4dkl | pdb_00004dkl

Crystal structure of the mu-opioid receptor bound to a morphinan antagonist

spinqualitylabelsall models 4dkl, resolution 2.80Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 4dkl is a 1 chain structure with sequence from Enterobacteria phage t4. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: 1PE, BF0, CL, CLR, MPG, SO4 Gene: Mor, Oprm, Oprm1, E (Enterobacteria phage T4) Activity: Lysozyme, with EC number 3.2.1.17 Resources: FirstGlance, OCA, RCSB, PDBsum Publication Abstract from PubMed Opium is one of the world's oldest drugs, and its derivatives morphine and codeine are among the most used clinical drugs to relieve severe pain. These prototypical opioids produce analgesia as well as many undesirable side effects (sedation, apnoea and dependence) by binding to and activating the G-protein-coupled micro-opioid receptor (micro-OR) in the central nervous system. Here we describe the 2.8 A crystal structure of the mouse micro-OR in complex with an irreversible morphinan antagonist. Compared to the buried binding pocket observed in most G-protein-coupled receptors published so far, the morphinan ligand binds deeply within a large solvent-exposed pocket. Of particular interest, the micro-OR crystallizes as a two-fold symmetrical dimer through a four-helix bundle motif formed by transmembrane segments 5 and 6. These high-resolution insights into opioid receptor structure will enable the application of structure-based approaches to develop better drugs for the management of pain and addiction. Crystal structure of the micro-opioid receptor bound to a morphinan antagonist.,Manglik A, Kruse AC, Kobilka TS, Thian FS, Mathiesen JM, Sunahara RK, Pardo L, Weis WI, Kobilka BK, Granier S Nature. 2012 Mar 21. doi: 10.1038/nature10954. PMID:22437502 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also G protein-coupled receptor Lysozyme 3D structures Mu Opioid Receptor Bound to a Morphinan Antagonist Opioid receptor

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