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See detailA new proposal of a simple model for the lateral-torsional buckling of unrestrained steel I-beams in case of fire: experimental and numerical validation
Vila Real, Paolo; Piloto, Paolo; Franssen, Jean-Marc ULg

in Journal of Constructional Steel Research (2003), 59(2), 179-199

The behaviour of Steel I-Beams exhibiting lateral-torsional buckling at elevated temperature has been studied by means of experimental and numerical analysis. The authors in an earlier paper have ... [more ▼]

The behaviour of Steel I-Beams exhibiting lateral-torsional buckling at elevated temperature has been studied by means of experimental and numerical analysis. The authors in an earlier paper have presented an analytical formula for the buckling resistance moment in the fire design situation. This new proposal, different from the actual proposal of the Eurocode 3 Part 1.2 has been validated in this work by comparison with the results from a set of 120 experimental and numerical tests performed on IPE 100 beams, submitted to temperatures varying from room temperature to 600 degreesC. The numerical simulations have been based on the measured geometrical dimensions of the cross-sections, the longitudinal imperfections, i.e. the out of straightness of the beams, the residual stresses and the yield strength. The Eurocode simple model promotes ultimate loads that depend mainly on the non-dimensional slenderness of the beams. The analytical results provided by the Eurocode 3, for a certain range of the slenderness, appear to be unsafe when compared with the numerical and experimental results. It is shown that the new proposal is safer than the Eurocode 3 formulas. (C) 2002 Elsevier Science Ltd. All rights reserved. [less ▲]

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See detailNew proposals for the design of Steel-Beam-Colums under fire conditions
Lopes, Nuno; Vila Real, P. M. M.; Simoes da Silva, Luis et al

in Franssen, Jean-Marc; Benichou; Kodur (Eds.) et al Proceedings of SiF'04: Third International Structures in Fire workshop (2004)

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See detailNew prospects for the grafting of functional groups onto aliphatic polyesters. Ring-opening polymerization of alpha- or gamma-substituted epsilon-caprolactone followed by chemical derivatization of the substituents
Lecomte, Philippe ULg; Riva, Raphaël ULg; Schmeits, Stephanie ULg et al

in Macromolecular Symposia (2006), 240

Recent progress in the synthesis of aliphatic polyesters, substituted by pendent functional groups, has been reviewed. Two main strategies have to be distinguished. The first route consists of the ring ... [more ▼]

Recent progress in the synthesis of aliphatic polyesters, substituted by pendent functional groups, has been reviewed. Two main strategies have to be distinguished. The first route consists of the ring-opening polymerization of F,caprolactone substituted by various functional groups, protected if needed, in alpha- or gamma-position. In a second strategy, the functional groups are grafted onto preformed polyesters chains in alpha-position of the carbonyl groups. alpha-chloro-epsilon-caprolactone is quite an interesting monomer because, after polymerization, the activated chloride can be easily derivatized by atom transfer radical addition and "click" chemistry, respectively. Similarly, gamma-acrylic-epsilon-caprolactone is precursor of (co)polyesters wellsuited to derivatization of the pendent double bonds by Michael addition. [less ▲]

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See detailNew prospects in flame retardant polymer materials: From fundamentals to nanocomposites
Laoutid, Fouad; Bonnaud, Leïla; Alexandre, Michaël ULg et al

in Materials Science & Engineering : R (2009), 63(3), 100-125

The objective of this review is to make the field of “flame retardants for polymer materials” more accessible to the materials science community, i.e. chemists, physicists and engineers. We present the ... [more ▼]

The objective of this review is to make the field of “flame retardants for polymer materials” more accessible to the materials science community, i.e. chemists, physicists and engineers. We present the fundamentals of polymer combustion theory, the main flame retardant properties and tests used to describe fire behavior, together with the nature and modes of action of the most representative flame retardants and the synergistic effects that can be achieved by combining them. We particularly focus on polymer nanocomposites, i.e. polymer matrices filled with specific, finely dispersed nanofillers, which will undoubtedly pave the way for future materials combining physicochemical and thermo-mechanical performances with enhanced flame retardant behavior. [less ▲]

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See detailNew prospects in the roles of the C-terminal domains of VEGF-A and their cooperation for ligand binding, cellular signaling and vessels formation.
Delcombel, Romain ULg; Janssen, Lauriane ULg; Vassy, Roger et al

in Angiogenesis (2013), 16(2), 353-71

VEGF-A is a crucial growth factor for blood vessel homeostasis and pathological angiogenesis. Due to alternative splicing of its pre-mRNA, VEGF-A is produced under several isoforms characterized by the ... [more ▼]

