Structural characterization of human Vaccinia-Related Kinases (VRK) bound to small-molecule inhibitors identifies different P-loop conformations
R. M. Counago, C. K. Allerston, P. Savitsky, H. Azevedo, P. H. Godoi, C. I. Wells, A. Mascarello, F. H. de Souza Gama, K. B. Massirer, W. J. Zuercher, C. R. W. Guimaraes, O. Gileadi
The paper identifies BI-D1870 as a starting point for VRK inhibitors and reports co-crystal structures revealing different P-loop conformations in VRK1 and VRK2.
bioRxiv · Mar 2, 2017Biochemistry