Click chemistry is an approach that uses efficient and reliable reactions, such as Cu (I)-
catalyzed azide–alkyne cycloaddition (CuAAC), to bind two molecular building blocks …

Cancer is one of the major and leading causes of death worldwide. Two of the greatest
challenges in fighting cancer are early detection and effective treatments with no or …

The promise of exploiting combinatorial synthesis for small molecule discovery remains
unfulfilled due primarily to the “structure elucidation problem”: the back-end mass …

Protein–protein interactions represent a new class of exciting but challenging drug targets,
because their large, flat binding sites lack well-defined pockets for small molecules to bind …

Combinatorial chemistry provides a powerful tool for the rapid creation of large numbers of
synthetic compounds. Ideally, these libraries should be a rich source of bioactive molecules …

The proteasome is a multisubunit complex responsible for most nonlysosomal turnover of
proteins in eukaryotic cells. Proteasome inhibitors are of great interest clinically, particularly …

One-bead-one-compound (OBOC) libraries provide a powerful tool for drug discovery as
well as biomedical research. However, screening a large number of beads/compounds (> 1 …

Large combinatorial libraries of N-substituted peptides would be an attractive source of
protein ligands, because these compounds are known to be conformationally constrained …

Transient, regulated binding of globular protein domains to Short Linear Motifs (SLiMs) in
disordered regions of other proteins drives cellular signaling. Mapping the energy …

DNA-encoded library (DEL) technology is emerging as a key element of the small molecule
discovery toolbox. Conventional DEL screens (ie, on-DNA screening) interrogate large …