8dwc

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CryoEM structure of Gq-coupled MRGPRX1 with peptide agonist BAM8-22CryoEM structure of Gq-coupled MRGPRX1 with peptide agonist BAM8-22

Structural highlights

8dwc is a 6 chain structure with sequence from Bos taurus, Homo sapiens and Mus musculus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

PENK_BOVIN Neuropeptide that competes with and mimic the effects of opiate drugs. They play a role in a number of physiologic functions, including pain perception and responses to stress.[UniProtKB:P01210] Neuropeptide that competes with and mimic the effects of opiate drugs. They play a role in a number of physiologic functions, including pain perception and responses to stress.[UniProtKB:P01210] Met-enkephalin-Arg-Phe neuropeptide acts as a strong ligand of Mu-type opioid receptor OPRM1. Met-enkephalin-Arg-Phe-binding to OPRM1 in the nucleus accumbens of the brain increases activation of OPRM1, leading to long-term synaptic depression of glutamate release.[UniProtKB:P22005] Increases glutamate release in the striatum and decreases GABA concentration in the striatum.[UniProtKB:P04094] Increases glutamate release in the striatum.[UniProtKB:P04094] Enkelytin possesses antibacterial activity against Gram-positive bacteria such as Micrococcus luteus and Bacillus megaterium.[1]

References

  1. Goumon Y, Strub JM, Moniatte M, Nullans G, Poteur L, Hubert P, Van Dorsselaer A, Aunis D, Metz-Boutigue MH. The C-terminal bisphosphorylated proenkephalin-A-(209-237)-peptide from adrenal medullary chromaffin granules possesses antibacterial activity. Eur J Biochem. 1996 Feb 1;235(3):516-25. doi:, 10.1111/j.1432-1033.1996.t01-1-00516.x. PMID:8654396 doi:http://dx.doi.org/10.1111/j.1432-1033.1996.t01-1-00516.x

8dwc, resolution 2.87Å

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OCA