Role of the agonist binding site in up-regulation of neuronal nicotinic α4β2 receptors

Molecular Pharmacology

Volumn 70, Issue 6, 2006, Pages 2037-2044

  Kishi, Masashi ^a   Steinbach, Joe Henry ^a  

^a WASHINGTON UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CARBACHOL; LOBELINE; NICOTINE; NICOTINIC ALPHA4BETA2 RECEPTOR; NICOTINIC RECEPTOR; RECEPTOR SUBUNIT; UNCLASSIFIED DRUG;

ARTICLE; CONTROLLED STUDY; DRUG BINDING SITE; GENE MUTATION; GENETIC TRANSFECTION; HUMAN; HUMAN CELL; NERVE CELL; NUCLEOTIDE SEQUENCE; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN STRUCTURE; RECEPTOR BINDING; RECEPTOR DOWN REGULATION; RECEPTOR UPREGULATION; SIGNAL TRANSDUCTION;

BINDING SITES; CELL LINE; ENZYME-LINKED IMMUNOSORBENT ASSAY; HUMANS; MUTATION; NICOTINIC AGONISTS; RECEPTORS, NICOTINIC; UP-REGULATION;

EID: 33751097513     PISSN: 0026895X     EISSN: 15210111     Source Type: Journal    
DOI: 10.1124/mol.106.029298     Document Type: Article

References (36)

