inhibition of protein-protein interactions

What is it about?

This work is about developing synthetic small molecules that can recognise proteins that mis-function in diseases such as cancer. A major challenge in drug-discovery is to inhibit such proteins as this offers opportunities for better treatments with fewer side-effects, however this class of protein has historically been much more difficult to recognise using small molecules.

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Why is it important?

This work is significant because it demonstrates for the first time several key properties that a molecule with good protein-recognition properties should bear. Using p53/hDM2, BH3/Mcl-1 and other cancer targets we show that a class of molecule termed a "proteomimetic" (because it structurally resembles a segment of protein) has recognition properties that depend on the composition and 3-D spatial positioning of recognition groups.