Varenicline Interactions at the 5-HT3 Receptor Ligand Binding Site are Revealed by 5-HTBP

ACS Chemical Neuroscience

Volumn 6, Issue 7, 2015, Pages 1151-1157

  Price, Kerry L ^a   Lillestol, Reidun K ^a   Ulens, Chris ^b   Lummis, Sarah C R ^a  

^a UNIVERSITY OF CAMBRIDGE   (United Kingdom)

^b LABORATORY OF MOLECULAR AND CELLULAR SIGNALING   (Belgium)

Author keywords

Cys loop receptor; Ligand gated ion channel; serotonin receptor

Indexed keywords

BINDING PROTEIN; SEROTONIN 3 RECEPTOR; SEROTONIN BINDING PROTEIN; UNCLASSIFIED DRUG; VARENICLINE; CARRIER PROTEIN; HTR3A PROTEIN, MOUSE; SEROTONIN; SEROTONIN RECEPTOR AFFECTING AGENT; WATER;

ANIMAL CELL; ARTICLE; BINDING SITE; CONCENTRATION RESPONSE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG POTENCY; DRUG PROTEIN BINDING; GENE MUTATION; HEK293 CELL LINE; HYDROGEN BOND; LIGAND BINDING; MOLECULAR INTERACTION; MOUSE; NONHUMAN; OOCYTE; PARTIAL AGONISM; PRIORITY JOURNAL; XENOPUS; AMINO ACID SEQUENCE; ANIMAL; DRUG EFFECTS; GENETICS; HUMAN; METABOLISM; MOLECULAR MODEL; MUTATION; PATCH CLAMP TECHNIQUE; PROTEIN SECONDARY STRUCTURE; X RAY CRYSTALLOGRAPHY;

AMINO ACID SEQUENCE; ANIMALS; BINDING SITES; CARRIER PROTEINS; CRYSTALLOGRAPHY, X-RAY; HEK293 CELLS; HUMANS; HYDROGEN BONDING; MICE; MODELS, MOLECULAR; MUTATION; OOCYTES; PATCH-CLAMP TECHNIQUES; PROTEIN STRUCTURE, SECONDARY; RECEPTORS, SEROTONIN, 5-HT3; SEROTONIN; SEROTONIN AGENTS; VARENICLINE; WATER; XENOPUS;

EID: 84937034571     PISSN: None     EISSN: 19487193     Source Type: Journal    
DOI: 10.1021/cn500369h     Document Type: Article

References (30)

