Document Detail


Effect of Inhibiting Histone Deacetylase with Short-Chain Carboxylic Acids and Their Hydroxamic Acid Analogs on Vertebrate Development and Neuronal Chromatin.
MedLine Citation:
PMID:  21874153     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
Carboxylic acids with known central nervous system and histone deacetylase (HDAC) inhibitory activities were converted to hydroxamic acids and tested using a suite of in vitro biochemical assays with recombinant HDAC isoforms, cell based assays in human cervical carcinoma Hela cells and primary cultures from mouse forebrain, and a whole animal (Xenopus laevis) developmental assay. Relative to the parent carboxylic acids, two of these analogs exhibited enhanced potency, and one analog showed altered HDAC isoform selectivity and in vivo activity in the Xenopus assay. We discuss potential uses of these novel hydroxamic acids in studies aimed at determining the utility of HDAC inhibitors as memory enhancers and mood stabilizers.
Authors:
Daniel M Fass; Rishita Shah; Balaram Ghosh; Krista Hennig; Stephanie Norton; Wen-Ning Zhao; Surya A Reis; Peter S Klein; Ralph Mazitschek; Rebecca L Maglathlin; Timothy A Lewis; Stephen J Haggarty
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Publication Detail:
Type:  JOURNAL ARTICLE    
Journal Detail:
Title:  ACS medicinal chemistry letters     Volume:  2     ISSN:  1948-5875     ISO Abbreviation:  -     Publication Date:  2010 Oct 
Date Detail:
Created Date:  2011-8-29     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101521073     Medline TA:  ACS Med Chem Lett     Country:  -    
Other Details:
Languages:  ENG     Pagination:  39-42     Citation Subset:  -    
Affiliation:
Stanley Center for Psychiatric Research, Broad Institute of Harvard and MIT, 7 Cambridge Center, Cambridge, MA 02142, USA.
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Grant Support
ID/Acronym/Agency:
R01 DA028301-01//NIDA NIH HHS; R01 DA028301-02//NIDA NIH HHS; R01 DA028301-03//NIDA NIH HHS

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