8x2k

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OEA bound GPR3-Gs complex structureOEA bound GPR3-Gs complex structure

Structural highlights

8x2k is a 5 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:Electron Microscopy, Resolution 3.03Å
Ligands:
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

GPR3_HUMAN Constitutively active G-protein coupled receptor that maintains high 3'-5'-cyclic adenosine monophosphate (cAMP) levels that a plays a role in serveral processes including meiotic arrest in oocytes or neuronal development via activation of numerous intracellular signaling pathways. Acts as an essential activator of thermogenic adipocytes and drives thermogenesis via its intrinsic G(s)-coupling activity without the requirement of a ligand (PubMed:34048700). Has a potential role in modulating a number of brain functions, including behavioral responses to stress (By similarity), amyloid-beta peptide generation in neurons (By similarity). Stimulates neurite outgrowth in cerebellar granular neurons modulated via PKA, ERK, and most strongly PI3K-mediated signaling pathways (By similarity).[UniProtKB:P35413][1] [2] C562_ECOLX Electron-transport protein of unknown function.

References

  1. Thathiah A, Spittaels K, Hoffmann M, Staes M, Cohen A, Horré K, Vanbrabant M, Coun F, Baekelandt V, Delacourte A, Fischer DF, Pollet D, De Strooper B, Merchiers P. The orphan G protein-coupled receptor 3 modulates amyloid-beta peptide generation in neurons. Science. 2009 Feb 13;323(5916):946-51. PMID:19213921 doi:10.1126/science.1160649
  2. Sveidahl Johansen O, Ma T, Hansen JB, Markussen LK, Schreiber R, Reverte-Salisa L, Dong H, Christensen DP, Sun W, Gnad T, Karavaeva I, Nielsen TS, Kooijman S, Cero C, Dmytriyeva O, Shen Y, Razzoli M, O'Brien SL, Kuipers EN, Nielsen CH, Orchard W, Willemsen N, Jespersen NZ, Lundh M, Sustarsic EG, Hallgren CM, Frost M, McGonigle S, Isidor MS, Broholm C, Pedersen O, Hansen JB, Grarup N, Hansen T, Kjær A, Granneman JG, Babu MM, Calebiro D, Nielsen S, Rydén M, Soccio R, Rensen PCN, Treebak JT, Schwartz TW, Emanuelli B, Bartolomucci A, Pfeifer A, Zechner R, Scheele C, Mandrup S, Gerhart-Hines Z. Lipolysis drives expression of the constitutively active receptor GPR3 to induce adipose thermogenesis. Cell. 2021 Jun 24;184(13):3502-3518.e33. PMID:34048700 doi:10.1016/j.cell.2021.04.037

8x2k, resolution 3.03Å

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OCA