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Peer Reviewed
See detailDevelopment of original pyridinic analogues of nimesulide as cycloxygenase inhibitors
Renard, Jean-François ULg; de Leval, Xavier; Pirotte, Bernard ULg

Conference (2007, October)

Detailed reference viewed: 7 (1 ULg)
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See detailDevelopment of paleoseismic trench logging and dating techniques: a case study on the Central North Anatolian Fault
Fraser, Jeff; Pigati, J.S.; Hubert, Aurelia ULg et al

in Geophysical Research Abstracts (2007, April), 9

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See detailDEVELOPMENT OF PHARMACOLOGICAL TOOLS FOR THE IDENTIFICATION OF G PROTEIN-COUPLED RECEPTORS LIGANDS
Gilissen, Julie ULg

Doctoral thesis (2016)

G protein-coupled receptors (GPCRs) represent the protein family most successfully targeted for treating human diseases. They couple to G proteins to mobilize second messenger pathways that lead to ... [more ▼]

G protein-coupled receptors (GPCRs) represent the protein family most successfully targeted for treating human diseases. They couple to G proteins to mobilize second messenger pathways that lead to cellular responses and ultimately to physiological changes. However many are poorly characterized with few ligands reported or remain completely orphans. Therefore, there is a growing need for screening-compatible and sensitive assays in order to identify new ligands. The present project aims at developing pharmacological tools to characterize the pharmacology and physiology of GPCRs. Our approach rely on i) development of receptor models and assays for the identification of ligands, ii) screening of chemical and virtual small molecules libraries and iii) analysis of structure-activity relationships study of active molecules. The project has been divided in two parts. To set-up assays for the evaluation of GPCRs activation, we selected the understudied succinate receptor 1 (SUCNR1) that is proposed to affect cellular metabolism and pathophysiology of diseases in multiple organs. Nevertheless the receptor has never been validated as a drug target because very few ligands have been described. So, developing pharmacological tools for SUCNR1 remains of great interest in therapeutic drug discovery. First, we have started by examining SUCNR1 signaling pathways in HEK293 cells. Our investigations have highlighted the efficient coupling to Gαi and thus the negative modulation of intracellular cAMP levels. Consequently we have implemented an assay sensitive to cAMP variations to identify ligands able to induce SUCNR1 activation. However, an important drawback to track agonists for Gαi-coupled receptors is the mandatory stimulation of cAMP levels. Inducers such as forskolin must be used and are sources of variations and errors. In order to avoid these artifacts we have set-up and validated a cAMP-inducer free method based on the GloSensor biosensor. This real time assay was amenable to high-throughput screening for the detection of Gαi-coupled receptors agonists. The strategy monitoring basal cAMP levels compared to the stimulated cAMP levels allowed to decrease recording time and artifcats from forskolin use, leading to the identification of fewer false positives and unidentified false negatives. Although both methods found agonists in the chemical library screened, no active new scaffolds on SUCNR1 were discovered. We infer that this method could facilitate the study and screening of Gαi-coupled receptors for active ligands. Secondly, given the interesting potential of SUCNR1 for promising therapeutic advances, we have carried out the study of the receptor interaction with its natural ligand, succinate. We have optimized the previous three-dimensional model for SUCNR1 binding pocket by means of more detailed structure-activity relationships study of succinate related molecules. The study of structure-activity relationships performed by Pierre Geubelle, in parallel to this work, allowed the deduction of the structural elements required to be active on SUCNR1. Thus we have defined a pharmacophore for activity on the receptor and subsequently evaluated various cycloalkanes. With our cAMP assay, Pierre Geubelle has highlighted the (1R, 2S)-1,2-cyclopropanedicarboxylate to be able to activate SUCNR1. We confirmed the activity of this compound on SUCNR1 capacity to recruit arrestin 3 and determined the pharmacological properties of this new ligand as SUCNR1 agonist, in vitro and in vivo. To confirm our in vitro results, we have also assessed the hypertensive properties of this cyclic analogue. Intravenous addition at the dose of 0.1 mg.kg-1 in rats has been demonstrated to increase blood pressure in the same range as succinate. Consequently we have demonstrated that (1R, 2S)-1,2-cyclopropanedicarboxylate could be regarded as an original synthetic full agonist for SUCNR1. In addition, the pharmacophore for SUCNR1 should help to generate synthetic compounds characterized by an increased potency and/or efficacy compared to succinate. [less ▲]

