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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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.",

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doi = "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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KW - depsides

KW - inhibitors

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KW - sekikaic acid

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

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Keywords

ASJC Scopus subject areas

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