5glh

Human endothelin receptor type-B in complex with ET-1

spinqualitylabelsall models 5glh, resolution 2.80Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 5glh is a 2 chain structure. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Related: 5gli Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function [EDN1_HUMAN] Endothelins are endothelium-derived vasoconstrictor peptides. Publication Abstract from PubMed Endothelin, a 21-amino-acid peptide, participates in various physiological processes, such as regulation of vascular tone, humoral homeostasis, neural crest cell development and neurotransmission. Endothelin and its G-protein-coupled receptor are involved in the development of various diseases, such as pulmonary arterial hypertension, and thus are important therapeutic targets. Here we report crystal structures of human endothelin type B receptor in the ligand-free form and in complex with the endogenous agonist endothelin-1. The structures and mutation analysis reveal the mechanism for the isopeptide selectivity between endothelin-1 and -3. Transmembrane helices 1, 2, 6 and 7 move and envelop the entire endothelin peptide, in a virtually irreversible manner. The agonist-induced conformational changes are propagated to the receptor core and the cytoplasmic G-protein coupling interface, and probably induce conformational flexibility in TM6. A comparison with the M2 muscarinic receptor suggests a shared mechanism for signal transduction in class A G-protein-coupled receptors. Activation mechanism of endothelin ETB receptor by endothelin-1.,Shihoya W, Nishizawa T, Okuta A, Tani K, Dohmae N, Fujiyoshi Y, Nureki O, Doi T Nature. 2016 Sep 5;537(7620):363-368. doi: 10.1038/nature19319. PMID:27595334 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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