Loop B is a major structural component of the 5-HT3 receptor

Biophysical Journal

Volumn 95, Issue 12, 2008, Pages 5728-5736

  Thompson, A J ^a   Lochner, M ^b   Lummis, Sarah C R ^a  

^a UNIVERSITY OF CAMBRIDGE   (United Kingdom)

^b UNIVERSITY OF WARWICK   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

ALANINE; MUTANT PROTEIN; SEROTONIN 3 RECEPTOR;

AMINO ACID SEQUENCE; ANIMAL; ARTICLE; CATTLE; CELL LINE; CHEMICAL STRUCTURE; CHEMISTRY; GENETICS; HUMAN; IMMUNOHISTOCHEMISTRY; METABOLISM; MOLECULAR GENETICS; MUTAGENESIS; MUTATION; NUCLEOTIDE SEQUENCE; PROTEIN BINDING; PROTEIN CONFORMATION;

ALANINE; AMINO ACID SEQUENCE; ANIMALS; CATTLE; CELL LINE; CONSERVED SEQUENCE; HUMANS; IMMUNOHISTOCHEMISTRY; MODELS, MOLECULAR; MOLECULAR SEQUENCE DATA; MUTAGENESIS; MUTANT PROTEINS; MUTATION; PROTEIN BINDING; PROTEIN CONFORMATION; RECEPTORS, SEROTONIN, 5-HT3;

EID: 58749083050     PISSN: 00063495     EISSN: 15420086     Source Type: Journal    
DOI: 10.1529/biophysj.108.135624     Document Type: Article

References (33)

1. 3 Receptor as a therapeutic target. Expert Opin. Ther. Targets. 11:527-540.
2. Brejc, K., W. J. van Dijk, R. V. Klaassen, M. Schuurmans, J. van Der Oost, A. B. Smit, and T. K. Sixma. 2001. Crystal structure of an ACh-binding protein reveals the ligand-binding domain of nicotinic receptors. Nature. 411:269-276.
3. Celie, P. H., S. E. van Rossum-Fikkert, W. J. van Dijk, K. Brejc, A. B. Smit, and T. K. Sixma. 2004. Nicotine and carbamylcholine binding to nicotinic acetylcholine receptors as studied in AChBP crystal structures. Neuron. 41:907-914.
4. Celie, P. H., R. V. Klaassen, S. E. van Rossum-Fikkert, R. van Elk, P. van Nierop, A. B. Smit, and T. K. Sixma. 2005. 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. 280:26457-26466.
5. Unwin, N. 2005. Refined structure of the nicotinic acetylcholine receptor at 4Å resolution. J. Mol. Biol. 346:967-989.
6. Dellisanti, C. D., Y. Yao, J. C. Stroud, Z. Z. Wang, and L. Chen. 2007. Crystal structure of the extracellular domain of nAChR α1 bound to α-bungarotoxin at 1.94 Å resolution. Nat. Neurosci. 10:953-962.
7. Hilf, R. J., and R. Dutzler. 2008. X-ray structure of a prokaryotic pentameric ligand-gated ion channel. Nature. 452:375-379.
8. 3 receptors. Curr. Pharm. Des. 12:3615-3630.
9. 3 receptor binding site using modeling and radioligand binding. J. Biol. Chem. 280:20476-20482.
10. 3 receptor. Mol. Pharmacol. 68:365-371.
11. 3A receptor model. Biochemistry. 45:1099-1105.
12. Chen, C. A., and H. Okayama. 1988. Calcium phosphate-mediated gene transfer: a highly efficient transfection system for stably transforming cells with plasmid DNA. Biotechniques. 6:632-638.
13. Jordan, M., A. Schallhorn, and F. M. Wurm. 1996. Transfecting mammalian cells: optimization of critical parameters affecting calcium-phosphate precipitate formation. Nucleic Acids Res. 24:596-601.
14. Kunkel, T. A. 1985. Rapid and efficient site-specific mutagenesis without phenotypic selection. Proc. Natl. Acad. Sci. USA. 82:488-492.
15. Price, K. L., and S. C. Lummis. 2004. The role of tyrosine residues in the extracellular domain of the 5-hydroxytryptamine3 receptor. J. Biol. Chem. 279:23294-23301.
16. Bylund, D. B., and M. L. Toews. 1993. Radioligand binding methods: practical guide and tips. Am. J. Physiol. 265:421-429.
17. 3 receptor label both native and recombinant receptors. Brain Res. Mol. Brain Res. 67:221-230.
18. Fitch, R.W., Y. Xiao, Y., K.J. Kellar, and J. W. Daly. 2003 Membrane potential fluorescence: a rapid and highly sensitive assay for nicotinic receptor channel function. Proc. Natl. Acad. Sci. USA. 100:4909-4914.
19. 2+ - and membrane potential-sensitive dyes: advantages and potential problems. J. Neurosci. Methods. 149:172-177.
20. Chakrapani, S., T. D. Bailey, and A. Auerbach. 2003. The role of loop 5 in acetylcholine receptor channel gating. J. Gen. Physiol. 122:521-539.
21. 3 receptor agonist-binding residues using homology modeling. Biophys. J. 84:2338-2344.
22. Sali, A., and T. L. Blundell. 1993. Comparative protein modelling by satisfaction of spatial restraints. J. Mol. Biol. 234:779-815.
23. Weiner, S. J., P. A. Kollman, D. A. Case, U. C. Singh, C. Ghio, G. Alagona, S. Profeta, and P. Weiner. 1984. A new force-field for molecular mechanical simulation of nucleic-acids and proteins. J. Am. Chem. Soc. 106:765-784.
24. 3 receptor ligand binding domain. J. Biol. Chem. 275:5620-5625.
25. 3 receptor F-loop. J. Biol. Chem. 281:16576-16582.
26. Mukhtasimova, N., C. Free, and S. M. Sine. 2005. Initial coupling of binding to gating mediated by conserved residues in the muscle nicotinic receptor. J. Gen. Physiol. 126:23-39.
27. Cashin, A. L., E. J. Petersson, H. A. Lester, and D. A. Dougherty. 2005. Using physical chemistry to differentiate nicotinic from cholinergic agonists at the nicotinic acetylcholine receptor. J. Am. Chem. Soc. 127:350-356.
28. 3 receptor. Mol. Membr. Biol. 23:1-10.
29. Unwin, N., A. Miyazawa, J. Li, and Y. Fujiyoshi. 2002. Activation of the nicotinic acetylcholine receptor involves a switch in conformation of the alpha subunits. J. Mol. Biol. 319:1165-1176.
30. 3A) and nicotinic acetylcholine receptors: the anomalous binding properties of nicotine. Biochemistry. 41:10262-10269.
31. C receptor. Chem. Biol. 12:993-997.
32. Zhong, W. G., J. P. Gallivan, Y. O. Zhang, L. T. Li, H. A. Lester, and D. A. Dougherty. 1998. From ab initio quantum mechanics to molecular neurobiology: A cation-π binding site in the nicotinic receptor. Proc. Natl. Acad. Sci. USA. 95:12088-12093.
33. A receptor binding site residues reveals a novel cation-π interaction between GABA and β2 Tyr97. J. Neurosci. 27:886-892.