About the Neurocypres Project
The Cys-loop receptors comprise a superfamily of ligand-gated ion channels that is crucial to the function of the peripheral and central nervous system. Cys-loop receptors (CLRs) share a generic protein architecture consisting of five subunits with an integral ion-channel that can open and close depending on ligand binding. The CLR group comprises nicotinic acetylcholine-, GABA-A-, 5HT3-, and Glycine receptors.
Dysfunction of CLRs is linked to muscle disorders (e.g. myasthenic syndromes), hyperexcitabiliy of the brain (e.g. epilepsy) and spinal cord (e.g. hyperekplexia / stiff baby syndrome) as well as nicotine addiction, while CLR subunit genes are candidates for frequent psychiatric diseases (e.g. schizophrenia).
The CLRs are molecular targets for clinically important drugs, including curare-like muscle relaxants, tranquillizers and anticonvulsants like the benzodiazepines, as well as anti-emetics. Novel drugs are on the horizon, mediating highly selective therapeutic effects and providing new avenues for therapeutic use.
Today, the quality of crystallographic data and the general knowledge of structure-function relationships has progressed to such an extent that the rational design of ligands becomes a feasible objective.
For this to become reality, coordinated approaches to increase our knowledge of ligand-gated ion channel structure at high-resolution are required. This is what the Neurocypres project aims at.