Homologous mutations on different subunits cause unequal but additive effects on n-alcohol block in the nicotinic receptor pore

Biophysical Journal

Volumn 72, Issue 5, 1997, Pages 2170-2179

  Forman, Stuart A ^a  

^a MASSACHUSETTS GENERAL HOSPITAL   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CHOLINERGIC RECEPTOR; NICOTINIC RECEPTOR;

AMINO ACID SEQUENCE; ANIMAL CELL; ARTICLE; CHANNEL GATING; CHOLINERGIC RECEPTOR BLOCKING; GENE EXPRESSION; NONHUMAN; OOCYTE; SITE DIRECTED MUTAGENESIS; XENOPUS LAEVIS;

ANIMALIA; XENOPUS LAEVIS;

EID: 0030933010     PISSN: 00063495     EISSN: None     Source Type: Journal    
DOI: 10.1016/s0006-3495(97)78860-x     Document Type: Article

References (43)

1. Adams, P. R. 1976. Drug blockade of open end-plate channels. J. Physiol. (Lond.). 260:531-552.
2. Akabas, M. H., C. Kaufmann, P. Archdeacon, and A. Karlin. 1994. Identification of acetylcholine receptor channel-lining residues in the entire M2 segment of the alpha subunit. Neuron. 13:919-927.
3. Buller, A. L., and M. M. White. 1990. Functional acetylcholine receptors expressed in Xenopus oocytes after injection of Torpedo beta, gamma, and delta subunit RNAs are a consequence of endogenous oocyte gene expression. Mol. Pharmacol. 37:423-428.
4. Charnet, P., C. Labarca, R. J. Leonard, N. J. Vogelaar, L. Czyzyk, A. Gouin, N. Davidson, and H. A. Lester. 1990. An open-channel blocker interacts with adjacent turns of alpha-helices in the nicotinic acetylcholine receptor. Neuron. 4:87-95.
5. Charnet, P., C. Labarca, and H. A. Lester. 1992. Structure of the gamma-less nicotinic acetylcholine receptor: learning from omission. Mol. Pharmacol. 41:708-717.
6. + permeability ratios of nicotinic acetylcholine receptors are reduced by mutations near the intracellular end of the M2 region. J. Gen. Physiol. 99:545-572.
7. Cohen, B. N., C. Labarca, N. Davidson, and H. A. Lester. 1992b. Mutations in M2 alter the selectivity of the mouse nicotinic acetylcholine receptor for organic and alkali metal cations. J. Gen. Physiol. 100: 373-400.
8. Devillers-Thiery, A., J. L. Galzi, J. L. Eisele, S. Bertrand, D. Bertrand, and J. P. Changeux. 1993. Functional architecture of the nicotinic acetylcholine receptor, a prototype of ligand-gated ion channels. [Review]. J. Membr. Biol. 136:97-112.
9. Dilger, J. P., and R. S. Brett. 1991. Actions of volatile anesthetics and alcohols on cholinergic receptor channels. Ann. N.Y. Acad. Sci. 625: 616-627.
10. Dilger, J. P., R. S. Brett, and L. A. Lesko. 1991. Effects of isoflurane on acetylcholine receptor channels. 1. Single-channel currents. Mol. Pharmacol. 41:127-133.
11. Filatov, G. N., and M. M. White. 1995. The role of conserved leucines in the M2 domain of the acetylcholine receptor in channel gating. Mol. Pharmacol. 48:379-384.
12. Finer-Moore, J., and R. M. Stroud. 1984. Amphipathic analysis and possible formation of the ion channel in an acetylcholine receptor. Proc. Natl. Acad. Sci. USA. 81:155-159.
13. Forman, S. A., K. W. Miller, and G. Yellen. 1995. A discrete site for general anesthetics on a postsynaptic receptor. Mol. Pharmacol. 48: 574-581.
14. 3H]chlorpromazine. Proc. Natl. Acad. Sci. USA. 83: 2719-2723.
15. 3H]chlorpromazine labels homologous residues in the beta and delta chains. Biochemistry. 26:2410-2418.
16. Heginbotham, L., and R. MacKinnon. 1992. The aromatic binding site for tetraethylammonium ion on potassium channels. Neuron. 8:483-491.
17. Hucho, F., W. Oberthur, and F. Lottspeich. 1986. The ion channel of the nicotinic acetylcholine receptor is formed by the homologous helices M II of the receptor subunits. FEBS Lett. 205:137-142.
18. Imoto, K., C. Busch, B. Sakmann, M. Mishina, T. Konno, J. Nakai, H. Bujo, Y. Mori, K. Fukuda, and S. Numa. 1988. Rings of negatively charged amino acids determine the acetylcholine receptor channel conductance. Nature. 335:645-648.
19. Imoto, K., T. Konno, J. Nakai, F. Wang, M. Mishina, and S. Numa. 1991. A ring of uncharged polar amino acids as a component of channel constriction in the nicotinic acetylcholine receptor. FEBS Lett. 289: 193-200.
20. Jackson, M. B., K. Imoto, M. Mishina, T. Konno, S. Numa, and B. Sakmann. 1990. Spontaneous and agonist-induced openings of an acetylcholine receptor channel composed of bovine α-, β-, and δ-subunits. Pflugers Arch. 417:129-135.
