Fragment growing to retain or alter the selectivity of anchored kinase hinge-binding fragments†
Charlotte E. Allen,Amanda J. Welford,Thomas P. Matthews,John J. Caldwell,Ian Collins
MedChemComm Pub Date : 12/16/2013 00:00:00 , DOI:10.1039/C3MD00308F
Abstract

The activity patterns of kinase hinge-binding fragments can be retained or redirected in fragment growing strategies. Targeting conserved kinase features preserved the selectivity pattern of a PKB hinge-binding fragment over a 5000-fold increase in potency, while late-stage modification of a CHK1 hinge-binding fragment substantially changed the pattern.

Graphical abstract: Fragment growing to retain or alter the selectivity of anchored kinase hinge-binding fragments