Structural characterization and agonist binding to human α4β2 nicotinic receptors

Sine, 2006, Recent advances in Cys-loop receptor structure and function, Nature, 440, 448, 10.1038/nature04708 Baenziger, 2011, 3D structure and allosteric modulation of the transmembrane domain of pentameric ligand-gated ion channels, Neuropharmacology, 60, 116, 10.1016/j.neuropharm.2010.08.007 Unwin, 1998, The nicotinic acetylcholine receptor of the Torpedo electric ray, J. Struct. Biol., 121, 181, 10.1006/jsbi.1997.3949 Unwin, 2005, Refined structure of the nicotinic acetylcholine receptor at 4A resolution, J. Mol. Biol., 346, 967, 10.1016/j.jmb.2004.12.031 Smit, 2001, A glia-derived acetylcholine-binding protein that modulates synaptic transmission, Nature, 411, 261, 10.1038/35077000 Brejc, 2001, Crystal structure of an ACh-binding protein reveals the ligand-binding domain of nicotinic receptors, Nature, 411, 269, 10.1038/35077011 Tasneem, 2005, Identification of the prokaryotic ligand-gated ion channels and their implications for the mechanisms and origins of animal Cys-loop ion channels, Genome Biol., 6, R4, 10.1186/gb-2004-6-1-r4 Bocquet, 2009, X-ray structure of a pentameric ligand-gated ion channel in an apparently open conformation, Nature, 457, 111, 10.1038/nature07462 Hilf, 2008, X-ray structure of a prokaryotic pentameric ligand-gated ion channel, Nature, 452, 375, 10.1038/nature06717 Hilf, 2009, Structure of a potentially open state of a proton-activated pentameric ligand-gated ion channel, Nature, 457, 115, 10.1038/nature07461 Gotti, 2006, Brain nicotinic acetylcholine receptors: native subtypes and their relevance, Trends Pharmacol. Sci., 27, 482, 10.1016/j.tips.2006.07.004 Wonnacott, 1997, Presynaptic nicotinic ACh receptors, Trends Neurosci., 20, 92, 10.1016/S0166-2236(96)10073-4 Grady, 2010, Mouse striatal dopamine nerve terminals express alpha4alpha5beta2 and two stoichiometric forms of alpha4beta2∗-nicotinic acetylcholine receptors, J. Mol. Neurosci., 40, 91, 10.1007/s12031-009-9263-y Flores, 1992, A subtype of nicotinic cholinergic receptor in rat brain is composed of alpha 4 and beta 2 subunits and is up-regulated by chronic nicotine treatment, Mol. Pharmacol., 41, 31 Rueter, 2006, A-85380: a pharmacological probe for the preclinical and clinical investigation of the alphabeta neuronal nicotinic acetylcholine receptor, CNS Drug Rev., 12, 100, 10.1111/j.1527-3458.2006.00100.x Ebbert, 2009, Emerging drugs for the treatment of tobacco dependence, Expert Opin. Emerg. Drugs, 14, 23, 10.1517/14728210802623874 Damaj, 2007, Genetic approaches identify differential roles for alpha4beta2∗ nicotinic receptors in acute models of antinociception in mice, J. Pharmacol. Exp. Ther., 321, 1161, 10.1124/jpet.106.112649 Picciotto, 2008, Neuroprotection via nAChRs: the role of nAChRs in neurodegenerative disorders such as Alzheimer’s and Parkinson’s disease, Front. Biosci., 13, 492, 10.2741/2695 Zhang, 2003, Cytisine binds with similar affinity to nicotinic alpha4beta2 receptors on the cell surface and in homogenates, Brain Res., 959, 98, 10.1016/S0006-8993(02)03733-2 Hamouda, 2007, Identifying the lipid–protein interface of the alpha4beta2 neuronal nicotinic acetylcholine receptor: hydrophobic photolabeling studies with 3-(trifluoromethyl)-3-(m-[(125)I]iodophenyl)diazirine, Biochemistry, 46, 13837, 10.1021/bi701705r