8hj5

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.
Method:	Electron Microscopy, Resolution 3Å
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

↑ 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
↑ 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
↑ 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

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OCA

[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

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