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组蛋白去乙酰化酶抑制剂:专利审查报告(2009-2011)。

Histone deacetylase inhibitors: a patent review (2009 - 2011).

机构信息

Seconda Università degli Studi di Napoli, Dipartimento di Patologia Generale, Italy.

出版信息

Expert Opin Ther Pat. 2013 Jan;23(1):1-17. doi: 10.1517/13543776.2013.736493. Epub 2012 Oct 25.

Abstract

INTRODUCTION

Given the involvement of histone deacetylases (HDACs) in regulation of gene expression, they are believed to be 'master regulators' of many diseases. Thus, HDAC inhibitors (HDACis) are able to modulate transcriptional activity. These molecules can induce cell cycle arrest, differentiation and apoptosis of tumor cells in culture and in animal models and therefore are emerging as an exciting new class of potential anti-cancer agents for the treatment of solid and hematological malignancies.

AREAS COVERED

The aim of this review is to provide an overview of current knowledge and molecular mechanisms of HDACis, and the most recent patents existing in the field of HDACis from 2009 until 2011.

EXPERT OPINION

In recent years, an increasing number of structurally diverse HDACis have been identified. In addition, non-cancer diseases, including neurodegeneration, metabolic, inflammatory and autoimmune disorders, infectious and cardiovascular diseases have also been proposed for an HDACi treatment. The growing body of evidence of the potential benefits of disease treatment based on the use of HDACis has led to a large number of patent applications throughout the world.

摘要

简介

鉴于组蛋白去乙酰化酶(HDACs)在基因表达调控中的作用,它们被认为是许多疾病的“主调控因子”。因此,HDAC 抑制剂(HDACi)能够调节转录活性。这些分子可以诱导肿瘤细胞在培养物和动物模型中的细胞周期停滞、分化和凋亡,因此作为一类有前途的新型潜在抗癌药物,正在治疗实体瘤和血液系统恶性肿瘤。

涵盖领域

本综述的目的是概述 HDACi 的现有知识和分子机制,以及 2009 年至 2011 年 HDACi 领域的最新专利。

专家意见

近年来,已经确定了越来越多种结构不同的 HDACi。此外,还提出了非癌症疾病,包括神经退行性疾病、代谢、炎症和自身免疫性疾病、传染病和心血管疾病,也可以使用 HDACi 进行治疗。基于使用 HDACi 治疗疾病的潜在益处的证据越来越多,导致全世界范围内提出了大量的专利申请。

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