6rz9

Crystal structure of the human cysteinyl leukotriene receptor 2 in complex with ONO-2770372

spinqualitylabelsall models 6rz9, resolution 2.73Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 6rz9 is a 1 chain structure with sequence from Escherichia coli and Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: X-ray diffraction, Resolution 2.73Å Ligands: 1PE, CLR, KO5, OLA, OLC Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Disease CLTR2_HUMAN Uveal melanoma. Function C562_ECOLX Electron-transport protein of unknown function.CLTR2_HUMAN Receptor for cysteinyl leukotrienes. The response is mediated via a G-protein that activates a phosphatidylinositol-calcium second messenger system. Stimulation by BAY u9773, a partial agonist, induces specific contractions of pulmonary veins and might also have an indirect role in the relaxation of the pulmonary vascular endothelium. The rank order of affinities for the leukotrienes is LTC4 = LTD4 >> LTE4. Publication Abstract from PubMed Cysteinyl leukotriene G protein-coupled receptors CysLT1 and CysLT2 regulate pro-inflammatory responses associated with allergic disorders. While selective inhibition of CysLT1R has been used for treating asthma and associated diseases for over two decades, CysLT2R has recently started to emerge as a potential drug target against atopic asthma, brain injury and central nervous system disorders, as well as several types of cancer. Here, we describe four crystal structures of CysLT2R in complex with three dual CysLT1R/CysLT2R antagonists. The reported structures together with the results of comprehensive mutagenesis and computer modeling studies shed light on molecular determinants of CysLTR ligand selectivity and specific effects of disease-related single nucleotide variants. Structural basis of ligand selectivity and disease mutations in cysteinyl leukotriene receptors.,Gusach A, Luginina A, Marin E, Brouillette RL, Besserer-Offroy E, Longpre JM, Ishchenko A, Popov P, Patel N, Fujimoto T, Maruyama T, Stauch B, Ergasheva M, Romanovskaia D, Stepko A, Kovalev K, Shevtsov M, Gordeliy V, Han GW, Katritch V, Borshchevskiy V, Sarret P, Mishin A, Cherezov V Nat Commun. 2019 Dec 6;10(1):5573. doi: 10.1038/s41467-019-13348-2. PMID:31811124 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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