VEGF-A is a crucial growth factor for blood vessel homeostasis and pathological angiogenesis. Due to alternative splicing of its pre-mRNA, VEGF-A is produced under several isoforms characterized by the combination of their C-terminal domains, which determines their respective structure, availability and affinity for co-receptors. As controversies still exist about the specific roles of these exon-encoded domains, we systematically compared the properties of eight natural and artificial variants containing the domains encoded by exons 1-4 and various combinations of the domains encoded by exons 5, 7 and 8a or 8b. All the variants (VEGF(111)a, VEGF(111)b, VEGF(121)a, VEGF(121)b, VEGF(155)a, VEGF(155)b, VEGF(165)a, VEGF(165)b) have a similar affinity for VEGF-R2, as determined by Surface plasmon resonance analyses. They strongly differ however in terms of binding to neuropilin-1 and heparin/heparan sulfate proteoglycans. Data indicate that the 6 amino acids encoded by exon 8a must be present and cooperate with those of exons 5 or 7 for efficient binding, which was confirmed in cell culture models. We further showed that VEGF(165)b has inhibitory effects in vitro, as previously reported, but that the shortest VEGF variant possessing also the 6 amino acids encoded by exon 8b (VEGF(111)b) is remarkably proangiogenic, demonstrating the critical importance of domain interactions for defining the VEGF properties. The number, size and localization of newly formed blood vessels in a model of tumour angiogenesis strongly depend also on the C-terminal domain composition, suggesting that association of several VEGF isoforms may be more efficient for treating ischemic diseases than the use of any single variant. [less ▲]

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See detailNew proteins involved in cellular invasion
Paupert, Jenny ULg; Monferran, Sylvie; Dauvillier, Stéphanie et al

Conference (2005)

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See detailNew pyridinic analogues of nimesulide as potent COXs inhibitors.
Renard, Jean-François ULg; Garbacki, Nancy ULg; de Leval, Xavier et al

Poster (2008)

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See detailNew Pyridobenzodiazepine Derivatives as Potential Antipsychotics: Synthesis and Neurochemical Study
Liégeois, Jean-François ULg; Bruhwyler, J.; Damas, Jacques ULg et al

in Journal of Medicinal Chemistry (1993), 36(15), 2107-14

The discovery of a new, safe, atypical antipsychotic remains an important challenge. To achieve this goal, a series of N-methylpiperazinopyrido[2,3-b] [1,4]- and -[1,5]- and -pyrido[4,3-b][1,4]- and -[1,5 ... [more ▼]

The discovery of a new, safe, atypical antipsychotic remains an important challenge. To achieve this goal, a series of N-methylpiperazinopyrido[2,3-b] [1,4]- and -[1,5]- and -pyrido[4,3-b][1,4]- and -[1,5]- benzodiazepines were synthesized. The dopaminergic (D1, D2), serotonergic (5-HT2), and cholinergic (M) affinities, frequently remarked in the action mechanisms of antipsychotic drugs, were determined using their respective in vitro receptor binding assays. All affinities were reduced for each compound. Optimal substituents were found to be in the 2- or 8-position for the retention of affinities, while substitution at the 5-position by acyl or alkyl groups dramatically diminished binding affinities. Pyridobenzodiazepine derivatives, such as clozapine, were found to be inactive or only weakly effective against apomorphine-mediated stereotypes in rats. In an original and complex behavioral model developed in dogs and successfully used to differentiate distinct classes of psychotropic drugs and to discriminate between typical and atypical neuroleptic drugs, 8-chloro-6-(4-methyl-1-piperazinyl)-11H-pyrido[2,3-b] [1,4]benzodiazepine (9), 8-methyl-6-(4-methyl-1-piperazinyl)-11H-pyrido [2,3-b][1,4]benzodiazepine (12), and 5-(4-methyl-1-piperazinyl)-11H-pyrido[2,3-b][1,5]benzodiazepine (16) showed most of the behavioral characteristics previously described for neuroleptics. Their neurochemical profiles, particularly their 5-HT2/D2 pKi ratios, were compatible with an atypical antipsychotic effect. These compounds were selected for further investigation. The proposed modulations could lead to new possibilities for the pharmacochemistry of diarylazepines. [less ▲]

