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群体感应抑制剂:专利研究综述。

Quorum sensing inhibitors: a patent review.

机构信息

Shandong University, School of Pharmacy, Department of Medicinal Chemistry, Key Laboratory of Chemical Biology of Natural Products (MOE), Jinan, Shandong 250012, China.

出版信息

Expert Opin Ther Pat. 2013 Jul;23(7):867-94. doi: 10.1517/13543776.2013.779674. Epub 2013 Mar 19.

Abstract

INTRODUCTION

Quorum sensing (QS) is a cell-to-cell communication that regulates gene expression and coordinates their behavior in accordance with the cell population density as a result of discerning molecules termed autoinducers (AIs). The processes that QS governed include biofilm formation, bacterial virulence, antibiotic production, competence, conjugation, swarming motility and sporulation. Three main QS AIs are acyl-homoserine lactones, AI-2 and AI peptides. The attractive study of QS leads to an expansive number of QS inhibitors and approaches interfering with QS appearing.

AREAS COVERED

This review summarized the recent QS inhibitor-related patents published from 2009 to 2012. The authors have analyzed these patents and have provided an overview of QS inhibitors and their application.

EXPERT OPINION

The main strategies for QS inhibition related to the patents are disruption of the AI synthase, inactivation of the signal molecule, antagonism of the receptor and promotion of immune response to AI. Some of the natural or synthetic QS inhibitors display excellent activity to manipulate bacterial pathogenicity to offer significant potential in clinical therapy. However, more efforts are needed to be conducted to determine this form of communication to guide the development of QS inhibitors. Overall, QS is a suitable target for antimicrobial therapy and QS inhibitors are likely to lead to a renaissance of anti-virulence drugs without tolerance, which is the ultimate goal expected to achieve in this field.

摘要

简介

群体感应(QS)是一种细胞间通讯,通过辨别被称为自诱导物(AIs)的分子,根据细胞群体密度来调节基因表达并协调它们的行为。QS 调控的过程包括生物膜形成、细菌毒力、抗生素产生、感受态、共轭、群集运动和孢子形成。三种主要的 QS 诱导物是酰基高丝氨酸内酯、AI-2 和 AI 肽。QS 的诱人研究导致了大量的 QS 抑制剂和干扰 QS 的方法的出现。

涵盖领域

本文总结了 2009 年至 2012 年期间发表的与 QS 抑制剂相关的专利。作者对这些专利进行了分析,并对 QS 抑制剂及其应用进行了概述。

专家意见

与专利相关的 QS 抑制的主要策略是破坏 AI 合成酶、失活信号分子、拮抗受体和促进对 AI 的免疫反应。一些天然或合成的 QS 抑制剂对操纵细菌致病性表现出优异的活性,为临床治疗提供了巨大的潜力。然而,还需要做更多的工作来确定这种通讯形式,以指导 QS 抑制剂的开发。总的来说,QS 是抗菌治疗的一个合适目标,QS 抑制剂可能会导致抗毒力药物的复兴,而不会产生耐药性,这是该领域最终期望达到的目标。

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