7f6h

Cryo-EM structure of human bradykinin receptor BK2R in complex Gq proteins and bradykinin

spinqualitylabelsall models 7f6h, resolution 2.90Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 7f6h 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 2.9Å Ligands: CLR Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function BKRB2_HUMAN Receptor for bradykinin. It is associated with G proteins that activate a phosphatidylinositol-calcium second messenger system. Publication Abstract from PubMed The type 2 bradykinin receptor (B2R) is a G protein-coupled receptor (GPCR) in the cardiovascular system, and the dysfunction of B2R leads to inflammation, hereditary angioedema, and pain. Bradykinin and kallidin are both endogenous peptide agonists of B2R, acting as vasodilators to protect the cardiovascular system. Here we determine two cryo-electron microscopy (cryo-EM) structures of human B2R-G(q) in complex with bradykinin and kallidin at 3.0 A and 2.9 A resolution, respectively. The ligand-binding pocket accommodates S-shaped peptides, with aspartic acids and glutamates as an anion trap. The phenylalanines at the tail of the peptides induce significant conformational changes in the toggle switch W283(6.48), the conserved PIF, DRY, and NPxxY motifs, for the B2R activation. This further induces the extensive interactions of the intracellular loops ICL2/3 and helix 8 with G(q) proteins. Our structures elucidate the molecular mechanisms for the ligand binding, receptor activation, and G(q) proteins coupling of B2R. Cryo-EM structures of human bradykinin receptor-G(q) proteins complexes.,Shen J, Zhang D, Fu Y, Chen A, Yang X, Zhang H Nat Commun. 2022 Feb 7;13(1):714. doi: 10.1038/s41467-022-28399-1. PMID:35132089 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Transducin 3D structures

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