The epidermal growth factor receptor (EGFR) is a receptor tyrosine kinase that plays a critical
role in the pathogenesis of many cancers. The structure of intact forms of this receptor has …

In traditional folk medicine, Xanthoxylum plants are referred to as 'toothache trees' because
their anesthetic or counter-irritant properties render them useful in the treatment of pain. …

Drug discovery and chemical genetic efforts typically focus on the identification and design
of inhibitors or loss-of-function probes as a means to perturb enzyme function. These tools …

Virtually all of the 560 human proteases are stored as inactive proenyzmes and are strictly
regulated. We report the identification and characterization of the first small molecules that …

2-Aminopyridine-3,5-dicarbonitrile compounds were previously identified as mimetics of
dominant-negative prion protein mutants and inhibit prion replication in cultured cells. Here, we …

10.7554/eLife.06074.001 Bruton's tyrosine kinase (Btk), a Tec-family tyrosine kinase, is
essential for B-cell function. We present crystallographic and biochemical analyses of Btk, which …

More than 30% of acute myeloid leukemia (AML) patients possess activating mutations in
the receptor tyrosine kinase FMS-like tyrosine kinase 3 or FLT3. A small-molecule inhibitor of …

… JA Zorn reports personal fees from BMS outside the submitted work; and Dr Zorn is an
employee and shareholder of BMS. X. Wang reports personal fees from BMS outside the …

IgA antibodies have broad potential as a novel therapeutic platform based on their superior
receptor-mediated cytotoxic activity, potent neutralization of pathogens, and ability to …

Modulating enzyme function with small-molecule activators, as opposed to inhibitors, offers
new opportunities for drug discovery and allosteric regulation. We previously identified a …