Inside Cover: Discovery of a Potent BTK Inhibitor with a Novel Binding Mode by Using Parallel Selections with a DNA‐Encoded Chemical Library (ChemBioChem 9/2017)

The inside cover picture shows the discovery of a potent BTK inhibitor (orange) by affinity‐based selection from a DNA‐encoded library (top). Addition of ATP (beige) to the selection, which simulates the intracellular environment, displaced any low affinity compounds (purple) but could not displace...

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Bibliographic Details
Published inChembiochem : a European journal of chemical biology Vol. 18; no. 9; p. 826
Main Authors Cuozzo, John W., Centrella, Paolo A., Gikunju, Diana, Habeshian, Sevan, Hupp, Christopher D., Keefe, Anthony D., Sigel, Eric A., Soutter, Holly H., Thomson, Heather A., Zhang, Ying, Clark, Matthew A.
Format Journal Article
LanguageEnglish
Published Weinheim Wiley Subscription Services, Inc 04.05.2017
Subjects
Affinity
Bruton's tyrosine kinase
Coding
Deoxyribonucleic acid
DNA
DNA-encoded library
Inhibitors
kinase inhibitors
Libraries
small molecules
X-ray crystallography
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Summary:The inside cover picture shows the discovery of a potent BTK inhibitor (orange) by affinity‐based selection from a DNA‐encoded library (top). Addition of ATP (beige) to the selection, which simulates the intracellular environment, displaced any low affinity compounds (purple) but could not displace the high affinity inhibitor. As predicted by the selection results, the high affinity BTK inhibitor demonstrated potent cellular activity. More information can be found in the full paper by J. W. Cuozzo et al. on page 864 in Issue 9, 2017 (DOI: 10.1002/cbic.201600573).
ISSN:1439-4227
1439-7633
DOI:10.1002/cbic.201700180