Novel 20S proteasome inhibitors


Ref.-No.: 0706-6249-IKF

The proteasome is a central component of the protein degradation machinery in eukaryotic cells and plays a role in regulating cell cycle, neoplastic growth and metastasis. Disruption of this degradative process with small molecule inhibitors against one or more catalytic subunits has implications in a number of human diseases such as cancer, inflammation and ischemic stroke and has exposed the proteasome as an important therapeutic target. Three proteasome inhibitors have so far received regulatory approval: bortezomib, carfilzomib and ixazomib. However, since primary resistance to proteasome inhibitors remains a challenge in patients, there is a continued need for new and/or improved proteasome inhibitors.


Scientists from the Max-Planck-Institute for Terrestrial Microbiology have identified novel beta-lactone inhibitors from g-proteobacteria. The compounds specifically inhibit the eukaryotic 20S proteasome by covalently linking to subunit β5.

The compounds can be used

  • in proteasome inhibitor therapies against cancer, infectious, inflammatory or autoimmune diseases
  • as disinfection or sterilization agents of inanimate objects
  • in plant protection or control of plant diseases.

We are now looking for a collaboration partner to further develop the compounds.

Patent Information

A PCT application was filed on November, 15th 2022: WO2023084124A1.


Yi-Ming Shi et al., Nature 2022.

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