Potentiation of α7 nicotinic acetylcholine receptors via an allosteric transmembrane site

Proceedings of the National Academy of Sciences of the United States of America

Volumn 105, Issue 38, 2008, Pages 14686-14691

  Young, Gareth T ^a   Zwart, Ruud ^b   Walker, Alison S ^b   Sher, Emanuele ^b   Millar, Neil S ^a  

^a UNIVERSITY COLLEGE LONDON   (United Kingdom)

^b ELI LILLY AND COMPANY   (United States)

Author keywords

Allosteric modulators; Neurotransmitter receptor

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR; ACETYLCHOLINE; BUNGAROTOXIN RECEPTOR; GLYCINE RECEPTOR; INHALATION ANESTHETIC AGENT; LY 2087101; NEUROSTEROID; NOOTROPIC AGENT; PNU 120596; PROTEIN SUBUNIT; SEROTONIN 3 RECEPTOR; UNCLASSIFIED DRUG; 1 (5 CHLORO 2,4 DIMETHOXYPHENYL) 3 (5 METHYLISOXAZOL 3 YL)UREA; 1-(5-CHLORO-2,4-DIMETHOXYPHENYL)-3-(5-METHYLISOXAZOL-3-YL)UREA; AMINO ACID; CARBANILAMIDE DERIVATIVE; CHIMERIC PROTEIN; ISOXAZOLE DERIVATIVE; NICOTINIC RECEPTOR;

ALLOSTERISM; ARTICLE; BINDING SITE; COMPUTER SIMULATION; CONTROLLED STUDY; DRUG RECEPTOR BINDING; LONG TERM POTENTIATION; MEMBRANE POTENTIAL; NONHUMAN; POINT MUTATION; PRIORITY JOURNAL; PROTEIN STRUCTURE; RAT; XENOPUS LAEVIS; ANIMAL; CHEMICAL STRUCTURE; CHEMISTRY; CHICKEN; DOSE RESPONSE; DRUG EFFECT; GENETICS; HUMAN; METABOLISM; MOUSE; MUTATION; OOCYTE; PROTEIN TERTIARY STRUCTURE;

ALLOSTERIC REGULATION; ALLOSTERIC SITE; AMINO ACIDS; ANIMALS; BINDING SITES; CHICKENS; COMPUTER SIMULATION; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; ISOXAZOLES; MICE; MODELS, MOLECULAR; MUTANT CHIMERIC PROTEINS; MUTATION; OOCYTES; PHENYLUREA COMPOUNDS; PROTEIN STRUCTURE, TERTIARY; RATS; RECEPTORS, NICOTINIC; XENOPUS LAEVIS;

EID: 55749111553     PISSN: 00278424     EISSN: 10916490     Source Type: Journal    
DOI: 10.1073/pnas.0804372105     Document Type: Article

References (43)

