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)

• Published in: Chembiochem : 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
• Language: English
• 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
• DOI: 10.1002/cbic.201700180
• ISSN: 1439-4227

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).