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 …

Protein kinases regulate nearly all aspects of cell life, and alterations in their expression, or
mutations in their genes, cause cancer and other diseases. Here, we review the remarkable …

Summary KRAS G12C was recently identified to be potentially druggable by allele-specific
covalent targeting of Cys-12 in vicinity to an inducible allosteric switch II pocket (S-IIP) …

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

The human genome encodes 538 protein kinases that transfer a γ-phosphate group from
ATP to serine, threonine, or tyrosine residues. Many of these kinases are associated with …

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 …

Eradicating tumor dormancy that develops following epidermal growth factor receptor
(EGFR) tyrosine kinase inhibitor (TKI) treatment of EGFR-mutant non-small cell lung cancer …

Bruton's tyrosine kinase (BTK) is an essential component of multiple signaling pathways that
regulate B cell and myeloid cell proliferation, survival, and functions, making it a promising …

Small molecules are powerful tools for investigating protein function and can serve as leads
for new therapeutics. Most human proteins, however, lack small-molecule ligands, and …

Covalent drugs have made a major impact on human health but until recently were shunned
by the pharmaceutical industry over concerns about the potential for toxicity. A resurgence …