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Solid-Phase synthesis and biological evaluation of N-dipeptido L-homoserine lactones as quorum sensing activators

หน่วยงาน Nanyang Technological University, Singapore

รายละเอียด

ชื่อเรื่อง : Solid-Phase synthesis and biological evaluation of N-dipeptido L-homoserine lactones as quorum sensing activators
นักวิจัย : Hansen, Mette R. , Le Quement, Sebastian T. , Jakobsen, Tim H. , Skovstrup, Søren , Taboureau, Olivier , Tolker-Nielsen, Tim , Givskov, Michael , Nielsen, Thomas E.
คำค้น : DRNTU::Science::Biological sciences
หน่วยงาน : Nanyang Technological University, Singapore
ผู้ร่วมงาน : -
ปีพิมพ์ : 2557
อ้างอิง : Hansen, M. R., Le Quement, S. T., Jakobsen, T. H., Skovstrup, S., Taboureau, O., Tolker-Nielsen, T., et al. (2014). Solid-Phase Synthesis and Biological Evaluation of N -Dipeptido L -Homoserine Lactones as Quorum Sensing Activators . ChemBioChem, 15(3), 460-465. , 1439-4227 , http://hdl.handle.net/10220/19692 , http://dx.doi.org/10.1002/cbic.201300533
ที่มา : -
ความเชี่ยวชาญ : -
ความสัมพันธ์ : ChemBioChem
ขอบเขตของเนื้อหา : -
บทคัดย่อ/คำอธิบาย :

Bacteria use small signaling molecules to communicate in a process termed “quorum sensing” (QS), which enables the coordination of survival strategies, such as production of virulence factors and biofilm formation. In Gram-negative bacteria, these signaling molecules are a series of N-acylated L-homoserine lactones. With the goal of identifying non-native compounds capable of modulating bacterial QS, a virtual library of N-dipeptido L-homoserine lactones was screened in silico with two different crystal structures of LasR. The 30 most promising hits were synthesized on HMBA-functionalized PEGA resin and released through an efficient acid-mediated cyclative release mechanism. Subsequent screening for modulation of QS in Pseudomonas aeruginosa and E. coli identified six moderately strong activators. A follow-up library designed from the preliminary derived structure–activity relationships was synthesized and evaluated for their ability to activate the QS system in this bacterium. This resulted in the identification of another six QS activators (two with low micromolar activity) thus illuminating structural features required for QS modulation.

บรรณานุกรม :
Hansen, Mette R. , Le Quement, Sebastian T. , Jakobsen, Tim H. , Skovstrup, Søren , Taboureau, Olivier , Tolker-Nielsen, Tim , Givskov, Michael , Nielsen, Thomas E. . (2557). Solid-Phase synthesis and biological evaluation of N-dipeptido L-homoserine lactones as quorum sensing activators.
    กรุงเทพมหานคร : Nanyang Technological University, Singapore.
Hansen, Mette R. , Le Quement, Sebastian T. , Jakobsen, Tim H. , Skovstrup, Søren , Taboureau, Olivier , Tolker-Nielsen, Tim , Givskov, Michael , Nielsen, Thomas E. . 2557. "Solid-Phase synthesis and biological evaluation of N-dipeptido L-homoserine lactones as quorum sensing activators".
    กรุงเทพมหานคร : Nanyang Technological University, Singapore.
Hansen, Mette R. , Le Quement, Sebastian T. , Jakobsen, Tim H. , Skovstrup, Søren , Taboureau, Olivier , Tolker-Nielsen, Tim , Givskov, Michael , Nielsen, Thomas E. . "Solid-Phase synthesis and biological evaluation of N-dipeptido L-homoserine lactones as quorum sensing activators."
    กรุงเทพมหานคร : Nanyang Technological University, Singapore, 2557. Print.
Hansen, Mette R. , Le Quement, Sebastian T. , Jakobsen, Tim H. , Skovstrup, Søren , Taboureau, Olivier , Tolker-Nielsen, Tim , Givskov, Michael , Nielsen, Thomas E. . Solid-Phase synthesis and biological evaluation of N-dipeptido L-homoserine lactones as quorum sensing activators. กรุงเทพมหานคร : Nanyang Technological University, Singapore; 2557.