John Charles Kath

TL;DR: P perturbation of adhesion-mediated signaling with a FAK inhibitor, PF-573,228, serves as a useful tool to dissect the functions of FAK in integrin-dependent signaling pathways in normal and cancer cells and forms the basis for the generation of compounds amenable for preclinical and patient trials.

TL;DR: This work led to the discovery of 8k (PF-06463922), combining broad-spectrum potency, central nervous system ADME, and a high degree of kinase selectivity, which was found to be potent against wild-type ALK and clinically reported ALK kinase domain mutations.

TL;DR: PF-562,271 is a potent, ATP-competitive, reversible inhibitor of FAK and Pyk2 catalytic activity with a IC(50) of 1.5 and 14 nmol/L, resulting in robust antitumor activity.

TL;DR: This work uses activity-based protein profiling coupled with quantitative mass spectrometry to globally map the targets, both specific and non-specific, of covalent kinase inhibitors in human cells and shows that, when these windows are exceeded, rampant proteome-wide reactivity and kinase target-independent cell death conjointly occur.

TL;DR: PF-4708671 is the first S6K1-specific inhibitor to be reported and will be a useful tool for delineating S6k1- specific roles downstream of mTOR.