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 central role of dysregulated kinase activity in the etiology of progressive disorders,
including cancer, has fostered incremental efforts on drug discovery programs over the past …

Targeted covalent inhibitors (TCIs) are designed to bind poorly conserved amino acids by
means of reactive groups, the so-called warheads. Currently, targeting noncatalytic cysteine …

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 …

ATP-competitive fibroblast growth factor receptor (FGFR) kinase inhibitors, including
BGJ398 and Debio 1347, show antitumor activity in patients with intrahepatic …

Over the past decade, covalent kinase inhibitors (CKI) have seen a resurgence in drug
discovery. Covalency affords a unique set of advantages as well as challenges relative to …

Covalent probes can display unmatched potency, selectivity, and duration of action;
however, their discovery is challenging. In principle, fragments that can irreversibly bind their …

Although covalent inhibitors have been used as therapeutics for more than a century, there
has been general resistance in the pharmaceutical industry against their further …

Bruton's tyrosine kinase (BTK), a cytoplasmic tyrosine kinase, plays a central role in
immunity and is considered an attractive target for treating autoimmune diseases. The use of …

Some of the most widely used drugs, such as aspirin and penicillin, are covalent drugs.
Covalent binding can improve potency, selectivity, and duration of the effects, but the …