title: Sekikaic acid and lobaric acid target a dynamic interface of the coactivator CBP/p300.
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. These molecules are the most effective inhibitors of the GACKIX domain yet described and are uniquely selective for this domain.
authors.affiliation: Department of Chemistry, University of Michigan, Ann Arbor, USA.
authors.forename: Chinmay Y
authors.initials: CY
authors.lastname: Majmudar
authors.forename: Jonas W
authors.initials: JW
authors.lastname: Højfeldt
authors.forename: Carl J
authors.initials: CJ
authors.lastname: Arevang
authors.forename: William C
authors.initials: WC
authors.lastname: Pomerantz
authors.forename: Jessica K
authors.initials: JK
authors.lastname: Gagnon
authors.forename: Pamela J
authors.initials: PJ
authors.lastname: Schultz
authors.forename: Laura C
authors.initials: LC
authors.lastname: Cesa
authors.forename: Conor H
authors.initials: CH
authors.lastname: Doss
authors.forename: Steven P
authors.initials: SP
authors.lastname: Rowe
authors.forename: Victor
authors.initials: V
authors.lastname: Vásquez
authors.forename: Giselle
authors.initials: G
authors.lastname: Tamayo-Castillo
authors.forename: Tomasz
authors.initials: T
authors.lastname: Cierpicki
authors.forename: Charles L
authors.initials: CL
authors.lastname: Brooks
authors.forename: David H
authors.initials: DH
authors.lastname: Sherman
authors.forename: Anna K
authors.initials: AK
authors.lastname: Mapp
mesh_terms: D053630:Depsides / Q000737:chemistry* / Q000378:metabolism; D007783:Lactones / Q000737:chemistry* / Q000378:metabolism; D008958:Models, Molecular; D056004:Molecular Dynamics Simulation; D017434:Protein Structure, Tertiary; D012459:Salicylates / Q000737:chemistry* / Q000378:metabolism; D050880:p300-CBP Transcription Factors / Q000037:antagonists & inhibitors / Q000737:chemistry* / Q000235:genetics / Q000378:metabolism
chemical_list: D053630:Depsides; D007783:Lactones; D012459:Salicylates; C104417:lobaric acid; D050880:p300-CBP Transcription Factors