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nAChR PAM-to-gate: Gating mechanism and pharmacological modulation of nicotinic acetylcholine receptors.

Total cost: EUR 185 076

EU contribution: EUR 185 076

Topic(s):MSCA-IF-2014-EF - Marie Sklodowska-Curie Individual Fellowships (IF-EF)

Objective: Pentameric ligand-gated ion channels (pLGICs), including nicotinic acetylcholine, 5HT3, glycine, and GABAA receptors, are membrane proteins specialized in the communication between neurons. These neurotransmitter receptors are the target of general anaesthetics, anxiolytics, alcohols and nicotine. In particular, enhancing the activity of neuronal nicotinic receptors holds promises in the treatment of pathologies including nicotine addiction, schizophrenia and Alzheimers disease. The current project aims at deciphering the molecular and pharmacological determinants of positive allosteric modulators of neuronal nicotinic receptors. We will over-express and purify these proteins, study their pharmacology through electrophysiology in cell lines and planar lipid bilayer, and surface plasmon resonance binding studies. Our study will provide insights into the molecular mechanisms of allosteric regulation, paving the way for the rational design of allosteric modulators with therapeutic potential.

Coordinator

INSTITUT PASTEUR

France

EU contribution: EUR 185 076

Project completion date : 2017-03-31 12:00:00

Major organization : INSTITUT PASTEUR

Address : Rue Du Docteur Roux 25-28

75724 Paris Cedex 15

Country :France

Url : http://www.pasteur.fr/

Financier : EUROPEAN UNION (EU),

Financier address : European Union (EU)

Rue de la Loi 200/Wetstraat 200,

B-1049 Bruxelles/Brussels,

Belgium

Tel: 32-2-2999696, 2993085

Fax: 32-2-2961749

Url: ec.europa.eu/

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Publication:Mena Report
Date:Nov 3, 2016
Words:225
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