Quorum sensing inhibitors: a patent review

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.

Keywords::

• acyl-homoserine lactones
• antibacterial
• autoinducer-2
• autoinducer peptides
• biofilm
• inhibitor
• quorum sensing

Declaration of interest

This project was funded by the National Natural Science Foundation of China (No 81001362), the PhD Program Foundation of Ministry of Education of China (No 20090131120080), the Doctoral Fund of Shandong Province (No BS2009SW011), the Shandong Natural Science Foundation (No JQ201019) and the Independent Innovation Foundation of Shandong University, IIFSDU (No 2010JQ005). The authors state no other conflicts of interest.

Notes

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