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Project

Structure-based discovery of positive allosteric modulators of the alpha7 nicotinic ecetylcholine receptor as cognition enhancers.

Nicotinic acetylcholine receptors (nAChRs) are relevant therapeutic targets for diseases of the brain. The most promising target for disorders associated with cognitive dysfunction is the alpha7 subtype. The scientific goal is to develop novel molecules targeting the α7 nicotinic acetylcholine receptor and that improve cognition in schizophrenia and Alzheimer’s disease, both of which are disorders for which there remains an unmet medical need. The main goal is to obtain a patent for the novel compounds and to negotiate a license with a pharmaceutical company. A 3-dimensional structure of the alpha7 subtype of nAChR is not yet available, but detailed insight of protein structures at atomic level yields invaluable information about protein function and can facilitate the discovery and development of new drugs. A marine snail protein (called acetylcholine binding protein) has been engineered to mimic the human alpha7 nAChR and offers a realistic template for structure-based drug design. The goal of this project is the development of novel high affinity lead compounds with activity as positive allosteric modulators for alpha7 nAChR. These compounds will have potential application as cognition enhancers in schizophrenia and Alheimer's disease.

Date:2 Jul 2018 →  31 May 2021
Keywords:Ion channels, Positive allosteric modulators, Crystallography
Disciplines:Neurosciences, Biological and physiological psychology, Cognitive science and intelligent systems, Developmental psychology and ageing
Project type:PhD project