Sekikaic Acid and Lobaric Acid Target a Dynamic Interface of the Coactivator CBP/p300 (pages 11258–11262)
Dr. Chinmay Y. Majmudar, Dr. Jonas W. Højfeldt, Carl J. Arevang, Dr. William C. Pomerantz, Jessica K. Gagnon, Pamela J. Schultz, Laura C. Cesa, Conor H. Doss, Dr. Steven P. Rowe, Victor Vásquez, Prof. Dr. Giselle Tamayo-Castillo, Prof. Dr. Tomasz Cierpicki, Prof. Dr. Charles L. Brooks III, Prof. Dr. David H. Sherman and Prof. Dr. Anna K. Mapp
Article first published online: 8 OCT 2012 | DOI: 10.1002/anie.201206815
Capturing a coactivator, naturally: The natural products sekikaic acid and lobaric acid, isolated after a high-throughput screen of a structurally diverse extract collection, effectively target the dynamic binding interfaces of the GACKIX domain of the coactivator CBP/p300 (see structure). These molecules are the most effective inhibitors of the GACKIX domain yet described and are uniquely selective for this domain.