Extraordinary hit compounds with API-like properties

News
20 March 2018

At the end of 2017, Prof Reuven Stein received an extraordinary Qualified Hit List from the European Lead Factory. His research group studies the tumour microenvironment (TME) and has discovered a protein that plays an essential role in tumour progression. With the promising ELF compounds, they hope to develop new treatments for cancers such as glioma and melanoma.

In the best cases, the current treatments for glioma give the patients one more year to live, in most cases just a few months. Reuven Stein and his team have discovered an enzyme that regulates the ability of the tumour microenvironment cells to promote tumour progression. After failing to find tractable and attractive hits in a small-scale screen for inhibitors in-house, they successfully applied to the European Lead Factory.

The screen performed by the ELF scientists resulted in a Qualified Hit List of 50 compounds. Reuven Stein: ‘The results of the ELF screen exceeded all expectations. The list included several compound classes of unprecedented potency, with low nanomolar activities not only on the target itself, but also in the cell-based assay’. Prof Micha Fridman adds: ‘The compounds have the inhibition levels and physicochemical properties you would expect from an Active Pharmaceutical Ingredient.’

Once further characterization is finished, they are planning to test the use of the ELF compounds in a mouse model. ‘We have a fair chance of actually ending up with a drug candidate. We would never have been able to reach the point where we’re at now without the European Lead Factory’, concludes Micha Fridman.

Read the testimonial of Reuven Stein and Micha Fridman here.