Scientific Publications

Effect of Inhibiting Histone Deacetylase with Short-Chain Carboxylic Acids and Their Hydroxamic Acid Analogs on Vertebrate Development and Neuronal Chromatin.

Publication TypeJournal Article
AuthorsFass, DM, Shah R., Ghosh B., Hennig K., Norton S., Zhao WN, Reis SA, Klein PS, Mazitschek R., Maglathlin RL, Lewis TA, and Haggarty SJ
AbstractCarboxylic 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.
Year of Publication2010
JournalACS medicinal chemistry letters
Volume2
Issue1
Pages39-42
Date Published (YYYY/MM/DD)2010/10/08
DOI10.1021/ml1001954
PubMedhttp://www.ncbi.nlm.nih.gov/pubmed/21874153?dopt=Abstract