Cambridge Healthtech Institute’s 18th Annual
Protein-Protein Interactions
Macrocyclic & Small Molecule Drug Leads Against Intracellular Protein Complexes
April 16-17, 2025
CHI's Protein-Protein Interactions (PPI) conference convenes medicinal, structural, and biophysical chemists to share progress and insights on tackling a specific type of difficult-to-drug target: PPI sites that are part of protein complexes relevant to disease. PPIs, as opposed to most catalytic sites of enzymatic proteins, have larger and flatter interaction surfaces, making it hard for the deployed therapeutic molecule to have enough specific interaction sites through which to grab the target. In addition, screening methods for PPI-targeted compounds need to rely on binding detection, rather than enzymatic assays. The challenge in finding therapeutic agents for PPIs is especially acute for intracellular PPIs, because the "larger" agents still need to be small enough to cross a cell’s membrane to reach the PPI target. Learn how leading discovery scientists are discovering and designing small molecules or larger, beyond rule of five (bRo5) molecules such as macrocyclic peptides to disrupt or stabilize medically relevant protein complexes, especially intracellular PPIs.