1. Akk G (2001) Aromatics at the murine nicotinic receptor agonist binding site: mutational analysis of the αY93 and αW149 residues. J Physiol 535 (Pt 3):729-740.
2. Auta J, Longone P, Guidotti A, and Costa E (1999) The regulation of hippocampal nicotinic acetylcholine receptors (nAChRs) after a protracted treatment with selective or nonselective nAChR agonists. J Mol Neurosci 13:31-45.
3. Bertrand D, Galzi JL, Devillers-Thiery A, Bertrand S, and Changeux JP (1993) Mutations at two distinct sites within the channel domain M2 alter calcium permeability of neuronal α7 nicotinic receptor. Proc Natl Acad Sci USA 90:6971-6975.
4. Bonnert TP, McKernan RM, Farrar S, LeBourdelles B, Heavens RP, Smith DW, Hewson L, Rigby MR, Sirinathsinghji D, Brown N, et al. (1999) θ, a novel γ-aminobutyric acid type A receptor subunit. Proc Natl Acad Sci USA 96:9891-9896.
5. Buisson B and Bertrand D (2001) Chronic exposure to nicotine upregulates the human α4β2 nicotinic acytylcholine receptor function. J Neurosci 21:1819-1829.
6. Buisson B, Gopalakrishnan M, Arneric SP, Sullivan JP, and Bertrand D (1996) Human α4β2 neuronal nicotinic acetylcholine receptor in HEK 293 cells: a patch-clamp study. J Neurosci 16:7880-7891.
7. Chen J, Zhang Y, Akk G, Sine S, and Auerbach A (1995) Activation kinetics of recombinant mouse nicotinic acetylcholine receptors - mutations of α-subunit tyrosine 190 affect both binding and gating. Biophys J 69:849-859.
8. Corringer PJ, Galzi JL, Eisele JL, Bertrand S, Changeux JP, and Bertrand D (1995) Identification of a new component of the agonist binding site of the nicotinic α7 homooligomeric receptor. J Biol Chem 270:11749-11752.
9. Damaj MI, Patrick GS, Creasy KR, and Martin BR (1997) Pharmacology of lobeline, a nicotinic receptor ligand. J Pharmacol Exp Ther 282:410-419.
10. De Fusco M, Becchetti A, Patrignani A, Annesi G, Gambardella A, Quattrone A, Ballabio A, Wanke E, and Casari G (2000) The nicotinic receptor β2 subunit is mutant in nocturnal frontal lobe epilepsy. Nat Genet 26:275-276.
11. Fenster CP, Whitworth TL, Sheffield EB, Quick MW, and Lester RA (1999) Upregulation of surface α4β2 nicotinic receptors is initiated by receptor desensitization after chronic exposure to nicotine. J Neurosci 19:4804-4814.
12. Galzi JL, Bertrand D, Devillers-Thiery A, Revah F, Bertrand S, and Changeux JP (1991) Functional significance of aromatic amino acids from three peptide loops of the α7 neuronal nicotinic receptor site investigated by site-directed mutagenesis. FEBS Lett 294:198-202.
13. Gentry C and Lukas R (2002) Regulation of nicotinic acetylcholine receptor numbers and function by chronic nicotine exposure. Curr Drug Targets CNS Neurol Disord 1:359-385.
14. Gopalakrishnan M, Molinari EJ, and Sullivan JP (1997) Regulation of human α4β2 neuronal nicotinic acetylcholine receptors by cholinergic channel ligands and second messenger pathways. Mol Pharmacol 52:524-534.
15. Gopalakrishnan M, Monteggia LM, Anderson DJ, Molinari EJ, Piattonikaplan M, Donnelly-Roberts D, Arneric SP, and Sullivan JP (1996) Stable expression, pharmacologic properties and regulation of the human neuronal nicotinic acetylcholine α4β2 receptor. J Pharmacol Exp Ther 276:289-297.
16. Harkness PC and Millar NS (2002) Changes in conformation and subcellular distribution of α4β2 nicotinic acetylcholine receptors revealed by chronic nicotine treatment and expression of subunit chimeras. J Neurosci 22:10172-10181.
17. Khiroug SS, Harkness PC, Lamb PW, Sudweeks SN, Khiroug L, Millar NS, and Yakel JL (2002) Rat nicotinic ACh receptor α7 and β2 subunits co-assemble to form functional heteromeric nicotinic receptor channels. J Physiol 540 (Pt 2):425-434.
18. 2+ permeability, conductance, and gating of human α4β2 nicotinic acetylcholine receptors. J Neurosci 17:9035-9047.
19. Kuryatov A, Luo J, Cooper J, and Lindstrom J (2005) Nicotine acts as a pharmacological chaperone to up-regulate human α4β2 acetylcholine receptors. Mol Pharmacol 68:1839-1851.
20. Labarca C, Schwarz J, Deshpande P, Schwarz S, Nowak MW, Fonck C, Nashmi R, Kofuji P, Dang H, Shi W, et al. (2001) Point mutant mice with hypersensitive α4 nicotinic receptors show dopaminergic deficits and increased anxiety. Proc Natl Acad Sci USA 98:2786-2791.
21. 2+-binding sites. Proc Natl Acad Sci USA 99:3210-3215.
22. Lester HA, Dibas MI, Dahan DS, Leite JF, and Dougherty DA (2004) Cys-loop receptors: new twists and turns. Trends Neurosci 27:329-336.
23. Matsushima N, Hirose S, Iwata H, Fukuma G, Yonetani M, Nagayama C, Hamanaka W, Matsunaka Y, Ito M, Kaneko S, et al. (2002) Mutation (Ser284Leu) of neuronal nicotinic acetylcholine receptor α4 subunit associated with frontal lobe epilepsy causes faster desensitization of the rat receptor expressed in oocytes. Epilepsy Res 48:181-186.
24. Moroni M, Zwart R, Sher E, Cassels BK, and Bermudez I (2006) α4β2 nicotinic receptors with high and low acetylcholine sensitivity: pharmacology, stoichiometry and sensitivity to chronic exposure to nicotine. Mol Pharmacol 70:755-768.
25. Nashmi R, Dickinson ME, McKinney S, Jareb M, Labarca C, Fraser SE, and Lester HA (2003) Assembly of α4β2 nicotinic acetylcholine receptors assessed with functional fluorescently labeled subunits: effects of localization, trafficking, and nicotine-induced upregulation in clonal mammalian cells and in cultured midbrain neurons. J Neurosci 23:11554-11567.
26. Nelson ME, Kuryatov A, Choi CH, Zhou Y, and Lindstrom J (2003) Alternate stoichiometries of α4β2 nicotinic acetylcholine receptors. Mol Pharmacol 63:332-341.
27. Paradiso KG and Steinbach JH (2003) Nicotine is highly effective at producing desensitization of rat α4β2 neuronal nicotinic receptors. J Physiol 553 (Pt 3):857-871.
28. Peng X, Gerzanich V, Anand R, Whiting PJ, and Lindstrom J (1994) Nicotine-induced increase in neuronal nicotinic receptors results from a decrease in the rate of receptor turnover. Mol Pharmacol 46:523-530.
29. Sabey K, Paradiso K, Zhang J, and Steinbach JH (1999) Ligand binding and activation of rat nicotinic α4β2 receptors stably expressed in HEK293 cells. Mol Pharmacol 55:58-66.
30. Sallette J, Pons S, Devillers-Thiery A, Soudant M, Prado de Carvalho L, Changeux JP, and Corringer PJ (2005) Nicotine upregulates its own receptors through enhanced intracellular maturation. Neuron 46:595-607.
31. Sine SM (2002) The nicotinic receptor ligand binding domain. J Neurobiol 53:431-446.
32. Sine SM, Quiram P, Papanikolaou F, Kreienkamp HJ, and Taylor P (1994) Conserved tyrosines in the α subunit of the nicotinic acetylcholine receptor stabilize quaternary ammonium groups of agonists and curariform antagonists. J Biol Chem 269:8808-8816,.
33. Vallejo YF, Buisson B, Bertrand D, and Green WN (2005) Chronic nicotine exposure upregulates nicotinic receptors by a novel mechanism. J Neurosci 25:5563-5572.
34. Valluru L, Xu J, Zhu Y, Yan S, Contractor A, and Swanson GT (2005) Ligand binding is a critical requirement for plasma membrane expression of heteromeric kainate receptors. J Biol Chem 280:6085-6093.
35. Whiteaker P, Sharples CGV, and Wonnacott S (1998) Agonist-induced up-regulation of α4β2 nicotinic acetylcholine receptors in m10 cells - pharmacological and spatial definition. Mol Pharmacol 53:950-962.
36. Zhang J and Steinbach JH (2003) Cytisine binds with similar affinity to nicotinic α4β2 receptors on the cell surface and in homogenates. Brain Res 959:98-102.