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See detailDevelopment of photo- or thermo-reversible cross-linked recyclable shape-memory materials
Defize, Thomas ULg; Riva, Raphaël ULg; Thomassin, Jean-Michel ULg et al

Conference (2015, September 01)

Shape-memory polymers (SMPs) are remarkable materials able to switch from a stressed deformed state (temporary shape) to their initial relaxed state (permanent shape) by the application of a stimulus ... [more ▼]

Shape-memory polymers (SMPs) are remarkable materials able to switch from a stressed deformed state (temporary shape) to their initial relaxed state (permanent shape) by the application of a stimulus, such as heat or light. Typically, the shape-memory property is generally observed for chemically or physically cross-linked polymers that exhibit an elastomeric behavior above a phase transition, e.g. glass or melting transition. As an example, cross-linked semi-crystalline poly(ε-caprolactone) (PCL) is widely studied for the development of SMPs. As most of SMPs are irreversibly cross-linked material, their reprocessing is impossible preventing any recycling. Thereby, reversible reactions, allowing the formation/cleavage of the network, raise tremendous interest for the development of new SMPs. Recently, we reported the preparation reversibly cross-linked PCL-based SMP using the Diels-Alder (DA) reaction between furan and maleimide end-groups of 4-arm star-shaped PCL, well-known to create reversible bonds. After implementation, this shape-memory material was demonstrated to be recyclable, and was characterized by excellent fixity and recovery before and after recycling experiments. However, the relatively low retro DA temperature of the furan-maleimide adducts led to an inelastic deformation during shape-memory tensile cycles. In order to get rid of this drawback, an alternative approach was investigated. The substitution of the DA reaction by a photo-reversible reaction, typically the photo-induced (2+2) cycloaddition of coumarins, was proposed to prepare cross-linked PCL matrix presenting one-way and two-way memory properties, since photolabile adducts are supposed to be stable during shape-memory tensile cycles. [less ▲]

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Peer Reviewed
See detailDevelopment of pH–responsive nanocarriers using trimethylchitosans and methacrylic acid copolymer for siRNA delivery
Dehousse, Vincent ULg; Garbacki, Nancy ULg; Colige, Alain ULg et al

in Biomaterials (2010), 31

RNA interference-based therapies are dependent on intracellular delivery of siRNA. The release of siRNA from the endosomal compartment may be a rate limiting step in the transfection process. The purpose ... [more ▼]

RNA interference-based therapies are dependent on intracellular delivery of siRNA. The release of siRNA from the endosomal compartment may be a rate limiting step in the transfection process. The purpose of this study was to produce pH–responsive nanocarriers made of trimethylchitosan (TMC). To this end, pHsensitive methacrylic acid (MAA) copolymer was added to TMC–siRNA formulations. Four different TMCs associated or not with MAA were evaluated as siRNA carriers. Nanoparticles were characterized in terms of size, surface charge, morphology and interaction with siRNA. A swelling behaviour due to a decrease in pH was observed and was found to be dependent on MAA content in the complexes. In vitro experiments aimed at evaluating how the capacity of the nanocarriers to transfect siRNA in L929 cells was affected by MAA content. Confocal microscopy experiments showed that fluorescent MAA-containing particles exhibit a different distribution pattern inside the cells comparing to their counterpart without this pH-sensitive polymer. Transfection efficiency was investigated by RhoA mRNA expression inhibition. MAA–TMC–siRNA complexes were able to transfect L929 cells with greater efficiency than corresponding TMC–siRNA complexes. This study gives an insight into the opportunity of pH-sensitive nanocarriers for siRNA delivery. Such formulations may represent an attractive strategy to improve endosomal escape of siRNA. [less ▲]

