| Title : Engineered site-directed labeling of nicotinic acetylcholine receptors using reactive epibatidine derivatives: appraisal of epibatidine-docking models in neuronal and muscular receptors - Sakr_2006_J.Mol.Neurosci_30_35 |
| Author(s) : Sakr E , Kotzyba-Hibert F , Grande J , Hovius R , Vogel H , Bertrand S , Bertrand D , Goeldner M |
| Ref : Journal of Molecular Neuroscience , 30 :35 , 2006 |
| Abstract : We developed an engineered site-directed labeling method (Foucaud et al., 2001) to investigate ligand receptor interactions on the acetylcholine (ACh)- binding site of nicotinic acetylcholine receptors (nAChRs). The method uses cysteine receptor mutants, together with cysteine-reactive ligand analogs, to generate a site-directed covalent reaction within the binding site. We selected epibatidine (EPB) as a prototypical ligand, acting at all types of nAChRs with sufficient affinity to allow this study. Accordingly, we synthesized three cysteine-reactive derivatives, all modified at the C-3 of the pyridine ring of the alkaloid with NCS; -NHCOCH2Cl, and -CH2Cl groups, respectively (Fig. 1). The binding properties have been established on rat brain, alpha7-5HT3 chimera, and Torpedo membranes, respectively, whereas the functional properties were tested on alpha4beta2 and alpha7 receptor expressed in oocytes and Cys-less muscular receptor expressed in HEK cells (Sakr et al., 2005). |
| ESTHER : Sakr_2006_J.Mol.Neurosci_30_35 |
| PubMedSearch : Sakr_2006_J.Mol.Neurosci_30_35 |
| PubMedID: 17192618 |
Sakr E, Kotzyba-Hibert F, Grande J, Hovius R, Vogel H, Bertrand S, Bertrand D, Goeldner M (2006)
Engineered site-directed labeling of nicotinic acetylcholine receptors using reactive epibatidine derivatives: appraisal of epibatidine-docking models in neuronal and muscular receptors
Journal of Molecular Neuroscience
30 :35
Sakr E, Kotzyba-Hibert F, Grande J, Hovius R, Vogel H, Bertrand S, Bertrand D, Goeldner M (2006)
Journal of Molecular Neuroscience
30 :35