Sekikaic acid and lobaric acid target a dynamic interface of the coactivator CBP/p300

Chinmay Y. Majmudar, Jonas W. Højfeldt, Carl J. Arevang, William C. Pomerantz, Jessica K. Gagnon, Pamela J. Schultz, Laura C. Cesa, Conor H. Doss, Steven P. Rowe, Victor Vásquez, Giselle Tamayo-Castillo, Tomasz Cierpicki, Charles L. Brooks, David H. Sherman, Anna K. Mapp

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Abstract

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.

Original languageEnglish (US)
Pages (from-to)11258-11262
Number of pages5
JournalAngewandte Chemie - International Edition
Volume51
Issue number45
DOIs
StatePublished - Nov 5 2012

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Keywords

  • coactivators
  • depsides
  • inhibitors
  • protein-protein interactions
  • sekikaic acid

Cite this

Majmudar, C. Y., Højfeldt, J. W., Arevang, C. J., Pomerantz, W. C., Gagnon, J. K., Schultz, P. J., Cesa, L. C., Doss, C. H., Rowe, S. P., Vásquez, V., Tamayo-Castillo, G., Cierpicki, T., Brooks, C. L., Sherman, D. H., & Mapp, A. K. (2012). Sekikaic acid and lobaric acid target a dynamic interface of the coactivator CBP/p300. Angewandte Chemie - International Edition, 51(45), 11258-11262. https://doi.org/10.1002/anie.201206815