期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 2, 期 1, 页码 39-42出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml1001954
关键词
HDAC inhibitors; hydroxamic acid; valproate; butyrate; phenylbuty-rate; histone acetylation
资金
- National Cancer Institute's Initiative for Chemical Genetics, NIH [N01-CO-12400]
- NIH [1RO1MH58324]
- NIDA/NIH [5R01DA028301-02]
- Stanley Medical Research Institute
- NATIONAL INSTITUTE ON DRUG ABUSE [R01DA028301] Funding Source: NIH RePORTER
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 analogues exhibited enhanced potency, and one analogue 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.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据