Document Detail


Sekikaic acid and lobaric acid target a dynamic interface of the coactivator CBP/p300.
MedLine Citation:
PMID:  23042634     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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:
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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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't     Date:  2012-10-08
Journal Detail:
Title:  Angewandte Chemie (International ed. in English)     Volume:  51     ISSN:  1521-3773     ISO Abbreviation:  Angew. Chem. Int. Ed. Engl.     Publication Date:  2012 Nov 
Date Detail:
Created Date:  2012-10-31     Completed Date:  2013-06-18     Revised Date:  2013-12-04    
Medline Journal Info:
Nlm Unique ID:  0370543     Medline TA:  Angew Chem Int Ed Engl     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  11258-62     Citation Subset:  IM    
Copyright Information:
Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
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MeSH Terms
Descriptor/Qualifier:
Depsides / chemistry*,  metabolism
Lactones / chemistry*,  metabolism
Models, Molecular
Molecular Dynamics Simulation
Protein Structure, Tertiary
Salicylates / chemistry*,  metabolism
p300-CBP Transcription Factors / antagonists & inhibitors,  chemistry*,  genetics,  metabolism
Grant Support
ID/Acronym/Agency:
F32 GM090550/GM/NIGMS NIH HHS; GM037554/GM/NIGMS NIH HHS; GM08597/GM/NIGMS NIH HHS; R01 CA140667/CA/NCI NIH HHS; R01 GM037554/GM/NIGMS NIH HHS; R01CA140667/CA/NCI NIH HHS; U01 TW007404/TW/FIC NIH HHS; UO1 TW007404/TW/FIC NIH HHS
Chemical
Reg. No./Substance:
0/Depsides; 0/Lactones; 0/Salicylates; 522-53-2/lobaric acid; EC 2.3.1.48/p300-CBP Transcription Factors
Comments/Corrections

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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