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Molecular Structure of Ionotropic Glutamate Receptors

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L-glutamate is the major excitatory neurotransmitter in the central nervous system (CNS). Although just a few glutamate receptor ligands have turned out to be clinically useful, primarily because of unfavorable psychotropic side effects, the glutamate system remains an attractive molecular target in the treatment of epilepsy, neurodegenerative diseases (Alzheimer's disease, Parkinson's disease, Huntington's chorea), schizophrenia, ischemia, pain, alcoholism and mood disorders.

Knowledge about the structure of ionotropic glutamate receptors (iGluRs) at atomic resolution is vital for the determination of their physiological and pathological importance and, thus, for drug design. Recently, tremendous progress has been made in structure elucidation and understanding of the functioning of iGluRs. The data about general topology and modular composition of iGluRs as well as numerous crystal structures of ligand binding domains of many iGluR subtypes has been supplemented with the first molecular models of the whole receptor protein, followed by the first crystal structures of N-terminal domains and finally by the first crystal structure of the whole tetrameric iGluR.

This review summarizes experimental and computational efforts to determine iGluR molecular architecture and focus on the above listed achievements of the last years. In particular, the aspects of iGluR structure which are important for drug design, like the molecular characterstics of the ligand binding sites, are depicted in detail.

Keywords: LBD of ionotropic glutamate receptors; NTD of ionotropic glutamate receptors; gating of glutamate ion channels; glutamate ion channel; symmetry of ionotropic glutamate receptors

Document Type: Research Article


Affiliations: Department of Synthesis and Chemical Technology of Pharmaceutical Substances, Faculty of Pharmacy, Medical University of Lublin, 6 Staszica Str., 20081 Lublin, Poland.

Publication date: August 1, 2010

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.

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