Electrophilic groups are one of the key pillars of contemporary chemical biology and
medicinal chemistry. For instance, 3‐membered N‐heterocyclic compounds—such as …

Advances in targeted covalent inhibitors (TCIs) have been made by using lysine‐reactive
chemistries. Few aminophiles possessing balanced reactivity/stability for the development of …

The element boron has not received much attention in biomedical applications compared to
its periodic table neighbors carbon, nitrogen and oxygen. Arguably, this might be due to the …

Resurgent interest in covalent target engagement in drug discovery has demonstrated that
small molecules containing weakly reactive electrophiles can be safe and effective …

This Perspective delineates how redox signaling affects the activity of specific enzyme
isoforms and how this property may be harnessed for rational drug design. Covalent drugs …

While elucidating the inhibitory mechanism of a hydrolytic enzyme by aldehyde-containing
natural products, we discovered a reaction involving a rapid 6π-azaelectrocyclization of …

The choice of an appropriate electrophile is crucial in the design of targeted covalent
inhibitors (TCIs). In this report, we systematically investigated the glutathione (GSH) …

Covering: 1900 to 2011 The study of biologically active natural products has resulted in
seminal contributions to our understanding of living systems. In the case of electrophilic …

The emerging use of covalent ligands as chemical probes and drugs would benefit from an
expanded repertoire of cysteine-reactive electrophiles for efficient and diverse targeting of …

Strategies to target specific protein cysteines are critical to covalent probe and drug
discovery. 3-Bromo-4, 5-dihydroisoxazole (BDHI) is a natural product-inspired, synthetically …