Development of Narrow Spectrum ATP-competitive Kinase Inhibitors as Probes for BIKE and AAK1
Rafael M. Couñago, Alison D. Axtman, Stephen J. Capuzzi, Hátylas Azevedo, David H. Drewry, Jonathan M. Elkins, Opher Gileadi, Cristiano R. W. Guimarães, Alessandra Mascarello, Ricardo A. M. Serafim, Carrow I. Wells, Timothy M. Willson, William J. Zuercher
The paper describes two compounds with minimal structural differences that show significant differential kinase activity, using x-ray crystallography and computational analysis to explain the selectivity.
bioRxiv · Mar 2, 2017 · PreprintPharmacology & Toxicology