1. Lester HA, Dibas MI, Dahan DS, Leite JF, Dougherty DA (2004) Cys-loop receptors: New twists and turns. Trends Neurosci 27:329-336.
2. Ortells MO, Lunt GG (1995) Evolutionary history of the ligand-gated ion-channel superfamily of receptors. Trends Neurosci 18:121-127.
3. Changeux J-P, Edelstein SJ (2005) Allosteric mechanisms of signal transduction. Science 308:1424-1428.
4. Changeux J-P, Taly A (2008) Nicotinic receptors, allosteric proteins and medicine. Trends Mol Med 14:93-102.
5. Weiland S, Bertrand D, Leonard S (2000) Neuronal nicotinic acetylcholine receptors: From the gene to the disease. Behav Brain Res 113:43-56.
6. Levin ED, Rezvani AH (2007) Nicotinic interactions with antipsychotic drugs, models of schizophrenia and impacts on cognitive function. Biochem Pharmacol 74:1182-1191.
7. Jensen AA, Frolund B, Liljefors T, Krogsgaard-Larsen P (2005) Neuronal nicotinic acetylcholine receptors: Structural revelations, target identification, and therapeutic inspirations. J Med Chem 48:4705-4745.
8. Arneric SP, Holladay M, Williams M (2007) Neuronal nicotinic receptors: A perspective on two decades of drug discovery research. Biochem Pharmacol 74:1092-1101.
9. Le Novère N, Corringer P-J, Changeux J-P (2002) The diversity of subunit composition in nAChRs: Evolutionary origins, physiologic and pharmacologic consequences. J Neurobiol 53:447-456.
10. Millar NS (2003) Assembly and subunit diversity of nicotinic acetylcholine receptors. Biochem Soc Trans 31:869-874.
11. Couturier S, et al. (1990) A neuronal nicotinic acetylcholine receptor subunit (α7) is developmentally regulated and forms a homo-oligomeric channel blocked by α-BTX. Neuron 5:847-856.
12. Gerzanich V, Anand R, Lindstrom J (1994) Homomers of α8 and α7 subunits of nicotinic receptors exhibit similar channels but contrasting binding site properties. Mol Pharmacol 45:212-220.
13. 3 receptor, a serotonin-gated ion channel. Science 254:432-437.
14. Eiselé J-L, et al. (1993) Chimaeric nicotinic-serotonergic receptor combines distinct ligand binding and channel specificities. Nature 366:479-483.
15. 3 receptor subunit chimaeras. Br J Pharmacol 152:501-512.
16. Bertrand D, Gopalakrishnan M (2007) Allosteric modulation of nicotinic acetylcholine receptors. Biochem Pharmacol 74:115-1163.
17. Hurst RS, et al. (2005) A novel positive allosteric modulator of the α7 neuronal nicotinic acetylcholine receptor: In vitro and in vivo characterization. J Neurosci 25:4396-4405.
18. Timmermann DB, et al. (2007) An allosteric modulator of the α7 nicotinic acetylcholine receptor possessing cognition-enhancing properties in vivo. J Pharm Exp Ther 323:294-307.
19. A receptor modulators. Proc Natl Acad Sci USA 104:8059-8064.
20. Grønlien JH, et al. (2007) Distinct profiles of α7 nAChR positive allosteric modulation revealed by structurally diverse chemotypes. Mol Pharmacol 72:715-724.
21. Broad LM, et al. (2006) Identification and pharmacological profile of a new class of selective nicotinic acetylcholine receptor potentiators. J Pharm Exp Ther 318:1108-1117.
22. A and glycine receptors. Nature 389:385-389.
23. A receptors through two different discrete transmembrane sites. Nature 444:486-489.
24. Taly A, et al. (2005) Normal mode analysis suggests a quaternary twist model for the nicotinic receptor gating mechanism. Biophys J 88:3954-3965.
25. Cheng X, Benzhuo L, Grant B, Law RJ, McCammon JA (2006) Channel opening motion of α7 nicotinic acetylcholine receptor as suggested by normal mode analysis. J Mol Biol 355:310-234.
26. Miyazawa A, Fujiyoshi Y, Unwin N (2003) Structure and gating mechanism of the acetylcholine receptor pore. Nature 423:949-955.
27. Unwin N (2005) Refined structure of the nicotinic acetylcholine receptor at 4Å resolution. J Mol Biol 346:967-989.
28. Morris GM, et al. (1998) Automated docking using a lamarckian genetic algorithm and an empirical binding free energy function. J Comput Chem 19:1639-1662.
29. Taly A, et al. (2006) Implications of the quaternary twist allosteric model for the physiology and pathology of nicotinic acetylcholine receptors. Proc Natl Acad Sci USA 103:16965-16970.
30. Hetényi C, van der Spoel D (2006) Blind docking of drug-sized compounds to proteins with up to a thousand residues. FEBS Lett 580:1447-1450.
31. Unwin N (1995) Acetylcholine receptor channel imaged in the open state. Nature 373:37-43.
32. Monod J, Wyman J, Changeux J-P (1965) On the nature of allosteric transitions: A plausible model. J Mol Biol 12:88-118.
33. Changeux J-P, Edelstein SJ (2005) Nicotinic Acetylcholine Receptors from Molecular Biology to Cognition (Odile Jacob, New York).
34. Galzi J-L, Edelstein SJ, Changeux J-P (1996) The multiple phenotypes of allosteric receptor mutants. Proc Natl Acad Sci USA 93:1853-1858.
35. Ye Q, et al. (1998) Enhancement of glycine receptor function by ethanol is inversely correlated with molecular volume at position α267. J Biol Chem 273:3314-3319.
36. Lobo IA, Trudell JR, Harris RA (2006) Accessibility to residues in transmembrane segment four of the glycine receptor. Neuropharmacol 50:174-181.
37. 3H]azietomidate, a photoactivatable general anesthetic. J Biol Chem 279:17640-17649.
38. 3H]Benzophenone photolabeling identifies state-dependent changes in nicotinic acetylcholine receptor structure. Biochem 46:10296-10307.
39. Schrattenholz A, Godovac-Zimmernamm J, Schäfer H-J, Albuquerque EX, Maelicke A (1993) Photoaffinity labeling of. Torpedo acetylcholine receptor by physostigmine. Eur J Biochem 216:671-677.
40. Iorga B, Herlem D, Barré E, Guillou C (2006) Acetylcholine nicotinic receptors: Finding the putative binding site of allosteric modulators using the "blind docking" approach. J Mol Model 12:366-372.
41. Hansen SB, Taylor P (2007) Galanthamine and non-competitive inhibitor binding to ACh-binding protein: Evidence for a binding site on non-α-subunit interfaces of heteromeric neuronal nicotinic receptors. J Mol Biol 369:895-901.
42. Young GT, et al. (2007) Species selectivity of a nicotinic acetylcholine receptor agonist is conferred by two adjacent extracellular β4 amino acids that are implicated in the coupling of binding to channel gating. Mol Pharmacol 71:389-397.
43. Huey R, Morris GM, Olson AJ, Goodsell DS (2007) A semiemprical free energy force field with charge-based desolvation. J Comput Chem 28:1145-1152.