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 …

Activity-based protein profiling (ABPP) is a versatile strategy for identifying and
characterizing functional protein sites and compounds for therapeutic development …

The ubiquitin system contains a wealth of potential drug targets for many diseases and
conditions, including neurodegenerative, immune, metabolic and developmental diseases …

Tryptophan (Trp) plays a variety of critical functional roles in protein biochemistry; however,
owing to its low natural frequency and poor nucleophilicity, the design of effective methods …

Proteome profiling by activated esters identified> 9000 ligandable lysines but they are
limited as covalent inhibitors due to poor hydrolytic stability. Here we report our efforts to …

The S‐alkylation of Cys residues with a maleimide and the Nϵ‐acylation of Lys residues
with an N‐hydroxysuccinimide (NHS) ester are common methods for bioconjugation. Using …

The progressive emergence of protein biomarkers promises a revolution in the healthcare
industry and a shift of focus from disease management to much earlier intervention. Here …

Recently, numerous efforts have been devoted to identifying drug targets and binding sites
in complex proteomes, which is of great importance in modern drug discovery. In this study …

The use of light‐responsive proteins to control both living or synthetic cells, is at the core of
the expanding fields of optogenetics and synthetic biology. It is thus apparent that a richer …

Covalent modification of endogenous proteins by chemical probes is used for proteome-
wide profiling of cellular protein function and drug discovery. However, probe selectivity in …