21. Karlin, A., P. N. Kao, and M. DiPaola. 1986. Molecular pharmacology of the nicotinic acetylcholine receptor. Trends Pharmacol. Sci. 7:304-308.
22. Kienker, P., G. Tomaselli, M. Jurman, and G. Yellen. 1994. Conductance mutations of the nicotinic acetylcholine receptor do not act by a simple electrostatic mechanism. Biophys. J. 66:325-334.
23. Kistler, J., R. M. Stroud, W. Klymkowsky, R. A. Lalancette, and R. H. Fairclough. 1982. Structure and function of an acetylcholine receptor. Biophys. J. 37:371-383.
24. Krieg, P. A., and D. A. Melton. 1984. Functional messenger RNAs are produced by SP6 in vitro transcription of cloned cDNAs. Nucleic Acids. Res. 12:7057-7070.
25. Labarca, C., M. W. Nowak, H. Zhang, L. Tang, P. Deshpande, and H. A. Lester. 1995. Channel gating governed symmetrically by conserved leucine residues in the M2 domain of nicotinic receptors. Nature. 376: 514-516.
26. Lechleiter, J., and R. Gruener. 1984. Halothane shortens acetylcholine receptor channel kinetics without affecting conductance. Proc. Natl. Acad. Sci. USA. 81:2929-2933.
27. Leonard, R. J., C. G. Labarca, P. Charnet, N. Davidson, and H. A. Lester. 1988. Evidence that the M2 membrane-spanning region lines the ion channel pore of the nicotinic receptor. Science. 242:1578-1581.
28. Liu, Y., and J. P. Dilger. 1991. Opening rate of acetylcholine receptor channels. Biophys. J. 60:424-432.
29. Lo, D. C., J. L. Pinkham, and C. F. Stevens. 1990. Influence of the gamma subunit and expression system on acetylcholine receptor gating. Neuron. 5:857-866.
30. McLarnon, J. G., P. Pennefather, and D. M. J. Quastel. 1988. Mechanisms of nicotinic channel blockade by anesthetics. In Molecular and Cellular Mechanisms of Anesthetics. S. H. Roth and K. W. Miller, editors. Plenum Publishing Corp., New York. 155-164.
31. Miller, C. 1989. Genetic manipulation of ion channels: a new approach to structure and function. Neuron. 2:1195-1205.
32. Nelson, R. M., and G. L. Long. 1989. A general method of site-specific mutagenesis using a modification of the Thermus aquaticus polymerase chain reaction. Anal. Biochem. 180:147-151.
33. Ogden, D. C., and D. Colquhoun. 1983. The efficacy of agonists at the frog neuromuscular junction studied with single channel recording. Pflugers Arch. 399:246-248.
34. 3H]meproadifen mustard reacts selectively with alpha-subunit Glu-262. J. Biol. Chem. 267:10489-10499.
35. 3H]chlorpromazine labels three amino acids of the acetylcholine receptor gamma subunit: implications for the alpha-helical organization of regions MII and for the structure of the ion channel. Proc. Natl. Acad. Sci. USA. 87:4675-4679.
36. Sankararamakrishnan, R., C. Adcock, and M. S. P. Sansom. 1996. The pore domain of the nicotinic acetylcholine receptor: molecular modeling, pore dimensions, and electrostatics. Biophys. J. 71:1659-1671.
37. Tomaselli, G. F., J. T. McLaughlin, M. E. Jurman, E. Hawrot, and G. Yellen. 1991. Mutations affecting agonist sensitivity of the nicotinic acetylcholine receptor. Biophys. J. 60:721-727.
38. Unwin, N. 1993. Nicotinic acetylcholine receptor at 9 Å resolution. J. Mol. Biol. 229:1101-1124.
39. Villarroel, A., S. Herlitze, M. Koenen, and B. Sakmann. 1991. Location of a threonine residue in the alpha-subunit M2 transmembrane segment that determines the ion flow through the acetylcholine receptor channel. Proc. R. Soc. Lond. B. 243:69-74.
40. Villarroel, A., S. Herlitze, V. Witzemann, M. Koenen, and B. Sakmann. 1992. Asymmetry of the rat acetylcholine receptor subunits in the narrow region of the pore. Proc. R. Soc. Lond. B. 249:317-324.
41. Wells, J. A. 1990. Additivity of mutational effects in proteins. Biochemistry. 29:8509-8517.
42. White, B. H., and J. B. Cohen. 1992. Agonist-induced changes in the structure of the acetylcholine receptor M2 regions revealed by photoincorporation of an uncharged nicotinic noncompetitive antagonist. J. Biol. Chem. 267:15770-15783.
43. Wood, S. C., P. H. Tonner, A. J. de Armendi, B. Bugge, and K. W. Miller. 1995. Channel inhibition by alkanols occurs at a binding site on the nicotinic acetylcholine receptor. Mol. Pharmacol. 47:121-130.