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Molecules 2015, 20(9), 17659-17674; doi:10.3390/molecules200917659

Small-Molecule Inhibitors of the Type III Secretion System

School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou 213164, China
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Author to whom correspondence should be addressed.
Academic Editor: Panayiotis A. Koutentis
Received: 16 July 2015 / Revised: 17 September 2015 / Accepted: 18 September 2015 / Published: 23 September 2015
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Abstract

Drug-resistant pathogens have presented increasing challenges to the discovery and development of new antibacterial agents. The type III secretion system (T3SS), existing in bacterial chromosomes or plasmids, is one of the most complicated protein secretion systems. T3SSs of animal and plant pathogens possess many highly conserved main structural components comprised of about 20 proteins. Many Gram-negative bacteria carry T3SS as a major virulence determinant, and using the T3SS, the bacteria secrete and inject effector proteins into target host cells, triggering disease symptoms. Therefore, T3SS has emerged as an attractive target for antimicrobial therapeutics. In recent years, many T3SS-targeting small-molecule inhibitors have been discovered; these inhibitors prevent the bacteria from injecting effector proteins and from causing pathophysiology in host cells. Targeting the virulence of Gram-negative pathogens, rather than their survival, is an innovative and promising approach that may greatly reduce selection pressures on pathogens to develop drug-resistant mutations. This article summarizes recent progress in the search for promising small-molecule T3SS inhibitors that target the secretion and translocation of bacterial effector proteins. View Full-Text
Keywords: type III secretion system; pathogens; small-molecule inhibitors; effector proteins; Gram-negative bacteria; virulence; antibacterial agents type III secretion system; pathogens; small-molecule inhibitors; effector proteins; Gram-negative bacteria; virulence; antibacterial agents
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Gu, L.; Zhou, S.; Zhu, L.; Liang, C.; Chen, X. Small-Molecule Inhibitors of the Type III Secretion System. Molecules 2015, 20, 17659-17674.

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