daCosta, 2009, A lipid-dependent uncoupled conformation of the acetylcholine receptor, J. Biol. Chem., 284, 17819, 10.1074/jbc.M900030200 daCosta, 2002, Lipid–protein interactions at the nicotinic acetylcholine receptor. A functional coupling between nicotinic receptors and phosphatidic acid-containing lipid bilayers, J. Biol. Chem., 277, 201, 10.1074/jbc.M108341200 Baenziger, 1992, Probing conformational changes in the nicotinic acetylcholine receptor by Fourier transform infrared difference spectroscopy, Biophys. J., 62, 64, 10.1016/S0006-3495(92)81780-0 Baenziger, 1992, Incorporation of the nicotinic acetylcholine receptor into planar multilamellar films: characterization by fluorescence and Fourier transform infrared difference spectroscopy, Biophys. J., 61, 983, 10.1016/S0006-3495(92)81905-7 Methot, 1995, Structure of both the ligand- and lipid-dependent channel-inactive states of the nicotinic acetylcholine receptor probed by FTIR spectroscopy and hydrogen exchange, Biochemistry, 34, 15142, 10.1021/bi00046a021 Baenziger, 1995, Fourier transform infrared and hydrogen/deuterium exchange reveal an exchange-resistant core of alpha-helical peptide hydrogens in the nicotinic acetylcholine receptor, J. Biol. Chem., 270, 29129, 10.1074/jbc.270.49.29129 Dousseau, 1990, Determination of the secondary structure content of proteins in aqueous solutions from their amide I and amide II infrared bands. Comparison between classical and partial least-squares methods, Biochemistry, 29, 8771, 10.1021/bi00489a038 Baenziger, 1997, Desensitization of the nicotinic acetylcholine receptor mainly involves a structural change in solvent-accessible regions of the polypeptide backbone, Biochemistry, 36, 3617, 10.1021/bi962845m Baenziger, 1993, Fourier transform infrared difference spectroscopy of the nicotinic acetylcholine receptor: evidence for specific protein structural changes upon desensitization, Biochemistry, 32, 5448, 10.1021/bi00071a022 Baenziger, 2008, Lipid composition alters drug action at the nicotinic acetylcholine receptor, Mol. Pharmacol., 73, 880, 10.1124/mol.107.039008 Ryan, 1999, A structure-based approach to nicotinic receptor pharmacology, Mol. Pharmacol., 55, 348, 10.1124/mol.55.2.348 Ryan, 2002, Dissecting the chemistry of nicotinic receptor–ligand interactions with infrared difference spectroscopy, J. Biol. Chem., 277, 10420, 10.1074/jbc.M107412200 Barth, 2000, Prog. Biophys. Mol. Biol., 74, 141, 10.1016/S0079-6107(00)00021-3 Celie, 2004, Nicotine and carbamylcholine binding to nicotinic acetylcholine receptors as studied in AChBP crystal structures, Neuron, 41, 907, 10.1016/S0896-6273(04)00115-1 Blum, 2010, Inaugural article: nicotinic pharmacophore: the pyridine N of nicotine and carbonyl of acetylcholine hydrogen bond across a subunit interface to a backbone NH, Proc. Natl. Acad. Sci. USA, 107, 13206, 10.1073/pnas.1007140107 Xiu, 2009, Nicotine binding to brain receptors requires a strong cation–pi interaction, Nature, 458, 534, 10.1038/nature07768 Hill, 2006, The net orientation of nicotinic receptor transmembrane alpha-helices in the resting and desensitized states, Biophys. J., 91, 705, 10.1529/biophysj.106.082693 Zhong, 1998, From ab initio quantum mechanics to molecular neurobiology: a cation–pi binding site in the nicotinic receptor, Proc. Natl. Acad. Sci USA, 95, 12088, 10.1073/pnas.95.21.12088