Cytoskeletal and protein-protein interaction interfaces (PPI)

Cytoskeletal and protein-protein interaction (PPI) interfaces represent a broad category of therapeutic targets rather than a single molecular entity. These interfaces are the physical regions where proteins contact one another to form complexes, which are essential for nearly all biological processes, including the assembly of the cytoskeleton (e.g., actin filaments and microtubules) and the execution of signal transduction cascades. In many diseases, such as cancer and neurodegeneration, these interactions are often dysregulated, leading to aberrant cell signaling or structural instability. While historically considered undruggable due to their large, flat surfaces, modern drug discovery has successfully developed small molecules and biologics that can either disrupt or stabilize these interfaces. Examples of drugs targeting these systems include microtubule-stabilizing agents like paclitaxel and PPI inhibitors like venetoclax, which targets the Bcl-2 interaction interface.

Other names

Protein-protein interaction interfacesCytoskeletal protein interfacesPPIs

Inhibition or stabilization of physical interactions between two or more protein subunits to modulate biological pathways.