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丙戊酸的分子特性、治疗潜力及毒性

Molecular and therapeutic potential and toxicity of valproic acid.

作者信息

Chateauvieux Sébastien, Morceau Franck, Dicato Mario, Diederich Marc

机构信息

Laboratoire de Biologie Moléculaire et Cellulaire du Cancer (LBMCC), Fondation de Recherche Cancer et Sang, Hôpital Kirchberg, Kirchberg 2540, Luxembourg.

出版信息

J Biomed Biotechnol. 2010;2010. doi: 10.1155/2010/479364. Epub 2010 Jul 29.

Abstract

Valproic acid (VPA), a branched short-chain fatty acid, is widely used as an antiepileptic drug and a mood stabilizer. Antiepileptic properties have been attributed to inhibition of Gamma Amino Butyrate (GABA) transaminobutyrate and of ion channels. VPA was recently classified among the Histone Deacetylase Inhibitors, acting directly at the level of gene transcription by inhibiting histone deacetylation and making transcription sites more accessible. VPA is a widely used drug, particularly for children suffering from epilepsy. Due to the increasing number of clinical trials involving VPA, and interesting results obtained, this molecule will be implicated in an increasing number of therapies. However side effects of VPA are substantially described in the literature whereas they are poorly discussed in articles focusing on its therapeutic use. This paper aims to give an overview of the different clinical-trials involving VPA and its side effects encountered during treatment as well as its molecular properties.

摘要

丙戊酸(VPA)是一种支链短链脂肪酸,被广泛用作抗癫痫药物和情绪稳定剂。其抗癫痫特性归因于对γ-氨基丁酸(GABA)转氨酶和离子通道的抑制作用。VPA最近被归类为组蛋白去乙酰化酶抑制剂,通过抑制组蛋白去乙酰化并使转录位点更易接近,直接作用于基因转录水平。VPA是一种广泛使用的药物,尤其用于患有癫痫的儿童。由于涉及VPA的临床试验数量不断增加,且取得了有趣的结果,该分子将被应用于越来越多的治疗方法中。然而,VPA的副作用在文献中有大量描述,而在专注于其治疗用途的文章中却很少被讨论。本文旨在概述涉及VPA的不同临床试验、治疗期间遇到的副作用及其分子特性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d66d/2926634/fb109c909522/JBB2010-479364.001.jpg

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