Fragment-based screening maps inhibitor interactions in the ATP-binding site of checkpoint kinase 2.

Fragment-based screening maps inhibitor interactions in the ATP-binding site of checkpoint kinase 2.

Checkpoint kinase 2 (CHK2) is an important serine/threonine kinase in the cellular response to DNA damage. A fragment-based screening campaign using a combination of a high-concentration AlphaScreen™ kinase assay and a biophysical thermal shift assay, followed by X-ray crystallography, identified a...

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Main Authors: M Cris Silva-Santisteban, Isaac M Westwood, Kathy Boxall, Nathan Brown, Sam Peacock, Craig McAndrew, Elaine Barrie, Meirion Richards, Amin Mirza, Antony W Oliver, Rosemary Burke, Swen Hoelder, Keith Jones, G Wynne Aherne, Julian Blagg, Ian Collins, Michelle D Garrett, Rob L M van Montfort
Format: Article
Language:English
Published: Public Library of Science (PLoS) 2013-01-01
Series:PLoS ONE
Online Access:https://journals.plos.org/plosone/article/file?id=10.1371/journal.pone.0065689&type=printable
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https://journals.plos.org/plosone/article/file?id=10.1371/journal.pone.0065689&type=printable

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