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 …

Despite advances in genetic and proteomic techniques, a complete portrait of the proteome
and its complement of dynamic interactions and modifications remains a lofty, and as of yet …

Recent advances in chemical proteomics have begun to characterize the reactivity and
ligandability of lysines on a global scale. Yet, only a limited diversity of aminophilic …

Nimbolide, a terpenoid natural product derived from the Neem tree, impairs cancer
pathogenicity; however, the direct targets and mechanisms by which nimbolide exerts its …

Nucleophilic amino acids make important contributions to protein function, including
performing key roles in catalysis and serving as sites for post-translational modification …

Emerging from the origins of supramolecular chemistry and the development of selective
chemical receptors that rely on lock‐and‐key binding, activity‐based sensing (ABS)—which …

The two main strategies for enzyme engineering, directed evolution and rational design,
have found widespread applications in improving the intrinsic activities of proteins. Although …

Conspectus One of the biggest bottlenecks in modern drug discovery efforts is in tackling the
undruggable proteome. Currently, over 85% of the proteome is still considered undruggable …

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

Protein modification by chemical reagents has played an essential role in the treatment of
human diseases. However, the reagents currently used are limited to the covalent …