Detailed reference viewed: 61 (21 ULg)
Peer Reviewed
See detailDevelopment of pilot Trans-European service (Rhine-Main-Danube) for combined freight transport between Walloon region and the Black Sea
Marchal, Jean ULg; Kicheva, D.; Petkov, N. et al

in Eigth international conference on Marine sciences and Technologies “Balack Sea 2006” (2006, September)

Detailed reference viewed: 21 (0 ULg)
Peer Reviewed
See detailDevelopment of Procedural Learning in Children : The “Toy Task”
Lejeune, Caroline ULg; Meulemans, Thierry ULg

Poster (2008)

The authors generally agree that procedural learning abilities play an important role in the child development and that they are present early in childhood. However, few studies have been carried out in ... [more ▼]

The authors generally agree that procedural learning abilities play an important role in the child development and that they are present early in childhood. However, few studies have been carried out in this area because of the difficulty to develop tests specifically designed for the evaluation of these capacities in young children. In this study, we presented a new task aimed to evaluate visuo-motor skill learning in the young child. The purpose of the present study was to explore whether procedural learning abilities are present in the same extent in 4-year as 7- and 10-year-old children. Our sample is composed of 60 children divided into 3 age-groups. The task is composed of 5 blocks of 12 trials during which each subject has to use a reversed mouse of a computer in order to “catch” different toys appearing on the screen; 2 blocks of 12 trials was administered after a 15 minutes delay. Our results show an important difference between the groups for the first block; on the other hand, for the next blocks, the results show an absence of age-related difference between participants in our perceptive-motor skill learning task, confirming the idea according to which procedural learning abilities are efficient early in development (the difference observed during the first block being probably due to the intervention of executive mechanisms). [less ▲]

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See detailDevelopment of process control system for potential use of direct injection spraying technology
Aissaoui, Abdellah; Lebeau, Frédéric ULg; el bahir, et al

in Progress in Agricultural Engineering Sciences (2011), 7(1), 33-45

Small-scale farmers face to actual difficulties of applying pesticides accurately and safely on vegetables crops. They mainly use hand operated sprayers. As an issue, a small direct injection system based ... [more ▼]

Small-scale farmers face to actual difficulties of applying pesticides accurately and safely on vegetables crops. They mainly use hand operated sprayers. As an issue, a small direct injection system based on a five meter’s parallel boom layout was designed to improve chemical application. The boom layout was optimized to obtain the same minimal time lag response for the ten nozzles. The dynamic of the system was modeled using Simulink TM as first order model with delay. Two control strategies were implemented using PID (Proportional Integral Derivative) feedback control loops to monitor tracer injection (fluorescing) proportionally to simulated forward speed (from 0.6 to 1.2 m/s) and to control the constant operating pressure (constant carrier flow strategy) or the variable operating pressure proportionally to the injected chemical amount (variable total flow strategy). Different forward speed changes were induced using steps up and down, ramps, sine waves and sweeps excitations to evaluate the control feedback. The system stability was tested for its ability to maintain the expected concentration and application rate. The results show that the time lag remains less than 3 s (dead time < 2 s, time constant < 1 s) and the system keeps stable for the maximal speed variation (ΔV) and acceleration (ā) tested (ΔV = 200%, ā = 0.48 m/s2) which induce less than 10% variation of application rate. [less ▲]

Detailed reference viewed: 61 (21 ULg)
See detailDevelopment of products for GNSS users at the Belgian Solar-Terrestrial Centre of Excellence
Warnant, René ULg; Lejeune, Sandrine; Stankov, Stanimir et al

Conference (2008, December)

Detailed reference viewed: 117 (22 ULg)