3-D Conformation of GLIC and allosteric modulation thereof

摘要

The application relates to the ligand-gated ion channel of Gloebacter violaceus (GLIC), more particularly to its 3-D conformation. The application notably relates to crystal(s) comprising at least one GLIC monomer chain and a compound bound thereto, as well as to the biotechnological and medical applications thereof, including methods for screening and screening tools, such as a computer device system. The application describes GLIC allosteric site(s), which is(are) present in the transmembrane domain of each monomer of the pentameric GLIC. This(these) allosteric site(s) is(are), or contains(contain) binding site(s) for compounds which (allosterically) modulate the GLIC pore ion conductance, and therefore (allosterically) modulate cell excitability, more particularly neurotransmission.