Covalent drugs have been used to treat diseases for more than a century, but tools that
facilitate the rational design of covalent drugs have emerged more recently. The purposeful …

Fragment-based drug discovery (FBDD) continues to evolve and make an impact in the
pharmaceutical sciences. We summarize successful fragment-to-lead studies that were …

Targeted covalent inhibitors have regained widespread attention in drug discovery and have
emerged as powerful tools for basic biomedical research. Fueled by considerable …

Molecules that stabilize protein–protein interactions (PPIs) are invaluable as tool
compounds for biophysics and (structural) biology, and as starting points for molecular glue …

The intracellular interactions of biomolecules can be maneuvered to redirect signaling,
reprogram the cell cycle, or decrease infectivity using only a few dozen atoms. Such …

Protein–protein interactions (PPIs) are essential for biological processes including immune
reactions and diseases. Inhibition of PPIs by drug-like compounds is a common basis for …

With the increased focus on intrinsically disordered proteins (IDPs) and their large
interactomes, the question about their specificity—or more so on their multispecificity—arise …

The development of small-molecule inhibitors or stabilizers of selected protein–protein
interactions (PPIs) of interest holds considerable promise for the development of research …

Covalent inhibitors and other types of covalent modalities have seen a revival in the past two
decades, with a variety of new targeted covalent drugs having been approved in recent …

Molecular Glues, here defined as small molecules that interact with two protein surfaces to
induce or enhance affinity of these two proteins to each other, have received substantial …