Sekikaic Acid and Lobaric Acid Target a Dynamic Interface of the Coactivator CBP/p300

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

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Date

2012-10-08

Author

Majmudar, Chinmay Y.

Højfeldt, Jonas W.

Arevang, Carl J.

Pomerantz, William C.

Gagnon, Jessica K.

Schultz, Pamela J.

Cesa, Laura C.

Doss, Conor H.

Rowe, Steven P.

Vásquez Chaves, Víctor

Tamayo Castillo, Giselle

Cierpicki, Tomasz

Brooks, Charles L. III

Sherman, David H.

Mapp, Anna K.

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Abstract

Although there have been recent notable successes in thediscovery of ligands that target stable, high-affinity protein-protein interactions (PPIs), the transient and moderateaffinity PPIs that underpin many fundamental cellularprocesses have proven to be far less tractable for liganddiscovery.[1]Prime examples of this are the dynamic com-plexes formed between DNA-bound transcriptional activa-tors and coactivators that are part of eukaryotic transcriptioninitiation.