Metabotropic glutamate receptor: Difference between revisions

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**[[3lmk]] – hMGluR5 LBD (mutant) + positive allosteric modulator + Glu<br />
**[[3lmk]] – hMGluR5 LBD (mutant) + positive allosteric modulator + Glu<br />
**[[5cgc]], [[5cgd]] - hMGluR5 transmembrane domain + negative allosteric modulator<br />


*Metabotropic glutamate receptor 7
*Metabotropic glutamate receptor 7

Revision as of 10:28, 20 July 2017


Function

Metabotropic glutamate receptors are glutamate receptors that activate ion channels indirectly through a signaling cascade involving G proteins[1]. They are members of the large class of seven-transmembrane domain receptors, the G protein-coupled receptors. Glutamate receptors are classified into 3 groups based on their homology, mechanism and pharmacological properties. See also Ligand Binding N-Terminal of Metabotropic Glutamate Receptors.

  • Metabotropic glutamate receptor 1 and metabotropic glutamate receptor 5 belong to group I and activate phospholipase C. For details see Metabotropic glutamate receptor 5.
  • Metabotropic glutamate receptor 2 and metabotropic glutamate receptor 3 belong to group II and inhibit the cyclic AMP cascade.
  • Metabotropic glutamate receptor 7 belongs to group III and inhibits adenylate cyclase activity.

Articles in Proteopedia concerning Toll-like Receptors include:


Relevance

GluR are targets for Parkinson's disease drugs[2] as well as for Alzheimer's disease, depression, anxiety and schizophrenia[3].

Structural highlights

in the crevice between the N-terminal and C-terminal domains[4]. Water molecules shown as red spheres.


Structure of the glycosylated rat binding domain of the Metabotropic Glutamate Receptor, GluR1, bound to glutamate, Hepes and Mg+2 ions (1ewk)

Drag the structure with the mouse to rotate

3D structures of metabotropic glutamate receptor3D structures of metabotropic glutamate receptor

Updated on 20-July-2017

See AlsoSee Also

Membrane Channels & Pumps
Ionotropic_Glutamate_Receptors
Alzheimer's Disease

ReferencesReferences

  1. ↑ Traynelis SF, Wollmuth LP, McBain CJ, Menniti FS, Vance KM, Ogden KK, Hansen KB, Yuan H, Myers SJ, Dingledine R. Glutamate receptor ion channels: structure, regulation, and function. Pharmacol Rev. 2010 Sep;62(3):405-96. doi: 10.1124/pr.109.002451. PMID:20716669 doi:http://dx.doi.org/10.1124/pr.109.002451
  2. ↑ Johnson KA, Conn PJ, Niswender CM. Glutamate receptors as therapeutic targets for Parkinson's disease. CNS Neurol Disord Drug Targets. 2009 Dec;8(6):475-91. PMID:19702565
  3. ↑ Niswender CM, Conn PJ. Metabotropic glutamate receptors: physiology, pharmacology, and disease. Annu Rev Pharmacol Toxicol. 2010;50:295-322. doi:, 10.1146/annurev.pharmtox.011008.145533. PMID:20055706 doi:http://dx.doi.org/10.1146/annurev.pharmtox.011008.145533
  4. ↑ Kunishima N, Shimada Y, Tsuji Y, Sato T, Yamamoto M, Kumasaka T, Nakanishi S, Jingami H, Morikawa K. Structural basis of glutamate recognition by a dimeric metabotropic glutamate receptor. Nature. 2000 Oct 26;407(6807):971-7. PMID:11069170 doi:10.1038/35039564

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