- Role of the CAI-1 fatty acid tail in the Vibrio cholerae quorum sensing response
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Quorum sensing is a mechanism of chemical communication among bacteria that enables collective behaviors. In V. cholerae, the etiological agent of the disease cholera, quorum sensing controls group behaviors including virulence factor production and biofilm formation. The major V. cholerae quorum-sensing system consists of the extracellular signal molecule called CAI-1 and its cognate membrane bound receptor called CqsS. Here, the ligand binding activity of CqsS is probed with structural analogues of the natural signal. Enabled by our discovery of a structurally simplified analogue of CAI-1, we prepared and analyzed a focused library. The molecules were designed to probe the effects of conformational and structural changes along the length of the fatty acid tail of CAI-1. Our results, combined with pharmacophore modeling, suggest a molecular basis for signal molecule recognition and receptor fidelity with respect to the fatty acid tail portion of CAI-1. These efforts provide novel probes to enhance discovery of antivirulence agents for the treatment of V. cholerae.
- Perez, Lark J.,Ng, Wai-Leung,Marano, Paul,Brook, Karolina,Bassler, Bonnie L.,Semmelhack, Martin F.
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supporting information
p. 9669 - 9681
(2013/01/16)
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- AMINE COMPOUND AND PHARMACEUTICAL USE THEREOF
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Provided is a novel amine compound represented by the following formula (I) having a superior peripheral blood lymphocyte decreasing action and superior in the immunosuppressive action, rejection suppressive action and the like, which shows decreased side effects of, for example, bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or a hydrate thereof, or a solvate thereof. wherein each symbol is as defined in the specification.
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Page/Page column 90-91
(2010/04/25)
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- 96. Synthesis of 1,3,4,5-tetrahydro-2-benzoxepin derivatives as conformationally restricted analogues of cyclamenaldehyde-type compounds and as intermediates for highly odour-active homologues
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Nine 1,3,4,5-tetrahydro-2-benzoxepin derivatives have been prepared as mimics of the folded (gauche) conformation of cyclamenaldehyde (1) and related compounds, but none of them showed the typical lily-of-the valley (muguet) odour activity. However, conversion of these substances to previously unknown analogues of 1 having a Me substituent on the aromatic ring in an ortho position to the side chain led to new fragrance substances with remarkable properties. The results indicate that the extended (anti) conformation is more likely to be the 'bioactive' one at the receptor site(s).
- Skouroumounis, Georges,Winter, Beat
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p. 1095 - 1109
(2007/10/03)
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