Teasing Out Mechanisms of Small-Molecule Kinase Inhibition
This article was originally published in Start Up
Executive Summary
Even as kinases remain a popular target in oncology for industry, two recent papers show how much we have yet to learn about how to interfere with these molecules. These most recent laboratory studies help explain the confusing observation that the very act of inhibiting a kinase with a drug can also "prime" phosphorylation of that target, which in some cases can actually enhance tumor activity.