Small-molecule protein kinase inhibitors are widely used to elucidate cellular signaling
pathways and are promising therapeutic agents. Owing to evolutionary conservation of the ATP-…

Autoregulatory domains found within kinases may provide more unique targets for chemical
inhibitors than the conserved ATP-binding pocket targeted by most inhibitors. The kinase …

Chemical inhibitors, whether natural products or synthetic, have had an enormous impact
on the study of the eukaryotic cytoskeleton. Here we review the history of some of the most …

The soluble, calcium-binding protein calreticulin shares high sequence homology with
calnexin, a transmembrane chaperone of glycoprotein folding. Our experiments demonstrated …

Ferroptosis is associated with lipid hydroperoxides generated by the oxidation of polyunsaturated
acyl chains. Lipid hydroperoxides are reduced by glutathione peroxidase 4 (GPX4) …

Small-molecule BET bromodomain inhibitors (BETis) are actively being pursued in clinical
trials for the treatment of a variety of cancers, but the mechanisms of resistance to BETis …

Structural coverage of the human kinome has been steadily increasing over time. The structures
provide valuable insights into the molecular basis of kinase function and also provide a …

Current drug discovery efforts focus primarily on proteins with defined enzymatic or small
molecule binding sites. Autoregulatory domains represent attractive alternative targets for small …

Inspired by the usefulness of small molecules to study membrane traffic, we used high-throughput
synthesis and phenotypic screening to discover secramine, a molecule that inhibits …

Kinases are important therapeutic targets in oncology due to their frequent deregulation in
cancer. Typical ATP-competitive kinase inhibitors, however, also inhibit off-target kinases that …