Conformational changes in α7 acetylcholine receptors underlying allosteric modulation by divalent cations

BMC Pharmacology

Volumn 9, Issue , 2009, Pages

  McLaughlin, James T ^a   Barron, Sean C ^a   See, Jennifer A ^a   Rosenberg, Robert L ^a,b  

^a UNIVERSITY OF NORTH CAROLINA SCHOOL OF MEDICINE   (United States)

^b UNIVERSITY OF NORTH CAROLINA   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 AMINOETHYLMETHANE THIOSULFONATE; ALPHA 7 CHOLINERGIC RECEPTOR; BARIUM ION; CALCIUM ION; CHOLINERGIC RECEPTOR; CYSTEINE; DIVALENT CATION; GLUTAMIC ACID DERIVATIVE; SULFONIC ACID DERIVATIVE; UNCLASSIFIED DRUG; ACETYLCHOLINE; ACETYLCHOLINE RECEPTOR ALPHA SUBUNIT (125 148); ACETYLCHOLINE RECEPTOR ALPHA-SUBUNIT (125-148); BARIUM; CALCIUM; NICOTINIC RECEPTOR; PEPTIDE FRAGMENT;

ALLOSTERISM; AMINO ACID SUBSTITUTION; ARTICLE; BINDING SITE; CATION EXCHANGE; CHEMICAL MODIFICATION; CONFORMATIONAL TRANSITION; CONTROLLED STUDY; MOLECULAR MECHANICS; NONHUMAN; RESIDUE ANALYSIS; ANIMAL; CELL MEMBRANE POTENTIAL; DOSE RESPONSE; DRUG EFFECT; DRUG POTENTIATION; GENETICS; METABOLISM; OOCYTE; PHYSIOLOGY; PROTEIN BINDING; PROTEIN CONFORMATION; SITE DIRECTED MUTAGENESIS; XENOPUS LAEVIS;

ACETYLCHOLINE; ALLOSTERIC REGULATION; ALLOSTERIC SITE; AMINO ACID SUBSTITUTION; ANIMALS; BARIUM; CALCIUM; CATIONS, DIVALENT; CYSTEINE; DOSE-RESPONSE RELATIONSHIP, DRUG; MEMBRANE POTENTIALS; MUTAGENESIS, SITE-DIRECTED; OOCYTES; PEPTIDE FRAGMENTS; PROTEIN BINDING; PROTEIN CONFORMATION; RECEPTORS, NICOTINIC; XENOPUS LAEVIS;

EID: 60849136023     PISSN: None     EISSN: 14712210     Source Type: Journal    
DOI: 10.1186/1471-2210-9-1     Document Type: Article

References (40)

