A portable site: A binding element for 17β-estradiol can be placed on any subunit of a nicotinic α4β2 receptor

Journal of Neuroscience

Volumn 31, Issue 13, 2011, Pages 5045-5054

  Jin, Xiaochun ^a   Steinbach, Joe Henry ^a  

^a WASHINGTON UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ACETYLCHOLINE; COMPLEMENTARY DNA; ESTRADIOL; NICOTINIC RECEPTOR ALPHA4BETA2;

ANIMAL CELL; ARTICLE; BINDING SITE; CARBOXY TERMINAL SEQUENCE; CONTROLLED STUDY; ESTROGEN BINDING; HUMAN; NONHUMAN; NUCLEOTIDE SEQUENCE; OOCYTE; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN INTERACTION; XENOPUS;

AMINO ACID SEQUENCE; ANIMALS; BINDING SITES; ESTRADIOL; FEMALE; HUMANS; MOLECULAR SEQUENCE DATA; PROTEIN BINDING; PROTEIN STRUCTURE, TERTIARY; PROTEIN SUBUNITS; RECEPTORS, NICOTINIC; XENOPUS;

EID: 79955712436     PISSN: 02706474     EISSN: 15292401     Source Type: Journal    
DOI: 10.1523/JNEUROSCI.4802-10.2011     Document Type: Article

References (41)

