Journal
MOLECULES AND CELLS
Volume 28, Issue 5, Pages 447-453Publisher
KOREAN SOC MOLECULAR & CELLULAR BIOLOGY
DOI: 10.1007/s10059-009-0144-6
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Funding
- Korea Ministry of Environment [102-081-067]
- Korea Science and Engineering Foundation Korea government [R01-2007-000-20732-0]
- WCU (World Class University)
- Ministry of Education, Science and Technology [400-2008-0230]
- Research Team for Longevity Life Sciences in Pusan National University
- Korea Research Foundation Grant funded by the Korean Government (Ministry of Education and Human Resources Development) [KRF-2007-331-C00222]
- National Research Foundation of Korea Grant funded by the Korean Government [2009-0077238]
- National Research Foundation of Korea [2009-0077238, R01-2007-000-20732-0] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
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The quorum sensing (QS) inhibitors that antagonize TraR, a receptor protein for N-3-oxo-octanoyl-L-homoserine lactones (3-oxo-C8-HSL), a QS signal of Agrobacterium tumefaciens were developed. The structural analogues of 3-oxo-C8-HSL were designed by in silico molecular modeling using SYBYL packages, and synthesized by the solid phase organic synthesis (SPOS) method, where the carboxamide bond of 3-oxo-C8-HSL was replaced with a nicotinamide or a sulfonamide bond to make derivatives of N-nicotinyl-L-homoserine lactones or N-sulfonyl-L-homoserine lactones. The in vivo inhibitory activities of these compounds against QS signaling were assayed using reporter systems and compared with the estimated binding energies from the modeling study. This comparison showed fairly good correlation, suggesting that the in silico interpretation of ligand-receptor structures can be a valuable tool for the pre-design of better competitive inhibitors. In addition, these inhibitors also showed anti-biofilm activities against Pseudomonas aeruginosa.
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