[en] 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
Disciplines :
Chemistry
Author, co-author :
Quinton, Loïc ; Université de Liège - ULiège > Département de chimie (sciences) > GIGA-R : Laboratoire de spectrométrie de masse (L.S.M.)
Girard, E.; Centre National de la Recherche Scientifique - CNRS > Institut de Neurobiologie Alfred Fessard, Laboratoire de Neurobiologie Cellulaire et Moléculaire, Gif sur Yvette, France
Maiga, A.; Commissariat à l'Energie Atomique (Saclay) - CEA > iBiTecS, Service d’Ingénierie Moléculaire des Protéines (SIMOPRO)
Rekik, M.; Université Paul Sabatier - Toulouse 3 - UPS > UROsphere S.A.S., Faculté des Sciences Pharmaceutiques, Toulouse, France
Lluel, P.; Université Paul Sabatier - Toulouse 3 - UPS > UROsphere S.A.S., Faculté des Sciences Pharmaceutiques, Toulouse, France
Masuyer, G.; University of Bath- UK > Structural Molecular Biology Department of Biology & Biochemistry, University of Bath, UK
Larregola, M.; Université Pierre et Marie Currie - Paris 6 - UPMC > Laboratoire de Synthèse, Laboratoire des Biomolécules, Paris, France,
Marquer, C.; Commissariat à l'Energie Atomique (Saclay) - CEA > iBiTecS, Service d’Ingénierie Moléculaire des Protéines (SIMOPRO)
Ciolek, Justyna; N. Copernicus University > Laboratory of Biophysics, Institute of General and Molecular Biology, N. Copernicus University, Torun, Poland
Magnin, T.; Université de Strasbourg I > Institut Gilbert-Laustriat UMR 7175 CNRS/Université Strasbourg I, Département Récepteurs et Protéines Membranaires > Ecole Supérieure de Biotechnologie de Strasbourg, Illkirch, France,
Wagner, R.; Université de Strasbourg I > Institut Gilbert-Laustriat UMR 7175 CNRS/Université Strasbourg I, Département Récepteurs et Protéines Membranaires > Ecole Supérieure de Biotechnologie de Strasbourg, Illkirch, France,
Molgo, Jordi; Centre National de la Recherche Scientifique - CNRS > Institut de Neurobiologie Alfred Fessard, Laboratoire de Neurobiologie Cellulaire et Moléculaire, Gif sur Yvette, France
Thai, Robert; Commissariat à l'Energie Atomique (Saclay) - CEA > iBiTecS, Service d’Ingénierie Moléculaire des Protéines (SIMOPRO)
Fruchart-Gaillard, C.; Commissariat à l'Energie Atomique (Saclay) - CEA > iBiTecS, Service d’Ingénierie Moléculaire des Protéines (SIMOPRO)
Mourier, Gilles; Commissariat à l'Energie Atomique (Saclay) - CEA > iBiTecS, Service d’Ingénierie Moléculaire des Protéines (SIMOPRO)
Chamot-Rooke, Julia; Ecole Polytechnique (France) > Laboratoire des Mécanismes Réactionnels
Ménez, André; Muséum national d’Histoire Naturelle10Muséum national d’Histoire Naturelle, Paris, France
Palea, S.; Université Paul Sabatier - Toulouse 3 - UPS > UROsphere S.A.S., Faculté des Sciences Pharmaceutiques, Toulouse, France
Servent, Denis; Commissariat à l'Energie Atomique (Saclay) - CEA > iBiTecS, Service d’Ingénierie Moléculaire des Protéines (SIMOPRO)
Gilles, Nicolas; Commissariat à l'Energie Atomique (Saclay) - CEA > iBiTecS,Service d’Ingénierie Moléculaire des Protéines (SIMOPRO)
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