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 …

The cGAS–STING signalling pathway has emerged as a key mediator of inflammation in the
settings of infection, cellular stress and tissue damage. Underlying this broad involvement of …

Multiple anticancer drugs have been proposed to cause cell death, in part, by increasing the
steady-state levels of cellular reactive oxygen species (ROS). However, for most of these …

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 …

Within druggable target space, new small-molecule modalities, particularly covalent
inhibitors and targeted degraders, have expanded the repertoire of medicinal chemists …

Current methods used for measuring amino acid side-chain reactivity lack the throughput
needed to screen large chemical libraries for interactions across the proteome. Here we …

Advances in chemoproteomic technology have revealed covalent interactions between
small molecules and protein nucleophiles, primarily cysteine, on a proteome-wide scale …

Targeted protein degradation induced by heterobifunctional compounds and molecular
glues presents an exciting avenue for chemical probe and drug discovery. To date, small …

The Janus tyrosine kinase (JAK) family of non-receptor tyrosine kinases includes four
isoforms (JAK1, JAK2, JAK3, and TYK2) and is responsible for signal transduction …

Over the past decade, remarkable advances have been witnessed in the development of
small-molecule probes. These molecular tools have been widely applied for interrogating …