1. 3 receptors J. Biol. Chem. 287, 40239-40245
2. 3E Mol. Pharmacol. 72, 8-17
3. 3E receptor subunits: evolution, distribution and function J. Neurochem. 108, 384-396
4. Fagerstrom, K. and Hughes, J. (2008) Varenicline in the treatment of tobacco dependence Neuropsychiatr. Dis. Treat. 4, 353-363
5. Mihalak, K. B., Carroll, F. I., and Luetje, C. W. (2006) Varenicline is a partial agonist at α4β2 and a full agonist at α7 neuronal nicotinic receptors Mol. Pharmacol. 70, 801-805
6. 3 receptors expressed in Xenopus oocytes Neurosci. Lett. 247, 107-110
7. 3 receptor J. Pharmacol. Exp. Ther. 339, 125-131
8. 3 receptors Curr. Pharm. Des. 12, 3615-3630
9. 3 receptor antagonists: current uses and future directions Pharmacol Ther 130, 338-347
10. 3 receptors EMBO Rep. 14, 49-56
11. Billen, B., Spurny, R., Brams, M., van Elk, R., Valera-Kummer, S., Yakel, J. L., Voets, T., Bertrand, D., Smit, A. B., and Ulens, C. (2012) Molecular actions of smoking cessation drugs at α4β2 nicotinic receptors defined in crystal structures of a homologous binding protein Proc. Natl. Acad. Sci. U.S.A. 109, 9173-9178
12. Rucktooa, P., Haseler, C. A., van Elk, R., Smit, A. B., Gallagher, T., and Sixma, T. K. (2012) Structural characterization of binding mode of smoking cessation drugs to nicotinic acetylcholine receptors through study of ligand complexes with acetylcholine-binding protein J. Biol. Chem. 287, 23283-23293
13. 3 receptor Nature 512, 276-281
14. 3 receptor Biochemistry 47, 6370-6377
15. 3A) and Nicotinic Acetylcholine Receptors: The Anomalous Binding Properties of Nicotine Biochemistry 41, 10262-10269
16. Tavares, X. D. S., Blum, A. P., Nakamura, D. T., Puskar, N. L., Shanata, J. A. P., Lester, H. A., and Dougherty, D. A. (2012) Variations in Binding Among Several Agonists at Two Stoichiometries of the Neuronal, α4β2 Nicotinic Receptor J. Am. Chem. Soc. 134, 11474-11480
17. Van Arnam, E. B., Blythe, E. E., Lester, H. A., and Dougherty, D. A. (2013) An unusual pattern of ligand-receptor interactions for the α7 nicotinic acetylcholine receptor, with implications for the binding of varenicline Mol. Pharmacol. 84, 201-207
18. 3A serotonin receptor in an agonist-specific way ACS Chem. Neurosci. 3, 753-760
19. 3 receptor binding site using modeling and radioligand binding J. Biol. Chem. 280, 20476-20482
20. Puskar, N. L., Xiu, X., Lester, H. A., and Dougherty, D. A. (2011) Two neuronal nicotinic acetylcholine receptors, α4β4 and α7, show differential agonist binding modes J. Biol. Chem. 286, 14618-14627
21. 3 receptor ligand binding domain J. Biol. Chem. 275, 5620-5625
22. 3 receptor revealed by unnatural amino acid mutagenesis J. Neurosci. 24, 9097-9104
23. 3 receptor Biophys. J. 95, 5728-5736
24. 3A receptor model Biochemistry 45, 1099-1105
25. Blum, A. P., Lester, H. A., and Dougherty, D. A. (2010) Nicotinic pharmacophore: the pyridine N of nicotine and carbonyl of acetylcholine hydrogen bond across a subunit interface to a backbone NH Proc. Natl. Acad. Sci. U.S.A. 107, 13206-13211
26. Hansen, S. B., Sulzenbacher, G., Huxford, T., Marchot, P., Taylor, P., and Bourne, Y. (2005) Structures of Aplysia AChBP complexes with nicotinic agonists and antagonists reveal distinctive binding interfaces and conformations EMBO J. 24, 3635-3646
27. Brams, M., Pandya, A., Kuzmin, D., van Elk, R., Krijnen, L., Yakel, J. L., Tsetlin, V., Smit, A. B., and Ulens, C. (2011) A structural and mutagenic blueprint for molecular recognition of strychnine and d -tubocurarine by different Cys-loop receptors PLoS Biol. 9, e1001034
28. Hibbs, R. E., Sulzenbacher, G., Shi, J., Talley, T. T., Conrod, S., Kem, W. R., Taylor, P., Marchot, P., and Bourne, Y. (2009) Structural determinants for interaction of partial agonists with acetylcholine binding protein and neuronal α7 nicotinic acetylcholine receptor EMBO J. 28, 3040-3051
29. Rohde, L. A., Ahring, P. K., Jensen, M. L., Nielsen, E. O., Peters, D., Helgstrand, C., Krintel, C., Harpsoe, K., Gajhede, M., Kastrup, J. S., and Balle, T. (2012) Intersubunit bridge formation governs agonist efficacy at nicotinic acetylcholine α4β2 receptors: unique role of halogen bonding revealed J. Biol. Chem. 287, 4248-4259
30. 2+-and membrane potential-sensitive dyes: advantages and potential problems J. Neurosci. Methods 149, 172-177