New most selective proteasome inhibitors for use in the pharmaceutical industry

Researchers from the Universitat Jaume I of Castelló (Spain) and the Max Planck Institute (Germany) have developed new proteasome inhibitors with different pharmacological properties to those previously developed, which could be used in the pharmaceutical sector.

The proteasome is a multi-protein complex whose main function is the enzymatic degradation of unnecessary or harmful proteins, which are marked for degradation by another protein called "ubiquitin", whose role (discovered by Ciechanover, Hershko and Rose) earned them the Nobel Prize in 2004. Its function is fundamental, influencing activities such as the cell cycle, cell death and the immune response.

Proteasome inhibitors prevent this multi-protein complex from removing proteins that are important for controlling cell division. They are often used in tumour-related diseases, but could also have applications in autoimmune or neurodegenerative diseases, for example because they affect tumour cells more than healthy cells.

The advantages of the new proteasome inhibitors include higher affinity, more specificity and improved properties compared to commercial drugs (greater target selectivity). The research was funded by the Universitat Jaume I through the 2018 Research Promotion Plan project (UJI-B2018-41) and the UJI Lab Impuls project for the valorisation and transfer of research results 2023 (EvIPCaF).

The UJI Organic and Medicinal Chemistry research group, led by Professor Florenci González of the Department of Inorganic and Organic Chemistry, and the German institute have validated the inhibitors on an experimental scale in the laboratory. The technology has been filed for a European patent and can be developed and adapted for specific applications through specific agreements or licences.

The Universitat Jaume I, through the Office for Technological Cooperation and Development and the Vice-Rector's Office for Transfer, Innovation and Scientific Dissemination, facilitates the scientific and technological transfer of its research staff, with the aim of advancing its vocation to transmit and disseminate scientific, technical, social and humanistic knowledge.