Research

• KRAS G12D and G12V

Protein-Protein Interaction Modulators

One of our special interests is the rational discovery of protein-protein interaction (ppi) modulators. Indeed, it is considered to be, if not impossible, highly challenging. There are very few reported successes, where the first-in-class small molecule ppi modulators would had been identified via virtual screening, from which we were the very first ones - and now we have further successes, seven in total and increasing. Note that we have not only succeeded with blockers but also with identification of binding enhancers,

Our protein-protein interaction modulator discovery begun with collagen-binding integrins. Project started from protein modeling, went to ligand identification, optimization, and tool compound production. This was one of the key factors in our learning curve towards rationalization of the process (trial and error).

Our latest success: Protein-Protein Interaction stabilizers identified with hit rate 100%!

Low uM blockers for protein-protein interaction! We identified several compound classes for this PPI with hit rate of 50%! Currently optimizing the compounds.

Cellular homeostasis - Effector molecules that do not compete with natural small molecules

How about finding a new way to treat diseases? Quite often the homeostasis of our cells is disturbed when competitively acting drugs are employed - This leads into natural response where cells are producing more of the target protein, thus, collapsing the therapeutic effect of pharmaceutical agent. If drug would only interfere the consequent effect, not the binding of the natural ligand, the homeostasis of cell would be maintained, but still the disease would be treated. Again our startegy in blocking of protein-protein interactions would be the perfect solution.

Do you have an interesting case? We would love to hear it, and collaborate with you!!!! It is as easy as A-B-C-D-E-mail: webpagecontact@medchem.fi.