Cambridge Healthtech Institute’s 17th Annual
Protein-Protein Interactions
Small Molecule Lead Discovery and Optimization for Difficult Drug Targets
April 3-4, 2024
Cambridge Healthtech Institute's Protein-Protein Interactions (PPIs) conference covers discovery or design, and optimization of compounds that either disrupt or stabilize protein-protein or protein-nucleic acid complexes. Many of these protein complexes, which are often intracellular and therefore only amenable to cell-penetrating compounds such as small molecules, are crucial players in disease states. However, they have been typically considered ‘difficult-to-drug' because their flat interaction surfaces make the PPIs harder for small molecules to gain a foothold. Furthermore, they are not typically enzymes, so traditional high-throughput enzymatic assay-based screening for identifying small molecule drug leads hasn't been possible. Recent progress, however, in biophysical techniques that screen for molecular interactions rather than an enzymatic event, covalent drug discovery strategies, fragment-based ligand approaches, structure-based drug design, and other advances have spurred progress. Discovery of larger yet cell-permeable molecules such as macrocyclics has also furthered the field. Targeted protein degradation (TPD) 'destroy what you can't inhibit' approaches have also advanced the field and will be covered tangentially. Join fellow medicinal, biophysical, and structural chemists to learn the latest advances and share strategies.