Histaminergic pharmacology of homo-oligomeric β3 γ-aminobutyric acid type a receptors characterized by surface plasmon resonance biosensor technology

Biochemical Pharmacology

Volumn 84, Issue 3, 2012, Pages 341-351

  Seeger, Christian ^a,b   Christopeit, Tony ^b   Fuchs, Karoline ^c   Grote, Katharina ^c   Sieghart, Werner ^c   Danielson, U Helena ^a,b  

^a Beactica   (Sweden)

^b UPPSALA UNIVERSITY   (Sweden)

^c Medical University of Vienna   (Austria)

Author keywords

Aminobutyric acid type A receptor; Competition analysis; Histamine; Ligand gated ion channel; Surface plasmon resonance

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR BETA3; AMTHAMINE; ASTEMIZOLE; BACLOFEN; BURIMAMIDE; CETIRIZINE; CIMETIDINE; CLEMASTINE; CLOBENPROPIT; DIMAPRIT; DIPHENHYDRAMINE; DOXEPIN; FAMOTIDINE; FEXOFENADINE; GABAERGIC RECEPTOR AFFECTING AGENT; HISTAMINERGIC RECEPTOR AFFECTING AGENT; IMETIT; IODOPROXYFAN; KETOTIFEN; LORATADINE; MEPYRAMINE; MIRTAZAPINE; RANITIDINE; TERFENADINE; THIOPERAMIDE; TIOTIDINE; TRIPROLIDINE; UNINDEXED DRUG; ZOLANTIDINE; ZOTEPINE;

ARTICLE; BIOSENSOR; DRUG BINDING SITE; DRUG RECEPTOR BINDING; DRUG STRUCTURE; HUMAN; PRIORITY JOURNAL; PROTEIN INTERACTION; RECEPTOR AFFINITY; STEADY STATE; SURFACE PLASMON RESONANCE;

ANIMALS; BIOSENSING TECHNIQUES; CELL LINE; HISTAMINE AGENTS; HUMANS; INSECTS; PROTEIN BINDING; RATS; RECEPTORS, GABA-A; SURFACE PLASMON RESONANCE;

EID: 84861974582     PISSN: 00062952     EISSN: 18732968     Source Type: Journal    
DOI: 10.1016/j.bcp.2012.04.008     Document Type: Article

References (40)

