Metabotropic glutamate receptor: Difference between revisions

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== Structural highlights ==
== Structural highlights ==
<scene name='46/464134/Cv/3'>Glutamate is bound to GluR1</scene> in the crevice between the N-terminal and C-terminal domains<ref>PMID:11069170</ref>. Water molecules are shown as red spheres.
<scene name='46/464134/Cv/3'>Glutamate is bound to GluR1</scene> in the crevice between the N-terminal and C-terminal domains<ref>PMID:11069170</ref>. Water molecules are shown as red spheres.
==3D structures of metabotropic glutamate receptor ==
[[Metabotropic glutamate receptor 3D structures]]


</StructureSection>
</StructureSection>
Line 25: Line 28:


*Metabotropic glutamate receptor 1
*Metabotropic glutamate receptor 1
 
**[[1ewt]], [[1ewv]] - rMGluR1 LBD - rat<br />
**[[3ks9]] – hMGluR1 (mutant) + antagonist - human<br />
**[[3ks9]] – hMGluR1 (mutant) + antagonist - human<br />
**[[4or2]] - hMGluR1/cytochrome b526<br />
**[[4or2]] - hMGluR1/cytochrome b526<br />
**[[1ewt]], [[1ewv]] - rMGluR1 LBD - rat<br />
**[[1isr]], [[1ewk]] – rMGluR1 LBD + Glu<br />
**[[1isr]], [[1ewk]] – rMGluR1 LBD + Glu<br />
**[[1iss]] - rMGluR1 LBD + antagonist<br />
**[[1iss]] - rMGluR1 LBD + antagonist<br />
Line 42: Line 45:


**[[5cnk]] – hMGluR3 LBD + Glu <br />
**[[5cnk]] – hMGluR3 LBD + Glu <br />
**[[2e4u]] – rMGluR3 LBD (mutant) + Glu<br />
**[[2e4v]], [[2e4w]], [[2e4x]], [[2e4y]], [[2e4z]] - rMGluR3 LBD (mutant) + agonist<br />
**[[3sm9]] - hMGluR3 + antagonist<br />
**[[3sm9]] - hMGluR3 + antagonist<br />
**[[4xar]], [[6b7h]] – hMGluR3 LBD + agonist<br />
**[[4xar]], [[6b7h]] – hMGluR3 LBD + agonist<br />
**[[5cnm]] – hMGluR3 LBD + Glu analog<br />
**[[5cnm]] – hMGluR3 LBD + Glu analog<br />
**[[2e4u]] – rMGluR3 LBD (mutant) + Glu<br />
**[[2e4v]], [[2e4w]], [[2e4x]], [[2e4y]], [[2e4z]] - rMGluR3 LBD (mutant) + agonist<br />


*Metabotropic glutamate receptor 5
*Metabotropic glutamate receptor 5


**[[6n52]] – hMGluR5 – Cryo EM<br />
**[[6n51]], [[6n50]], [[6n4y]] – hMGluR5 + nanobody – Cryo EM<br />
**[[6n4x]] – hMGluR5 LBD<br />
**[[6ffh]], [[6ffi]] - hMGluR5 LBD (mutant) + positive allosteric modulator<br />
**[[6ffh]], [[6ffi]] - hMGluR5 LBD (mutant) + positive allosteric modulator<br />
**[[3lmk]] – hMGluR5 LBD (mutant) + positive allosteric modulator + Glu<br />
**[[3lmk]] – hMGluR5 LBD (mutant) + positive allosteric modulator + Glu<br />
Line 63: Line 69:
**[[6bsz]] – hMGluR8 LBD + Glu <br />
**[[6bsz]] – hMGluR8 LBD + Glu <br />
**[[6bt5]] – hMGluR8 LBD + phosphonobutanoic acid <br />
**[[6bt5]] – hMGluR8 LBD + phosphonobutanoic acid <br />
**[[6e5v]] – hMGluR8 N-terminal (mutant) + inhibitor <br />
}}
}}
==See Also==
==See Also==

Revision as of 12:01, 30 October 2019


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 and metabotropic glutamate receptor 8 belong 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 are shown as red spheres.

3D structures of metabotropic glutamate receptor

Metabotropic glutamate receptor 3D structures


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 30-October-2019

    • 3ks9 – hMGluR1 (mutant) + antagonist - human
    • 4or2 - hMGluR1/cytochrome b526
    • 1ewt, 1ewv - rMGluR1 LBD - rat
    • 1isr, 1ewk – rMGluR1 LBD + Glu
    • 1iss - rMGluR1 LBD + antagonist
  • Metabotropic glutamate receptor 2
    • 4xas, 4xaq – hMGluR2 LBD + agonist
    • 5kzq, 5kzn – hMGluR2 LBD + antagonist
    • 5cni – hMGluR2 LBD + Glu
    • 5cnj – hMGluR2 LBD + Glu analog
  • Metabotropic glutamate receptor 3
    • 5cnk – hMGluR3 LBD + Glu
    • 3sm9 - hMGluR3 + antagonist
    • 4xar, 6b7h – hMGluR3 LBD + agonist
    • 5cnm – hMGluR3 LBD + Glu analog
    • 2e4u – rMGluR3 LBD (mutant) + Glu
    • 2e4v, 2e4w, 2e4x, 2e4y, 2e4z - rMGluR3 LBD (mutant) + agonist
  • Metabotropic glutamate receptor 5
    • 6n52 – hMGluR5 – Cryo EM
    • 6n51, 6n50, 6n4y – hMGluR5 + nanobody – Cryo EM
    • 6n4x – hMGluR5 LBD
    • 6ffh, 6ffi - hMGluR5 LBD (mutant) + positive allosteric modulator
    • 3lmk – hMGluR5 LBD (mutant) + positive allosteric modulator + Glu
    • 5cgc, 5cgd - hMGluR5 transmembrane domain + negative allosteric modulator
  • Metabotropic glutamate receptor 7
    • 5c5c – hMGluR7 LBD (mutant)
    • 3mq4 – hMGluR7 LBD + antagonist
  • Metabotropic glutamate receptor 8
    • 6bsz – hMGluR8 LBD + Glu
    • 6bt5 – hMGluR8 LBD + phosphonobutanoic acid
    • 6e5v – hMGluR8 N-terminal (mutant) + inhibitor

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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Wayne Decatur, Michal Harel, Nikki Hunter, Alexander Berchansky
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