This result, published in Nature, describes the activation cycle of the 5-HT3 receptor, belonging to the family of serotonin receptors. These receptors influence various biological and neurological processes such as anxiety, appetite, mood and nausea. 5-HT3 receptors are the main target of anti-emetic drugs widely used to alleviate the side effect of chemotherapies.
Scientists from the IBS, the Institut Pasteur, the University of Lorraine, the University of Copenhagen, Danemark, the University of Illinois, US, and the biotech company Theranyx, solved the structure of the 5-HT3 receptor in four different conformations. These four snapshots taken at different steps of the activation cycle of the receptor allow to describe its molecular mechanism. They also provide structural knowledge for pharmacology, revealing details of the serotonin and drug binding site, and may therefore help the development of more efficient anti-emetics (see ESRF press release).
Conformational transitions of the serotonin 5-HT3 receptor. Lucie Polovinkin, Ghérici Hassaine, Jonathan Perot, Emmanuelle Neumann, Anders A. Jensen, Solène Lefebvre, Pierre-Jean Corringer, Jacques Neyton, Christophe Chipot, Francois Dehez, Guy Schoehn & Hugues Nury. Nature 563(7730):275-279