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A Small Molecule Discrimination Map of the...
Journal article

A Small Molecule Discrimination Map of the Antibiotic Resistance Kinome

Abstract

Kinase-mediated resistance to antibiotics is a significant clinical challenge. These enzymes share a common protein fold characteristic of Ser/Thr/Tyr protein kinases. We screened 14 antibiotic resistance kinases against 80 chemically diverse protein kinase inhibitors to map resistance kinase chemical space. The screens identified molecules with both broad and narrow inhibition profiles, proving that protein kinase inhibitors offer privileged …

Authors

Shakya T; Stogios PJ; Waglechner N; Evdokimova E; Ejim L; Blanchard JE; McArthur AG; Savchenko A; Wright GD

Journal

Cell Chemical Biology, Vol. 18, No. 12, pp. 1591–1601

Publisher

Elsevier

Publication Date

December 2011

DOI

10.1016/j.chembiol.2011.10.018

ISSN

2451-9456