Functional Characterization of Glutamate Receptor Ion Channels

Over the years, Creative Bioarray has made great strides in the field of structural characterization. We are well placed to provide our clients with more available structural data on iGluR subtypes, which in combination with functional characterization can help facilitate the study of the relationship between the structure, function, and allosteric regulation of iGluRs.

Introduction

iGluRs are ligand-gated ion channels that regulate the open and closed states of the channel by binding to glutamate. iGluRs play important physiological functions in organisms, including regulating multiple processes in the brain, retina, spinal cord, and peripheral nervous system. Understanding the functional characteristics and pharmacological properties of iGluRs could lead to the development of better drugs to treat glutamate receptor-related diseases such as depression, dementia, Parkinson's disease, epilepsy and stroke.

Different subgroups of the iGluR family play unique roles in neurotransmission and exhibit specific kinetic and pharmacological properties. Advances in multiple biophysical techniques, such as crystallography, calorimetry, computational chemistry, NMR, and optogenetics, have accelerated the development of iGluR structural biology. For functional studies of intact iGluRs, techniques such as single-channel recordings and whole-cell recordings are commonly used. Research in the field of iGluR structure and function has greatly accelerated the exploration of the principles of iGluR gating, as well as the molecular mechanisms underlying their subtype specific properties.

Fig. 1 State diagram for activation and desensitization of glutamate receptor ion channels. (Mayer, 2004)

Our Services

Our functional characterization aimed to analyze the physiological roles and molecular biology of iGluRs and their roles in synaptic function. Currently, we have established a variety of biochemical techniques including ultracentrifugation, NMR, spectroscopy, and molecular dynamics calculations to provide complementary insights into the X-ray crystal structures. We obtain this information to help our clients gain insight into the mechanisms of receptor activation, partial agonists, desensitization, and allosteric modulation. Our services include but not limited to:

• Analysis of iGluR domain organization and establishment of the correct iGluR topology, proving a basis for the direct analysis of iGluR structure and function.
• Expression of agonist-binding cores.
• Determination of structures for the ligand-binding cores of members of the iGluR gene family.
• Determination of the structures of complexes with additional agonists and antagonists, providing the information required for the design and synthesis of new iGluR subtype–selective ligands.

Applications

• Research on mechanisms of activation and desensitization of iGluRs
• Study on the role of glutamate receptors in normal functions
• Drug design for iGluR in neurological diseases

Creative Bioarray is committed to providing clients with high-quality iGluR function characterization services. Our technically qualified and experienced professional team will bring you the best service. If you are interested in our services, please contact us for more details.

Reference

1. Mayer, M. L.; Armstrong, N. Structure and function of glutamate receptor ion channels. Annual review of physiology, 2004, 66: 161.