Effect of Inhibiting Histone Deacetylase with Short-Chain Carboxylic Acids and Their Hydroxamic Acid Analogs on Vertebrate Development and Neuronal Chromatin.
Effect of Inhibiting Histone Deacetylase with Short-Chain Carboxylic Acids and Their Hydroxamic Acid Analogs on Vertebrate Development and Neuronal Chromatin.
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DOI：
10.1021/ml1001954
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发表时间：
2010-10-08
影响因子：
4.2
通讯作者：
Haggarty, Stephen J.
中科院分区：
文献类型：
--
作者：
Fass, Daniel M.;Shah, Rishita;Ghosh, Balaram;Hennig, Krista;Norton, Stephanie;Zhao, Wen-Ning;Reis, Surya A.;Klein, Peter S.;Mazitschek, Ralph;Maglathlin, Rebecca L.;Lewis, Timothy A.;Haggarty, Stephen J.
将具有已知中枢神经系统和组蛋白脱乙酰酶（HDAC）抑制活性的羧酸转化为异羟肟酸，并使用一套重组HDAC亚型的体外生化测定、人宫颈癌Hela细胞和小鼠前脑原代培养物中基于细胞的测定以及整个动物（非洲爪蟾）发育测定进行测试。相对于母体羧酸，这些类似物中的两种表现出增强的效力，并且一种类似物在非洲爪蟾试验中显示出改变的HDAC同种型选择性和体内活性。我们讨论了这些新的异羟肟酸在研究中的潜在用途，旨在确定HDAC抑制剂作为记忆增强剂和情绪稳定剂的效用。
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.
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影响因子：
64.8
作者：
Hubbert, C;Guardiola, A;Yao, TP
通讯作者：
Yao, TP
影响因子：
14.8
作者：
Bradner, James E.;West, Nathan;Grachan, Melissa L.;Greenberg, Edward F.;Haggarty, Stephen J.;Warnow, Tandy;Mazitschek, Ralph
通讯作者：
Mazitschek, Ralph
DOI：
10.1111/j.1533-2500.2004.04304.x
发表时间：
2004-09-01
期刊：
Pain practice : the official journal of World Institute of Pain
影响因子：
--
作者：
Walia, Kulbir S;Khan, Elizabeth A;Khan, Yasin N
通讯作者：
Khan, Yasin N
影响因子：
11.4
作者：
Göttlicher, M;Minucci, S;Heinzel, T
通讯作者：
Heinzel, T
影响因子：
7.6
作者：
Kilgore, Mark;Miller, Courtney A.;Rumbaugh, Gavin
通讯作者：
Rumbaugh, Gavin