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Lavie-Cambot A.,CNRS Institute of Molecular Sciences | Lincheneau C.,CNRS Institute of Molecular Sciences | Lincheneau C.,Center for Synthesis and Chemical Biology | Cantuel M.,CNRS Institute of Molecular Sciences | And 3 more authors.
Chemical Society Reviews | Year: 2010

A strategy to manage energy, following light absorption, and modulate excited-state properties, including luminescence lifetimes of multicomponent photoactive systems, is presented. The intervening mechanism, which is illustrated through the use of bi-/multi-chromophoric molecules, relies on energy shuttling between different matched chromophores under kinetic and thermodynamic control. This tutorial review is destined to show supramolecular and materials chemists, spectroscopists and nanoscientists how to harness reversible electronic energy transfer in a predictable fashion in designer molecule-based systems. © 2010 The Royal Society of Chemistry. Source


Moccia M.,National Research Council Italy | Adamo M.F.A.,Center for Synthesis and Chemical Biology | Saviano M.,National Research Council Italy
Artificial DNA: PNA and XNA | Year: 2015

PNAs are emerging as useful synthetic devices targeting natural miRNAs. In particular 3 classes of structurally modified PNAs analogs are herein described, namely α, β and γ, which differ by their backbone modification. Their mode and binding affinity for natural nucleic acids and their use in medicinal chemistry as potential miRNA binders is discussed. © 2015 Taylor & Francis Group, LLC Source


Borgeson E.,UCD Conway Institute | Docherty N.G.,Trinity College Dublin | Murphy M.,UCD Conway Institute | Rodgers K.,UCD Conway Institute | And 6 more authors.
FASEB Journal | Year: 2011

Unresolved inflammation underlies the development of fibrosis and organ failure. Here, we investigate the potential of the proresolving eicosanoid lipoxinA 4 (LXA 4) and its synthetic analog benzo-LXA 4to prophylactically modulate fibrotic and inflammatory responses in a model of early renal fibrosis, unilateral ureteric obstruction (UUO). Male Wistar rats (Animalia, Chordata, Rattus norvegicus) were injected intravenously with vehicle (0.1% ethanol), LXA 4 (45 μg/250-g rat), or benzo-LXA 4 (15 μg/250-g rat) 15 min prior to surgery and sacrificed 3 d postligation. Renal gene and protein expression, collagen deposition, macrophage infiltration, and apoptosis were analyzed using manipulated kidneys from sham operations as control. Lipoxins (LXs) attenuated collagen deposition and renal apoptosis (P<0.05) and shifted the inflammatory milieu toward resolution, inhibiting TNF-α and IFN-γexpression, while stimulating proresolving IL-10. LXs attenuated UUO-induced activation of MAP kinases, Akt, and Smads (P<0.05) in injured kidneys. We explored whether the underlying mechanism reflected LX-induced modulation of fibroblast activation. Using cultured rat renal NRK-49F fibroblasts, we report that LXA 4 (1 nM) inhibits TGF-β1 (10 ng/ml)-induced activation of Smad2 and MAP-kinases (P<0.05), and furthermore, LXA 4 reduced TGF-β1-stimulated PAI-1 luciferase activation (P<0.05) relative to vehicle-stimulated cells. We propose that LXs may represent a potentially useful and novel therapeutic strategy for consideration in the context of renal fibrosis. © FASEB. Source


Bernard E.,Center for Synthesis and Chemical Biology | Bernard E.,Royal College of Surgeons in Ireland | Bernard E.,Medical Research Council | Buckley V.,Center for Synthesis and Chemical Biology | And 5 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2012

β-Hairpin peptidomimetics mimicking the interaction sites of the platelet receptor glycoprotein (GP)Ibα with von Willebrand factor (vWF) were synthesised and evaluated for their ability to increase platelet velocity under high shear conditions and to inhibit shear-induced platelet aggregation. A cyclic and bridged dodecapeptide 2e containing a heterochiral diproline motif was identified as a lead compound for the generation of a novel class of potential antiplatelet agents. © 2012 Elsevier Ltd. All rights reserved. Source


Barth C.,Center for Synthesis and Chemical Biology | Guiry P.J.,Center for Synthesis and Chemical Biology
Future Medicinal Chemistry | Year: 2012

Leukotriene B 3 and B 4 are part of an important class of signaling molecules - the leukotrienes, implicated in the inflammation process. Their pro-inflammatory effects have been widely recognized for almost three decades but it is only recently that their benefit in host defense has begun to be acknowledged. Their use as therapeutic agents is, unfortunately, limited by rapid metabolism. However, over the past 25 years, a number of stable leukotriene B 3 and B 4 analogues have been produced. In this review, we examine their medicinal chemistry and biological evaluation. © 2012 Future Science Ltd. Source

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