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). (25th April 2017)

• Record Type: Journal Article
• 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.
• Is Part Of: Chembiochem. Volume 18:Number 9(2017)
• Page Start: 826
• Page End: 826
• Publication Date: 2017-04-25
• Subjects: Bruton's tyrosine kinase -- DNA-encoded library -- kinase inhibitors -- small molecules -- X-ray crystallography; Biochemistry -- Periodicals; Molecular biology -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1002/cbic.201700180
• Languages: English
• ISSNs: 1439-4227

Abstract

Abstract : 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. onpage 864 in Issue 9, 2017 (DOI:10.1002/cbic.201600573 ).