 (ACE2). From bioinformatics analysis, it was found that the S protein of SARS-CoV-2 produced an evolutionary mutation of K403R compared with the S protein of SARS-CoV, forming an adjacent RGD motif at the interaction surface.

A wide array of viruses utilize integrins as receptors to mediate multiple functions such as viral entry and activation of signalling events. Integrins are integral membrane proteins that mediate a variety of functions including cell adhesion and signalling events. Integrins are arranged as heterodimers on the cell surface composed of two transmembrane subunits: an α and a β subunit. The integrin heterodimers have a large extracellular domain to mediate binding to ligands, such as extracellular membrane proteins, including fibronectin or vitronectin, either through the I- (or A) domain within the α subunit or through an interface formed by the β propeller domain of the α subunit with the I- domain of the β subunit. Oftentimes integrins recognize and bind to their ligands through short, linear integrin-binding motifs, such as the arginine–glycine–aspartic acid (RGD) motifs. Integrins have a short cytoplasmic domain that can elicit the activation of signalling pathways and can promote cytoskeletal rearrangement within the cells.

As the RGD motif is considered as a ligand for many cell surface integrins, Gilon and Hoffman propose that the binding of S protein of SARS-CoV-2 with integrins may facilitate the infection process of the virus. Therefore they performed high-throughput virtual screening by choosing the key residues of S protein interface of SARS-CoV-2 and the adjacent RGD motif as potential binding site, to search for the potential agents targeting interaction of S protein of SARS-CoV-2 with both ACE2 and integrins as potential therapeutic drugs.

It has already been shown that the Zika virus (ZIKV), a close relative of the coronavirus SARS-CoV-2, uses integrin avb5 to infect neural stem cells. Gilon and Hoffman have developed a highly potent, orally available integrin avb3/avb5 inhibitor.

They propose to test whether this inhibitor will block the entry, activation and signalling events used by the coronavirus SARS-CoV-2 for infection.

Project manager

Keren-Or Amar
VP, Business Development, Healthcare

Project researchers

Chaim Gilon
HUJI, Faculty of Science
The Institute of Chemistry

Amnon Hoffman
HUJI, School of Medicine - IMRIC
School of Pharmacy- Institute for Drug Research

Related keywords

  • Infectious Diseases
  • Virus, Virology / Antibiotics / Bacteriology
  • Biological Sciences
  • Biology / Biotechnology
  • Medicine, Human Health
  • Covid-19
  • covid-19

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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