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

Protein kinases are key components in cellular signaling pathways as they carry out the
phosphorylation of proteins, primarily on Ser, Thr, and Tyr residues. The catalytic activity of …

We tested the interaction of 72 kinase inhibitors with 442 kinases covering> 80% of the
human catalytic protein kinome. Our data show that, as a class, type II inhibitors are more …

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

Eukaryotic and prokaryotic organisms possess huge numbers of uncharacterized enzymes.
Selective inhibitors offer powerful probes for assigning functions to enzymes in native …

Highlights•Summarized the diverse types of warheads across the human
kinome.•Highlighted facile covalent reactive functional groups which bind protein …

The existence of adult pancreatic progenitor cells has been debated. While some favor the
concept of facultative progenitors involved in homeostasis and repair, neither a location nor …

Abstract Doublecortin like kinase 1 (DCLK1) is an understudied kinase that is upregulated in
a wide range of cancers, including pancreatic ductal adenocarcinoma (PDAC). However …

The human FGF receptors (FGFRs) play critical roles in various human cancers, and several
FGFR inhibitors are currently under clinical investigation. Resistance usually results from …

The unfolded protein response (UPR) plays a central role in regulating endoplasmic
reticulum (ER) and global cellular physiology in response to pathologic ER stress. The UPR …