L. Zender

Thinking Outside the Binding Site: A Self-Encapsulating Kinase Inhibitor Remodels Its Pocket to Achieve Selectivity.

Rendering kinase inhibitors selective is a strict requirement in drug development and remains a persistent challenge. To identify new routes to engineer selectivity, we have discovered a first-in-class p38δ-isoform selective inhibitor reflecting 12 000-fold selectivity improvement over currently available compounds and...