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See detailNew pyridobenzodiazepine derivatives: Modifications of the basic side chain differentially modulate binding to dopamine (D-4.2, D-2L) and serotonin (5-HT2A) receptors
Liégeois, Jean-François ULg; Eyrolles, L.; Ellenbroek, B. A. et al

in Journal of Medicinal Chemistry (2002), 45(23), 5136-5149

A series of new pyridobenzodiazepines with variation of the basic side chain were synthesized and evaluated for their binding to D-4.2, D-2L, and 5-HT2A receptors in comparison with clozapine, haloperidol ... [more ▼]

A series of new pyridobenzodiazepines with variation of the basic side chain were synthesized and evaluated for their binding to D-4.2, D-2L, and 5-HT2A receptors in comparison with clozapine, haloperidol, and two parent compounds previously described, 8-chloro-6-(4-methyl-1-piperazinyl)-11H-pyrido[2,3-b][1,4]benzodiazepine (8) and 8-methyl-6-(4-methyl-1-piperazinyl)-11H-pyrido[2,3-b][1,4]benzodiazepine (9). In the piperazine series, replacing the N-methyl group by a N-phenyl moiety (15-17, 30-32) provided a dramatic decrease of affinity for all receptors (K-i > 1000 nM). A N-cyclohexyl group (20, 35) restored some affinity. Compounds with a N-benzyl (18, 33) or N-phenethyl side chain (19, 34) had significant affinities at D-4.2 and 5-HT2A receptors. Homologation of the piperazine nucleus (29, 44) led to a significant decrease of the affinity at all receptors investigated. In the 4-aminopiperidine series, N-methyl derivatives (21, 36) possessed less affinity in comparison with the N-metbylpiperazine analogues (8, 9) while the N-benzyl congeners (22, 37) showed similar affinities. The rigidification of piperidine nucleus as obtained in azabicyclo [3.2.1] octane derivatives (23, 38) involved a slight reduction of the affinity at D-4.2 and 5-HT2A receptors while the affinity at D-2L receptors was dramatically increased. The introduction of N-substituted aminoalkylamines to replace N-methylpiperazine generally led to a significant decrease in the affinity for D-4.2 receptors but some of these molecules (24, 25, 41) presented a significant 5-HT2A binding affinity. The presence of a more flexible side chain induced an increased conformational freedom. Consequently, the preferential position of the distal nitrogen or its basicity in piperazine derivatives was greatly modified. 19 with a high D-4.2 and 5-HT2A affinity (K-i = 40 and 103 nM, respectively) did not induce cataleptic phenomenon in the paw test in rats but significantly reduced the immobility time in Porsolt's test in mice suggesting antidepressant properties. [less ▲]

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See detailNew pyridobenzoxazepine derivatives derived from 5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine (JL13): chemical synthesis and pharmacological evaluation
Liégeois, Jean-François ULg; Deville, Marine; Dilly, Sébastien ULg et al

in Journal of Medicinal Chemistry (2012), 55(1572), 1582

A series of new pyridobenzoxazepine derivatives with various heterocyclic amine side chains were synthesized in order to explore two main parameters related to the distal basic nitrogen. These compounds ... [more ▼]

A series of new pyridobenzoxazepine derivatives with various heterocyclic amine side chains were synthesized in order to explore two main parameters related to the distal basic nitrogen. These compounds were tested for their affinity for dopamine D2L, D4, serotonin 5-HT1A, 5-HT2A and adrenergic 2A receptors in comparison with 5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine, JL13 (1) and other diarylazepine derivatives. In terms of multi-receptor target strategy, 2 and 5 present the most promising in vitro binding profile. Bulky, polar and more flexible side chains are not favourable in this context. 2 and 5 were tested in adult rats to evaluate their long-term effects on dopamine and serotonin receptors density in different brain areas. Similar to 1 and other second-generation antipsychotic drugs, repeated treatment with 2 significantly increased D1 and D4 receptors in nucleus accumbens and caudate putamen, and D2 receptors in medial prefrontal cortex and hippocampus while 5 significantly increased D2 and D4 receptors in nucleus accumbens. In addition, 2 increased 5-HT1A and decreased 5-HT2A receptors in cerebral cortex. In contrast, 5 did not alter levels of any 5-HT receptor subtype in any brain region examined. These results encourage further development of 2 as a novel second-generation antipsychotic agent. [less ▲]

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See detailNew quadrangular shell element in SAFIR
Talamona, Didier; Franssen, Jean-Marc ULg

in Franssen, Jean-Marc (Ed.) Proceedings of the 1st International Structures in Fire workshop (2000)

