Structural Insights into Function of Ionotropic Glutamate Receptors

— Ionotropic glutamate receptors (iGluRs) mediate fast excitatory neurotransmission. They are implicated in nervous system development and function, while their dysfunction is associated with neurological and psychiatric disorders. In this review, we describe recent progress in structural studies of...

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Bibliographic Details
Published in:Biochemistry (Moscow). Supplement series A, Membrane and cell biology Membrane and cell biology, 2022-09, Vol.16 (3), p.190-206
Main Authors: Yelshanskaya, M. V., Sobolevsky, A. I.
Format: Article
Language:English
Subjects:
Allosteric properties
Biomedical and Life Sciences
Cell Biology
Central nervous system
Crystal structure
Desensitization
Drug development
Glutamic acid receptors (ionotropic)
Ion channels
Life Sciences
Mental disorders
Modulators
Neurological diseases
Neuromodulation
Neurotransmission
Receptor mechanisms
Receptors
Reviews
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Summary:— Ionotropic glutamate receptors (iGluRs) mediate fast excitatory neurotransmission. They are implicated in nervous system development and function, while their dysfunction is associated with neurological and psychiatric disorders. In this review, we describe recent progress in structural studies of iGluRs and how crystal and cryo-EM structures helped determining the principles of iGluR architecture and assembly, and the mechanisms of activation, desensitization and regulation by auxiliary subunits, positive and negative allosteric modulators, and ion channel blockers. The new structural insights facilitate better understanding of iGluR physiological and pathophysiological roles in functioning of the central nervous system and provide valuable information for structure-based drug design.
ISSN:1990-7478
1990-7494
DOI:10.1134/S1990747822040043