8hj5: Difference between revisions

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'''Unreleased structure'''


The entry 8hj5 is ON HOLD
==Cryo-EM structure of Gq-coupled MRGPRX1 bound with Compound-16==
 
<StructureSection load='8hj5' size='340' side='right'caption='[[8hj5]], [[Resolution|resolution]] 3.00&Aring;' scene=''>
Authors:  
== Structural highlights ==
 
<table><tr><td colspan='2'>[[8hj5]] is a 6 chain structure with sequence from [https://en.wikipedia.org/wiki/Escherichia_coli Escherichia coli], [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens], [https://en.wikipedia.org/wiki/Mus_musculus Mus musculus] and [https://en.wikipedia.org/wiki/Vicugna_pacos Vicugna pacos]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=8HJ5 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8HJ5 FirstGlance]. <br>
Description:  
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=U2U:N-{2-[(1-aminoisoquinolin-6-yl)oxy]-4-methylphenyl}-2-methoxybenzene-1-sulfonamide'>U2U</scene></td></tr>
[[Category: Unreleased Structures]]
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=8hj5 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8hj5 OCA], [https://pdbe.org/8hj5 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8hj5 RCSB], [https://www.ebi.ac.uk/pdbsum/8hj5 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8hj5 ProSAT]</span></td></tr>
</table>
== Function ==
[https://www.uniprot.org/uniprot/C562_ECOLX C562_ECOLX] Electron-transport protein of unknown function.[https://www.uniprot.org/uniprot/MRGX1_HUMAN MRGX1_HUMAN] Orphan receptor. Probably involved in the function of nociceptive neurons. May regulate nociceptor function and/or development, including the sensation or modulation of pain. Potently activated by enkephalins including BAM22 (bovine adrenal medulla peptide 22) and BAM (8-22)(PubMed:26582731). BAM22 is the most potent compound and evoked a large and dose-dependent release of intracellular calcium in stably transfected cells. G(alpha)q proteins are involved in the calcium-signaling pathway. Activated by the antimalarial drug, chloroquine. May mediate chloroquine-induced itch, in a histamine-independent manner.<ref>PMID:11850634</ref> <ref>PMID:20004959</ref> <ref>PMID:26582731</ref>
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Escherichia coli]]
[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Mus musculus]]
[[Category: Vicugna pacos]]
[[Category: Gan B]]
[[Category: Ren RB]]
[[Category: Yu LY]]

Revision as of 08:45, 31 May 2023

Cryo-EM structure of Gq-coupled MRGPRX1 bound with Compound-16Cryo-EM structure of Gq-coupled MRGPRX1 bound with Compound-16

Structural highlights

8hj5 is a 6 chain structure with sequence from Escherichia coli, Homo sapiens, Mus musculus and Vicugna pacos. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

C562_ECOLX Electron-transport protein of unknown function.MRGX1_HUMAN Orphan receptor. Probably involved in the function of nociceptive neurons. May regulate nociceptor function and/or development, including the sensation or modulation of pain. Potently activated by enkephalins including BAM22 (bovine adrenal medulla peptide 22) and BAM (8-22)(PubMed:26582731). BAM22 is the most potent compound and evoked a large and dose-dependent release of intracellular calcium in stably transfected cells. G(alpha)q proteins are involved in the calcium-signaling pathway. Activated by the antimalarial drug, chloroquine. May mediate chloroquine-induced itch, in a histamine-independent manner.[1] [2] [3]

References

  1. ↑ Lembo PM, Grazzini E, Groblewski T, O'Donnell D, Roy MO, Zhang J, Hoffert C, Cao J, Schmidt R, Pelletier M, Labarre M, Gosselin M, Fortin Y, Banville D, Shen SH, Ström P, Payza K, Dray A, Walker P, Ahmad S. Proenkephalin A gene products activate a new family of sensory neuron--specific GPCRs. Nat Neurosci. 2002 Mar;5(3):201-9. PMID:11850634 doi:10.1038/nn815
  2. ↑ Liu Q, Tang Z, Surdenikova L, Kim S, Patel KN, Kim A, Ru F, Guan Y, Weng HJ, Geng Y, Undem BJ, Kollarik M, Chen ZF, Anderson DJ, Dong X. Sensory neuron-specific GPCR Mrgprs are itch receptors mediating chloroquine-induced pruritus. Cell. 2009 Dec 24;139(7):1353-65. doi: 10.1016/j.cell.2009.11.034. Epub 2009 Dec , 10. PMID:20004959 doi:http://dx.doi.org/10.1016/j.cell.2009.11.034
  3. ↑ Heller D, Doyle JR, Raman VS, Beinborn M, Kumar K, Kopin AS. Novel Probes Establish Mas-Related G Protein-Coupled Receptor X1 Variants as Receptors with Loss or Gain of Function. J Pharmacol Exp Ther. 2016 Feb;356(2):276-83. PMID:26582731 doi:10.1124/jpet.115.227058

8hj5, resolution 3.00Å

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