1. Akabas MH (2004) GABAA receptor structure-function studies: a reexamination in light of new acetylcholine receptor structures. Int Rev Neurobiol 62:1-43.
2. Akk G, Covey DF, Evers AS, Steinbach JH, Zorumski CF, Mennerick S (2007) Mechanisms of neurosteroid interactions with GABAA receptors. Pharmacol Ther 116:35-57.
3. Belelli D, Lambert JJ (2005) Neurosteroids: endogenous regulators of the GABAA receptor. Nat Rev Neurosci 6:565-575.
4. Bouzat C, Bren N, Sine SM (1994) Structural basis of the different gating kinetics of fetal and adult acetylcholine receptors. Neuron 13:1395-1402.
5. Brejc K, van Dijk WJ, Klaassen RV, Schuurmans M, van Der Oost J, Smit AB, Sixma TK (2001) Crystal structure of an ACh-binding protein reveals the ligand-binding domain of nicotinic receptors. Nature 411:269-276.
6. Carbone AL, Moroni M, Groot-Kormelink PJ, Bermudez I (2009) Pentameric concatenated α42β23 and α43β22 nicotinic acetylcholine receptors: subunit arrangement determines functional expression. Br J Pharmacol 156:970-981.
7. Chang Y, Wang R, Barot S, Weiss DS (1996) Stoichiometry of a recombinant GABAA receptor. J Neurosci 16:5415-5424.
8. Cornil CA, Charlier TD (2010) Rapid behavioural effects of oestrogens and fast regulation of their local synthesis by brain aromatase. J Neuroendocrinol 22:664-673.
9. Curtis L, Buisson B, Bertrand S, Bertrand D (2002) Potentiation of human α4β2 neuronal nicotinic acetylcholine receptor by estradiol. Mol Pharmacol 61:127-135.
10. Dani JA, Bertrand D (2007) Nicotinic acetylcholine receptors and nicotinic cholinergic mechanisms of the central nervous system. Annu Rev Pharmacol Toxicol 47:699-729.
11. Exley R, Cragg SJ (2008) Presynaptic nicotinic receptors: a dynamic and diverse cholinergic filter of striatal dopamine neurotransmission. Br J Pharmacol 153 [Suppl 1]:S283-S297.
12. Gillies GE, McArthur S (2010) Estrogen actions in the brain and the basis for differential action in men and women: a case for sex-specific medicines. Pharmacol Rev 62:155-198.
13. Gotti C, Moretti M, Gaimarri A, Zanardi A, Clementi F, Zoli M (2007) Heterogeneity and complexity of native brain nicotinic receptors. Biochem Pharmacol 74:1102-1111.
14. Hales TG, Dunlop JI, Deeb TZ, Carland JE, Kelley SP, Lambert JJ, Peters JA (2006) Common determinants of single channel conductance within the large cytoplasmic loop of 5-hydroxytryptamine type 3 and α4β2 nicotinic acetylcholine receptors. J Biol Chem 281:8062-8071.
15. 125I]A-85380. Biochim Biophys Acta 1788:1987-1995.
16. Hosie AM, Wilkins ME, da Silva HM, Smart TG (2006) Endogenous neurosteroids regulate GABAA receptors through two discrete transmembrane sites. Nature 444:486-489.
17. Hsiao B, Mihalak KB, Repicky SE, Everhart D, Mederos AH, Malhotra A, Luetje CW (2006) Determinants of zinc potentiation on the α4 subunit of neuronal nicotinic receptors. Mol Pharmacol 69:27-36.
18. Jenkins A, Greenblatt EP, Faulkner HJ, Bertaccini E, Light A, Lin A, Andreasen A, Viner A, Trudell JR, Harrison NL (2001) Evidence for a common binding cavity for three general anesthetics within the GABAA receptor. J Neurosci 21:RC136(1-4).
19. Jin X, Covey DF, Steinbach JH (2009) Kinetic analysis of voltage-dependent potentiation and block of the glycine α3 receptor by a neuroactive steroid analogue. J Physiol 587:981-997.
20. Kuo YP, Xu L, Eaton JB, Zhao L, Wu J, Lukas RJ (2005) Roles for nicotinic acetylcholine receptor subunit large cytoplasmic loop sequences in receptor expression and function. J Pharmacol Exp Ther 314:455-466.
21. Labarca C, Nowak MW, Zhang H, Tang L, Deshpande P, Lester HA (1995) Channel gating governed symmetrically by conserved leucine residues in the M2 domain of nicotinic receptors. Nature 376:514-516.
22. Li GD, Chiara DC, Sawyer GW, Husain SS, Olsen RW, Cohen JB (2006) Identification of a GABAA receptor anesthetic binding site at subunit interfaces by photolabeling with an etomidate analog. J Neurosci 26:11599-11605.
23. Lightfoot AP, Kew JN, Skidmore J (2008) α7 nicotinic acetylcholine receptor agonists and positive allosteric modulators. Prog Med Chem 46:131-171.
24. Moroni M, Zwart R, Sher E, Cassels BK, Bermudez I (2006) α4β2 nicotinic receptors with high and low acetylcholine sensitivity: pharmacology, stoichiometry, and sensitivity to long-term exposure to nicotine. Mol Pharmacol 70:755-768.
25. 2+ potentiation. J Neurosci 28:6884-6894.
26. Mukai H, Tsurugizawa T, Ogiue-Ikeda M, Murakami G, Hojo Y, Ishii H, Kimoto T, Kawato S (2006) Local neurosteroid production in the hippocampus: influence on synaptic plasticity of memory. Neuroendocrinology 84:255-263.
27. Paradiso K, Zhang J, Steinbach JH (2001) The C terminus of the human nicotinic α4β2 receptor forms a binding site required for potentiation by an estrogenic steroid. J Neurosci 21:6561-6568.
28. Revah F, Bertrand D, Galzi JL, Devillers-Thiéry A, Mulle C, Hussy N, Bertrand S, Ballivet M, Changeux JP (1991) Mutations in the channel domain alter desensitization of a neuronal nicotinic receptor. Nature 353:846-849.
29. Rudolph U, Möhler H (2004) Analysis of GABAA receptor function and dissection of the pharmacology of benzodiazepines and general anesthetics through mouse genetics. Annu Rev Pharmacol Toxicol 44:475-498.
30. Schlichter R, Keller AF, De Roo M, Breton JD, Inquimbert P, Poisbeau P (2006) Fast nongenomic effects of steroids on synaptic transmission and role of endogenous neurosteroids in spinal pain pathways. J Mol Neurosci 28:33-51.
31. Seo S, Henry JT, Lewis AH, Wang N, Levandoski MM (2009) The positive allosteric modulator morantel binds at noncanonical subunit interfaces of neuronal nicotinic acetylcholine receptors. J Neurosci 29:8734-8742.
32. Sigel E, Buhr A (1997) The benzodiazepine binding site of GABAA receptors. Trends Pharmacol Sci 18:425-429.
33. Sine SM, Engel AG (2006) Recent advances in Cys-loop receptor structure and function. Nature 440:448-455.
34. Steinbach JH, Bracamontes J, Yu L, Zhang P, Covey DF (2000) Subunitspecific action of an anticonvulsant thiobutyrolactone on recombinant glycine receptors involves a residue in the M2 membrane-spanning region. Mol Pharmacol 58:11-17.
35. Swope SL, Moss SJ, Raymond LA, Huganir RL (1999) Regulation of ligandgated ion channels by protein phosphorylation. Adv Second Messenger Phosphoprotein Res 33:49-78.
36. Wang HL, Ohno K, Milone M, Brengman JM, Evoli A, Batocchi AP, Middleton LT, Christodoulou K, Engel AG, Sine SM (2000) Fundamental gating mechanism of nicotinic receptor channel revealed by mutation causing a congenital myasthenic syndrome. J Gen Physiol 116:449-462.
37. Yevenes GE, Moraga-Cid G, Peoples RW, Schmalzing G, Aguayo LG (2008) A selective G βγ-linked intracellular mechanism for modulation of a ligand-gated ion channel by ethanol. Proc Natl Acad Sci U S A 105:20523-20528.
38. Zhou Y, Nelson ME, Kuryatov A, Choi C, Cooper J, Lindstrom J (2003) Human α4β2 acetylcholine receptors formed from linked subunits. J Neurosci 23:9004-9015.
39. Zwart R, Vijverberg HP (1997) Potentiation and inhibition of neuronal nicotinic receptors by atropine: competitive and noncompetitive effects. Mol Pharmacol 52:886-895.
40. Zwart R, Vijverberg HP (1998) Four pharmacologically distinct subtypes of α4β2 nicotinic acetylcholine receptor expressed in Xenopus laevis oocytes. Mol Pharmacol 54:1124-1131.
41. Zwart R, Broad LM, Xi Q, Lee M, Moroni M, Bermudez I, Sher E (2006) 5-I A-85380 and TC-2559 differentially activate heterologously expressed α4β2 nicotinic receptors. Eur J Pharmacol 539:10-17.