1. Lena C Changeux JP Allosteric modulations of the nicotinic acetylcholine receptor Trends Neurosci 1993, 16:181-186 7685943
2. Gao Z-G Jacobson KA Allosterism in membrane receptors Drug Discovery Today 2006, 11:191-202 16580596
3. Sigel E Mapping of the benzodiazepine recognition site on GABAA receptors Curr Top Med Chem 2002, 2:833-9 12171574
4. Changeux JP Taly A Nicotinic receptors, allosteric proteins and medicine Trends in Molecular Medicine 2008, 14:93-102 18262468
5. Sine SM The nicotinic receptor ligand binding domain J Neurobiol 2002, 53:431-46 12436411
6. Gay EA Yakel JL Gating of nicotinic ACh receptors; new insights into structural transitions triggered by agonist binding that induce channel opening J Physiol 2007, 584:727-733 2276999 17823204
7. Lee WY Sine SM Principal pathway coupling agonist binding to channel gating in nicotinic receptors Nature 2005, 438:243-7 16281039
8. Lummis SC Beene DL Lee LW Lester HA Broadhurst RW Dougherty DA Cis-trans isomerization at a proline opens the pore of a neurotransmitter-gated ion channel Nature 2005, 438:248-52 16281040
9. Mukhtasimova N Free C Sine SM Initial coupling of binding to gating mediated by conserved residues in the muscle nicotinic receptor J Gen Physiol 2005, 126:23-39 2266616 15955875
10. Brejc K van Dijk WJ Klaassen RV Schuurmans M Oost van Der J Smit AB Sixma TK Crystal structure of an ACh-binding protein reveals the ligand-binding domain of nicotinic receptors Nature 2001, 411:269-76 11357122
11. Celie PH Klaassen RV van Rossum-Fikkert SE van Elk R van Nierop P Smit AB Sixma TK Crystal structure of acetylcholine-binding protein from Bulinus truncatus reveals the conserved structural scaffold and sites of variation in nicotinic acetylcholine receptors J Biol Chem 2005, 280:26457-66 15899893
12. Celie PH van Rossum-Fikkert SE van Dijk WJ Brejc K Smit AB Sixma TK Nicotine and carbamylcholine binding to nicotinic acetylcholine receptors as studied in AChBP crystal structures Neuron 2004, 41:907-14 15046723
13. Smit AB Syed NI Schaap D van Minnen J Klumperman J Kits KS Lodder H Schors van der RC van Elk R Sorgedrager B Brejc K Sixma TK Geraerts WPM Glia-derived acetylcholine-binding protein that modulates synaptic transmission Nature 2001, 411:261-268 11357121
14. Hilf RJC Dutzler R X-ray structure of a prokaryotic pentameric ligand gated ion channel Nature 2008, 452:375-379 18322461
15. 2+-binding sites Proc Natl Acad Sci USA 2002, 99:3210-5 122498 11867716
16. Unwin N Refined structure of the nicotinic acetylcholine receptor at 4 Å resolution J Mol Biol 2005, 346:967-89 15701510
17. Kash TL Jenkins A Kelley JC Trudell JR Harrison NL Coupling of agonist binding to channel gating in the GABAA receptor Nature 2003, 421:272-275 12529644
18. Vernino S Amador M Luetje CW Patrick J Dani J Calcium modulation and high calcium permeability of neuronal nicotinic acetylcholine receptors Neuron 1992, 8:127-134 1370370
19. Mulle C Léna C Changeux JP Potentiation of nicotinic receptor response by external calcium in rat central neurons Neuron 1992, 8:937-45 1586487
20. Galzi JL Bertrand S Corringer PJ Changeux JP Bertrand D Identification of calcium binding sites that regulate potentiation of a neuronal nicotinic acetylcholine receptor EMBO J 1996, 15:5824-32 452330 8918460
21. 2+ , lines the extracellular vestibule Am J Physiol Cell Physiol 2002, 283:C1454-60 12372806
22. Dani JS Bertand D Nicotinic Acetylcholine Receptors and Nicotinic Cholinergic Mechanisms of the Central Nervous System Annu Rev Pharmacol Toxicol 2007, 47:699-729 17009926
23. Lyford LK Sproul AD Eddins D McLaughlin JT Rosenberg RL Agonist-induced conformational changes in the extracellular domain of alpha7 nicotinic acetylcholine receptors Mol Pharmacol 2003, 64:650-8 12920201
24. Karlin A Akabas MH Substituted-cysteine accessibility method Methods Enzymol 1993, 293:123-45
25. McLaughlin JT Fu J Rosenberg RL Agonist-driven conformational changes in the inner β sheet of alpha7 nicotinic receptors Mol Pharmacol 2007, 71:1312-8 17325129
26. McLaughlin JT Fu J Sproul AD Rosenberg RL Role of the outer β sheet in divalent cation modulation of alpha7 nicotinic receptors Mol Pharmacol 2006, 70:16-22 16533908
27. Monod J Wyman J Changeux JP On the nature of allosteric transitions: A plausible model J Mol Biol 1965, 12:88-118 14343300
28. Koshland DE Némethy G Filmer D Comparison of experimental binding data and theoretical models in proteins containing subunits Biochemistry 1966, 5:365-85 5938952
29. Prince RJ Sine SM Acetylcholine and epibatidine binding to muscle acetylcholine receptors distinguish between concerted and uncoupled models J Biol Chem 1999, 274:19623-9 10391899
30. Krauss M Korr D Herrmann A Hucho F Binding properties of agonists and antagonists to distinct allosteric states of the nicotinic acetylcholine receptor are incompatible with a concerted model J Biol Chem 2000, 275:30196-201 10900197
31. Sharkey LM Czajkowski C Individually monitoring ligand-induced changes in the structure of the GABAA receptor at benzodiazepine binding site and non-binding site interfaces Mol Pharmacol 2008, 74(1):203-12 18424553
32. Harding MM The architecture of metal coordination groups in proteins Acta Crystallogr D Biol Crystallogr 2004, 60:849-59 15103130
33. Santarelli VP Eastwood AL Dougherty DA Ahern CA Horn R Calcium Block of Single Sodium Channels: Role of a Pore-Lining Aromatic Residue Biophys J 2007, 93:2341-2349 1965434 17545248
34. Zhong W Gallivan JP Zhang Y Li L Lester HA Dougherty DA From ab initio quantum mechanics to molecular neurobiology: A cation-pi binding site in the nicotinic receptor Proc Natl Acad Sci USA 1998, 95:12088-93 22789 9770444
35. Revah F Bertrand D Galzi JL Devillers-Thiery A Mulle C Hussy N Bertrand S Ballivet M Changeux JP Mutations in the channel domain alter desensitization of a neuronal nicotinic receptor Nature 1991, 353:846-9 1719423
36. Colquhoun D Binding, gating, affinity and efficacy: The interpretation of structure-activity relationships for agonists and of the effects of mutating receptors Br J Pharmacol 1998, 125:924-47 1565672 9846630
37. Beene DL Brandt GS Zhong W Zacharias NM Lester HA Dougherty DA Cation-pi Interactions in Ligand Recognition by Serotonergic (5-HT3A) and Nicotinic Acetylcholine Receptors: The Anomalous Binding Properties of Nicotine Biochemistry 2002, 41:10262-10269 12162741
38. Halevi S McKay J Palfreyman M Yassin L Eshel M Jorgensen E Treinin M The C elegans ric-3 gene is required for maturation of nicotinic acetylcholine receptors EMBO J 2002, 21:1012-1020 125878 11867529
39. Millar NS RIC-3: A nicotinic acetylcholine receptor chaperone Br J Pharmacol 2008, 153(Suppl 1):S177-83 18246096
40. Pascual JM Karlin A State-dependent accessibility and electrostatic potential in the channel of the acetylcholine receptor. Inferences from rates of reaction of thiosulfonates with substituted cysteines in the M2 segment of the alpha subunit J Gen Physiol 1998, 111:717-39 2217151 9607933