Discovery of Covalent Inhibitors Targeting the Transcriptional Enhanced Associate Domain Central Pocket
Hacer Karataş, Mohammad Akbarzadeh, Hélène Adihou, G. Hahne, Ajaybabu V. Pobbati, Elizabeth Yihui Ng, Stéphanie M. Guéret, Sonja Sievers, Axel Pahl, Malte Metz, Sarah Zinken, Lara Dötsch, Christine Nowak, Sasikala Thavam, Alexandra Friese, CongBao Kang, Wanjin Hong, Herbert Waldmann
Abstract
values, and reduce TEAD target gene expression. This methodology promises to enable new medicinal chemistry programs aimed at the modulation of TEAD activity.
Topics & Concepts
ChemistrySmall moleculeCysteineTranscription factorKojic acidCovalent bondProtein–protein interactionBiochemistryGeneCell biologyComputational biologyBiologyEnzymeOrganic chemistryTyrosinaseHippo pathway signaling and YAP/TAZCellular Mechanics and InteractionsUbiquitin and proteasome pathways