7ymh

Cryo-EM structure of Nb29-alpha1AAR-miniGsq complex bound to noradrenaline

spinqualitylabelsall models 7ymh, resolution 3.52Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 7ymh is a 3 chain structure with sequence from Homo sapiens and Synthetic construct. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: Electron Microscopy, Resolution 3.52Å Ligands: E5E Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Publication Abstract from PubMed The alpha(1A-)adrenergic receptor (alpha(1A)AR) belongs to the family of G protein-coupled receptors that respond to adrenaline and noradrenaline. alpha(1A)AR is involved in smooth muscle contraction and cognitive function. Here, we present three cryo-electron microscopy structures of human alpha(1A)AR bound to the endogenous agonist noradrenaline, its selective agonist oxymetazoline, and the antagonist tamsulosin, with resolutions range from 2.9 A to 3.5 A. Our active and inactive alpha(1A)AR structures reveal the activation mechanism and distinct ligand binding modes for noradrenaline compared with other adrenergic receptor subtypes. In addition, we identified a nanobody that preferentially binds to the extracellular vestibule of alpha(1A)AR when bound to the selective agonist oxymetazoline. These results should facilitate the design of more selective therapeutic drugs targeting both orthosteric and allosteric sites in this receptor family. Structural basis of alpha(1A)-adrenergic receptor activation and recognition by an extracellular nanobody.,Toyoda Y, Zhu A, Kong F, Shan S, Zhao J, Wang N, Sun X, Zhang L, Yan C, Kobilka BK, Liu X Nat Commun. 2023 Jun 20;14(1):3655. doi: 10.1038/s41467-023-39310-x. PMID:37339967 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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