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 …

Receptor tyrosine kinase signalling pathways have been successfully targeted to inhibit
proliferation and angiogenesis for cancer therapy. However, kinase deregulation has been …

We recently described glutathione peroxidase 4 (GPX4) as a promising target for killing
therapy-resistant cancer cells via ferroptosis. The onset of therapy resistance by multiple …

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 …

The concept of cell signaling in the context of nonenzyme-assisted protein modifications by
reactive electrophilic and oxidative species, broadly known as redox signaling, is a uniquely …

In the first decade of targeted covalent inhibition, scientists have successfully reversed the
previous trend that had impeded the use of covalent inhibition in drug development …

Covalent enzyme inhibitors are widely applied as biochemical tools and therapeutic agents.
As a complement to categorization of these inhibitors by reactive group or modification site …

Targeted covalent inhibitors are an important class of drugs and chemical probes. However,
relatively few electrophiles meet the criteria for successful covalent inhibitor design. Here we …

Covalent inhibitors and other types of covalent modalities have seen a revival in the past two
decades, with a variety of new targeted covalent drugs having been approved in recent …

Selective covalent inhibition of kinases by targeting poorly conserved cysteines has proven
highly fruitful to date in the development of chemical probes and approved drugs. However …