By Drug Development & Delivery | March/April
The modern therapeutic toolbox has been dominated by two poles. Small molecules excel at oral dosing, distribution, and manufacturing, and they are superb when a target exposes deep, well defined pockets. Yet their very compactness, typically <600 Daltons, constrains the surface area they can contact, making it difficult to modulate large, relatively flat protein–protein interfaces (PPIs) or to discriminate among closely related binding epitopes.