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See detailG protein-coupled receptors, an unexploited animal toxin targets: Exploration of green mamba venom for novel drug candidates active against adrenoceptors
Maïga, Arhamatoulaye; Mourier, Gilles; Quinton, Loïc ULg et al

in Toxicon (2012), 59

At a time when pharmaceutical companies are having trouble finding new low MW drugs and when biologics are becoming more common, animal venoms could constitute an underexploited source of novel drug ... [more ▼]

At a time when pharmaceutical companies are having trouble finding new low MW drugs and when biologics are becoming more common, animal venoms could constitute an underexploited source of novel drug candidates. We looked for identifying novel animal toxins active against G protein-coupled receptors (GPCR), the most frequently exploited class of treatment targets, with the aim to develop novel research tools and drug candidates. Screening of green mamba (Dendroaspis angusticeps) venom against adrenoceptors identified two novel venom peptides. r-Da1a shown an affinity of 0.35 nM for the a1a-AR while r-Da1b displayed affinities between 14 and 73 nM for the three a2-ARs. These two venom peptides have sequences similar to those of muscarinic toxins and belong to the three-finger-fold protein family. a1a-AR is the primary target for the treatment of prostate hypertrophy. In vitro and in vivo tests demonstrated that r-Da1a reduced prostatic muscle tone as efficiently as tamsulosin (an antagonist presently used), but with fewer cardiovascular side effects. a2-ARs are the prototype of GPCRs not currently used as treatment targets due to a lack of specific ligands. Blockage of these receptors increases intestinal motility, which may be compromised by abdominal surgery and reduces orthosteric hypotension. In vitro and in vivo tests demonstrated that r-Da1b antagonizes a2-ARs in smooth muscles and increased heart rate and blood catecholamine concentrations. These results highlight possible exploitation of r-Da1a and r-Da1b in important pathologies. [less ▲]

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See detailIsolation and pharmacological characterization of AdTx1, a natural peptide displaying specific insurmountable antagonism of the alpha1A-adrenoceptor
Quinton, Loïc ULg; Girard, E.; Maiga, A. et al

in British Journal of Pharmacology (2010), 159

Venoms are a rich source of ligands for ion channels, but very little is known about their capacity to modulate G-protein coupled receptor (GPCR) activity. We developed a strategy to identify novel toxins ... [more ▼]

Venoms are a rich source of ligands for ion channels, but very little is known about their capacity to modulate G-protein coupled receptor (GPCR) activity. We developed a strategy to identify novel toxins targeting GPCRs. Experimental approach: We studied the interactions of mamba venom fractions with a1-adrenoceptors in binding experiments with 3H-prazosin. The active peptide (AdTx1) was sequenced by Edman degradation and mass spectrometry fragmentation. Its synthetic homologue was pharmacologically characterized by binding experiments using cloned receptors and by functional experiments on rabbit isolated prostatic smooth muscle [less ▲]

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See detailIdentification of a novel snake peptide displaying high affinity and antagonist behaviour for the alpha2-adrenoreceptors
Rouget, Céline; Quinton, Loïc ULg; Maïga, Arhamatoulaye et al

in British Journal of Pharmacology (2010), 161

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