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See detailA New Quicklook Optical Processor with Digital Input/Output
Litovchenko, Konstantin Ts.; Lemaire, Philippe; Barbier, Christian ULg

in Proceedings IGARSS'96 Symposium (1996)

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See detailNew quinazolinones structurally related to diazoxide and pinacidil as potential KATP channel openers
Somers, F.; Ouedraogo, R.; De Tullio, Pascal ULg et al

Conference (1998, February 14)

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See detailNew quinazolinones structurally related to diazoxide and pinacidil as potential KATP channel openers
Somers, F.; Ouedraogo, R.; De Tullio, Pascal ULg et al

in Fundamental & Clinical Pharmacology (1998), 12

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See detailNew R/S-3,4-dihydro-2,2-dimethyl-2H-1-benzopyrans as KATP channel openers: modulation of the 4-position
Florence, Xavier ULg; Sebille, Sophie; De Tullio, Pascal ULg et al

in Bioorganic & Medicinal Chemistry (2009), 17

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See detailNew radiocarbon dates for the Zagros Aurignacian from Yafteh cave, Iran
Otte, Marcel ULg; Shidrang, Sonia; Zwyns, Nicolas et al

in Journal of Human Evolution (2011), 61(3), 340-346

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See detailNew radioiodinated carboxylic and hydroxamic matrix metalloproteinase inhibitor tracers as potential tumor imaging agents
Oltenfreiter, R.; Staelens, L.; Lejeune, Annabelle ULg et al

in Nuclear Medicine & Biology (2004), 31(4), 459-468

Several studies have demonstrated a positive correlation between tumor progression and expression of extracellular proteinases such as matrix metalloproteinases (MMPs). MMP-2 and MMP-9 have become ... [more ▼]

Several studies have demonstrated a positive correlation between tumor progression and expression of extracellular proteinases such as matrix metalloproteinases (MMPs). MMP-2 and MMP-9 have become attractive targets for cancer research because of their increased expression in human malignant tumor tissues of various organs, providing a target for medical imaging techniques. Radioiodinated carboxylic and hydroxamic MMP inhibitors 2-(4'-[123]iodo-biphenyl-4-sulfonylainino)-3-(1H-indol-3-yl)-propionic acid (9) and 2-(4'-[I-123] iodo-biphenyl-4-sulfonylamino)-3-(1H-indol-3-yl)-propionamide (11) were synthesized by electrophilic aromatic substitution of the tributylstannyl derivatives and resulted in radiochemical yields of 60% +/- 5% (n - 3) and 70% +/- 5% (n = 6), respectively. In vitro zymography and enzyme assays showed high inhibition capacities of the inhibitors on gelatinases. In vivo biodistribution showed no long-terin accumulation in organs and the possibility to accumulate in the tumor. These results warrant further studies of radioiodinated carboxylic and hydroxamic MNIP inhibitor tracers as potential SPECT tumor imaging agents. (C) 2004 Elsevier Inc. All rights reserved. [less ▲]

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See detailNew rationales for using TGFbeta inhibitors in radiotherapy.
Andarawewa, Kumari L.; Paupert, Jenny ULg; Pal, Anupama et al

in International journal of radiation biology (2007), 83(11-12), 803-11

PURPOSE: The first reports that ionizing radiation (IR) induces rapid and persistent activation of transforming growth factor beta1 (TGFbeta) were nearly two decades ago. Subsequent studies have shown ... [more ▼]

PURPOSE: The first reports that ionizing radiation (IR) induces rapid and persistent activation of transforming growth factor beta1 (TGFbeta) were nearly two decades ago. Subsequent studies have shown that TGFbeta is a major mediator of cellular and tissue responses to IR and have revealed novel facets of its complex biology. RESULTS: We and others have recently shown that inhibition of production or signaling of TGFbeta in epithelial cells modulates radiosensitivity and impedes activation of the DNA damage response program. The primary transducer of cellular response to DNA damage caused by ionizing radiation is the nuclear protein kinase ataxia telangiectasia mutated, whose activity is severely compromised when TGFbeta is inhibited. Thus, in conjunction, with its well-recognized contribution to normal tissue fibrosis, the role of TGFbeta in the genotoxic stress program provides a previously unsuspected avenue to modulate radiotherapy. CONCLUSIONS: We hypothesize that identification of the circumstances and tumors in which TGFbeta manipulation enhances tumor cell radiosensitivity, while protecting normal tissues, could significantly increase therapeutic index. [less ▲]

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