1. Olsen RW, Sieghart W. International Union of Pharmacology. LXX. Subtypes of g-aminobutyric acid A receptors: classification on the basis of subunit composition, pharmacology, and function. Update. Pharmacol Rev 2008;60:243-60.
2. Rudolph U, Knoflach F. Beyond classical benzodiazepines: novel therapeuticpotential of GABAA receptor subtypes. Nat Rev Drug Discov 2011;10:685-97.
3. D'Hulst C, Kooy RF. The GABAA receptor: a novel target for treatment of fragile X? Trends Neurosci 2007;30:425-31. (Pubitemid 47088715)
4. Miller PS, Smart TG. Binding, activation and modulation of Cys-loop receptors. Trends Pharmacol Sci 2010;31:161-74.
5. Simon J, Wakimoto H, Fujita N, Lalande M, Barnard EA. Analysis of the set of GABAA receptor genes in the human genome. J Biol Chem 2004;279:41422-35. (Pubitemid 39313583)
6. Barnard E, Skolnick P, Olsen R, Mohler H, Sieghart W, Biggio G, et al. International Union of Pharmacology. XV. Subtypes of g-aminobutyric acid A receptors: classification on the basis of subunit structure and receptor function. Pharmacol Rev 1998;50:291-314.
7. Smith GB, Olsen RW. Functional domains of GABAA receptors. Trends Pharmacol Sci 1995;16:162-8.
8. Richter L, de Graaf C, Sieghart W, Varagic Z, Mörzinger M, de Esch IJP, Ecker GF, Ernst M. Diazepam-bound GABAA receptor models identify new benzodiazepine binding site ligands. Nature Chem Biol 2012;8:455-64.
9. Sieghart W, Sperk G. Subunit composition, distribution and function of GABAA receptor subtypes. Curr Top Med Chem 2002;2:795-816.
10. Slany A, Zezula J, Tretter V, Sieghart W. Rat beta 3 subunits expressed in human embryonic kidney 293 cells form high affinity [35S] t-butylbicyclophosphorothionate binding sites modulated by several allosteric ligands of gammaaminobutyric acid type A receptors. Mol Pharmacol 1995;48:385-91.
11. Wooltorton JRA, Moss SJ, Smart TG. Pharmacological and physiological characterization of murine homomeric beta3 GABAA receptors. Eur J Neurosci 1997;9:2225-35.
12. Saras A, Gisselmann G, Vogt-Eisele AK, Erlkamp KS, Kletke O, Pusch H, et al. Histamine action on vertebrate GABAA receptors: direct channel gating and potentiation of GABA responses. J Biol Chem 2008;283:10470-75.
13. Bianchi MT, Clark AG, Fisher JL. The wake-promoting transmitter histamine preferentially enhances alpha-4 subunit-containing GABAA receptors. Neuropharmacology 2011;61:747-52.
14. Cannon KE, Fleck MW, Hough LB. Effects of cimetidine-like drugs on recombinant GABAA receptors. Life Sci 2004;75:2551-8. (Pubitemid 39195261)
15. Lakoski JM, Aghajanian GK, Gallager DW. Interaction of histamine H2-receptor antagonists with GABA and benzodiazepine binding sites in the CNS. Eur J Pharmacol 1983;88:241-5. (Pubitemid 13109617)
16. Fleck MW, Thomson JL, Hough LB. Histamine-gated ion channels in mammals?Biochem Pharmacol 2012;83:1127-35.
17. Brejc K, van Dijk WJ, Klaassen RV, Schuurmans M, van der Oost J, Smit AB, et al.Crystal structure of an ACh-binding protein reveals the ligand-binding domainof nicotinic receptors. Nature 2001;411:269-76. (Pubitemid 32467026)
18. Geitmann M, Retra K, de Kloe GE, Homan EJ, Smit AB, de Esch IJP, et al. Interaction kinetic and structural dynamic analysis of ligand binding to acetylcholine-binding protein. Biochemistry 2010;49:8143-54.
19. Kang SU, Fuchs K, Sieghart W, Lubec G. Gel-based mass spectrometric analysis of recombinant GABAA receptor subunits representing strongly hydrophobic transmembrane proteins. J Proteome Res 2008;7:3498-506.
20. Heckman KL, Pease LR. Gene splicing and mutagenesis by PCR-driven overlap extension. Nat Protoc 2007;2:924-32. (Pubitemid 46758810)
21. Yagle MA, Martin MW, de Fiebre CM, de Fiebre NEC, Drewe JA, Dillon GH. [3H] Ethynylbicycloorthobenzoate ([3H]EBOB) binding in recombinant GABAA receptors. Neurotoxicology 2003;24:817-24. (Pubitemid 37486257)
22. Johnsson B, Löfås S, Lindquist G. Immobilization of proteins to a carboxymethyldextran- modified gold surface for biospecific interaction analysis in surface plasmon resonance sensors. Anal Biochem 1991;198:268-77.
23. Jönsson U, Fägerstam L, Ivarsson B, Johnsson B, Karlsson R, Lundh K, et al. Realtime biospecific interaction analysis using surface plasmon resonance and a sensor chip technology. Biotechniques 1991;11:620-7.
24. Lim HD, Van Rijn RM, Ling P, Bakker RA, Thurmond RL, Leurs R. Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. J Pharmacol Exp Ther 2005;314:1310-21. (Pubitemid 41205997)
25. Liu H, Altenbach RJ, Carr TL, Chandran P, Hsieh GC, Lewis LGR, et al. cis-4- (Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro [2,3-h] quinazolin- 2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia. J Med Chem 2008;51:7094-8.
26. Lim HD, Smits RA, Bakker RA, van Dam CME, de Esch IJP, Leurs R. Discovery of S-(2-guanidylethyl)-isothiourea (VUF 8430) as a potent nonimidazole histamine H4 receptor agonist. J Med Chem 2006;49:6650-1. (Pubitemid 44749731)
27. Cowart MD, Altenbach RJ, Liu H, Hsieh GC, Drizin I, Milicic I, et al. Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models. J Med Chem 2008;51:6547-57.
28. Karlsson OP, Löfås S. Flow-mediated on-surface reconstitution of G-protein coupled receptors for applications in surface plasmon resonance biosensors. Anal Biochem 2002;300:132-8. (Pubitemid 34097438)
29. Christopeit T, Stenberg G, Gossas T, Nyström S, Baraznenok V, Lindström E, et al. A surface plasmon resonance based biosensor with full-length BACE1 in a reconstituted membrane. Anal Biochem 2011;414:14-22.
30. Navratilova I, Sodroski J, Myszka DG. Solubilization, stabilization, and purification of chemokine receptors using biosensor technology. Anal Biochem2005;339:271-81. (Pubitemid 40395285)
31. Rich RL, Errey J, Marshall F, Myszka DG. Biacore analysis with stabilized G-protein- coupled receptors. Anal Biochem 2011;409:267-72.
32. Li GD, Chiara DC, Sawyer GW, Husain SS, Olsen RW, Cohen JB. Identification of a GABAA receptor anesthetic binding site at subunit interfaces by photolabeling with an etomidate analog. J Neurosci 2006;26:11599-605. (Pubitemid 44772131)
33. Dostalova Z, Liu A, Zhou X, Farmer SL, Krenzel ES, Arevalo E, et al. High-level expression and purification of Cys-loop ligand-gated ion channels in a tetracycline- inducible stable mammalian cell line: GABAA and serotonin receptors. Protein Sci 2010;19:1728-38.
34. Schubring S, Fleischer W, Lin J, Haas H, Sergeeva O. The bile steroid chenodeoxycholate is a potent antagonist at NMDA and GABAA receptors. Neurosci Lett 2012;506:322-6.
35. Stephenson FA, Olsen RW. Solubilization by CHAPS detergent of barbiturate-enhanced benzodiazepine-GABA receptor complex. J Neurochem 1982;39: 1579-86. (Pubitemid 13184133)
36. De Jong LAA, Uges DRA, Franke JP, Bischoff R. Receptor-ligand binding assays: technologies and applications. J Chromatogr B 2005;829:1-25. (Pubitemid 41773460)
37. Neher E, Sakmann B. Single-channel currents recorded from membrane of denervated frog muscle fibres. Nature 1976;260:799-802.
38. Geitmann M, Elinder M, Seeger C, Brandt P, de Esch IJP, Danielson UH. Identification of a novel scaffold for allosteric inhibition of wild type and drug resistant HIV-1 reverse transcriptase by fragment library screening. JMed Chem 2011;54:699-708.
39. Shuker SB, Hajduk PJ, Meadows RP, Fesik SW. Discovering high-affinity ligands for proteins: SAR by NMR. Science 1996;274:1531-4. (Pubitemid 26403929)
40. Nury H, Van Renterghem C, Weng Y, Tran A, Baaden M, Dufresne V, et al. X-ray structures of general anaesthetics bound to a pentameric ligand-gated ion channel. Nature 2011;469:428-31.