Category: Science

The approach of selectively targeting specific oncogenic protein-protein interactions (PPI) has been challenging in drug discovery so far. We developed and protected a unique cell-based phenotypic screening system that faithfully allows screening for inhibitors to disrupt such PPI.

Success of tyrosine kinase inhibitors in the clinics validated the advantages of targeted therapies. However, there are multiple targets thoroughly described in the literature as potent oncogenes, which are not yet addressed. Among other reasons for these targets being untargeted, are challenging PPI. A big class of such PPI belong to the proteins that are oncogenes only in certain conformations (e.g., oligomers) and are essential proteins in others (e.g., dimers) and therefore need to be selectively targeted. However, we managed to develop a phenotypical screening system to address these oncogenic conformations.  

The approach of selectively targeting specific oncogenic PPI has been challenging in drug discovery so far. We developed and protected a unique cell-based phenotypic screening system that faithfully allows screening for inhibitors to disrupt such PPI. The technology was used to screen a chemical library and successfully identified STAT5B oligomerization inhibitors that we aim to develop further in RIANA.

Targeting such oncogenic PPI (e.g., oligomerization of STAT5B) is a novel, highly innovative approach toward the development of potent and safe medicines for the treatment of hematopoietic and other cancer types. Due to the nature of this highly selective anti-cancer therapy, we expect significantly less side effects while maintaining adequate efficacy.