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

doi:10.1002/anie.201206815

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

Research output: Contribution to journal › Article › peer-review

43 Scopus citations

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 language	English (US)
Pages (from-to)	11258-11262
Number of pages	5
Journal	Angewandte Chemie - International Edition
Volume	51
Issue number	45
DOIs	https://doi.org/10.1002/anie.201206815
State	Published - Nov 5 2012
Externally published	Yes

Keywords

coactivators
depsides
inhibitors
protein-protein interactions
sekikaic acid

ASJC Scopus subject areas

Catalysis
General Chemistry

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10.1002/anie.201206815

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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

Majmudar, CY, Højfeldt, JW, Arevang, CJ, Pomerantz, WC, Gagnon, JK, Schultz, PJ, Cesa, LC, Doss, CH, Rowe, SP, Vásquez, V, Tamayo-Castillo, G, Cierpicki, T, Brooks, CL, Sherman, DH & Mapp, AK 2012, 'Sekikaic acid and lobaric acid target a dynamic interface of the coactivator CBP/p300', Angewandte Chemie - International Edition, vol. 51, no. 45, pp. 11258-11262. https://doi.org/10.1002/anie.201206815

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AU - Majmudar, Chinmay Y.

AU - Højfeldt, Jonas W.

AU - Arevang, Carl J.

AU - Pomerantz, William C.

AU - Gagnon, Jessica K.

AU - Schultz, Pamela J.

AU - Cesa, Laura C.

AU - Doss, Conor H.

AU - Rowe, Steven P.

AU - Vásquez, Victor

AU - Tamayo-Castillo, Giselle

AU - Cierpicki, Tomasz

AU - Brooks, Charles L.

AU - Sherman, David H.

AU - Mapp, Anna K.

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

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Keywords

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