Issue 2, 2014

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

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

Supplementary files

Article information

Article type
Concise Article
Submitted
15 Oct 2013
Accepted
13 Dec 2013
First published
16 Dec 2013
This article is Open Access
Creative Commons BY license

Med. Chem. Commun., 2014,5, 180-185

Author version available

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

C. E. Allen, A. J. Welford, T. P. Matthews, J. J. Caldwell and I. Collins, Med. Chem. Commun., 2014, 5, 180 DOI: 10.1039/C3MD00308F

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