Pharmacological characterization of human excitatory amino acid transporters EAAT1, EAAT2 and EAAT3 in a fluorescence-based membrane potential assay

Biochemical Pharmacology

Volumn 67, Issue 11, 2004, Pages 2115-2127

  Jensen, Anders A ^a   Bräuner Osborne, Hans ^a  

^a UNIVERSITY OF COPENHAGEN   (Denmark)

Author keywords

ALS; amyotrophic lateral sclerosis; Asp; aspartate; cis 1 aminocyclobutane 1,3 dicarboxylate; cis ACBD; DHK; dihydrokainate; DMEM; Dulbecco's Modified Eagle Medium; EAAT; excitatory amino acid transporter; FLIPR Membrane Potential; FMP; FU

Indexed keywords

1 AMINOCYCLOBUTANE 1,3 DICARBOXYLATE; 2 AMINO 3 (3 HYDROXY 1,2,5 THIADIAZOL 4 YL)PROPIONIC ACID; 3 HYDROXYASPARTIC ACID; AMINO ACID DERIVATIVE; ASPARTIC ACID; CARBOXYLIC ACID DERIVATIVE; DEXTRO ASPARTIC ACID; DEXTRO GLUTAMIC ACID; DEXTRO THREO BETA BENZYLOXYASPARTATE; DIHYDROKAINIC ACID; EXCITATORY AMINO ACID TRANSPORTER; GLUTAMIC ACID; KAINIC ACID; LEVO PYRROLIDINE 2,4 DICARBOXYLATE; PROPIONIC ACID DERIVATIVE; THREO 3 METHYLGLUTAMATE; UNCLASSIFIED DRUG;

AMINO ACID ANALYSIS; AMINO ACID TRANSPORT; ARTICLE; CONTROLLED STUDY; CORRELATION ANALYSIS; DRUG STRUCTURE; DRUG UPTAKE; ELECTROPHYSIOLOGY; EMBRYO; FLUORESCENCE ANALYSIS; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; MICHAELIS CONSTANT; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN INTERACTION; TRANSPORT KINETICS;

AMINO ACID TRANSPORT SYSTEM X-AG; BIOLOGICAL TRANSPORT; CELLS, CULTURED; ELECTROPHYSIOLOGY; EXCITATORY AMINO ACID TRANSPORTER 1; EXCITATORY AMINO ACID TRANSPORTER 2; EXCITATORY AMINO ACID TRANSPORTER 3; FLUORESCENCE; GLUTAMATE PLASMA MEMBRANE TRANSPORT PROTEINS; HUMANS; MEMBRANE POTENTIALS; SYMPORTERS; TRITIUM;

EID: 2342467905     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bcp.2004.02.013     Document Type: Article

References (45)

1. Wheal HV, Thomson AM. Excitatory amino acids and synaptic transmission. London; 1995.
2. Meldrum B.S. The glutamate synapse as a therapeutical target: perspectives for the future. Prog. Brain Res. 116:1998;441-458
3. Bräuner-Osborne H., Egebjerg J., Nielsen E.Ø., Madsen U., Krogsgaard-Larsen P. Ligands for glutamate receptors: design and therapeutic prospects. J. Med. Chem. 43:2000;2609-2645
4. Jensen AA. Molecular pharmacology of the metabotropic glutamate receptors. In: Schousboe A, Bräuner-Osborne H, editors. Molecular neuropharmacology. Strategies and methods. Totowa (NJ, USA): Humana Press, 2004. p. 47-82.
5. Dingledine R., Borges K., Bowie D., Traynelis S.F. The glutamate receptor ion channels. Pharmacol. Rev. 51:1999;7-61
6. Slotboom D.J., Konings W.N., Lolkema J.S. Structural features of the glutamate transporter family. Microbiol. Mol. Biol. Rev. 63:1999;293-307
7. Seal R.P., Amara S.G. Excitatory amino acid transporters: a family in flux. Annu. Rev. Pharmacol. Toxicol. 39:1999;431-456
8. Clements J.D. Transmitter timecourse in the synaptic cleft: its role in central synaptic function. Trends Neurosci. 19:1996;163-171
9. Wadiche J.I., Amara S.G., Kavanaugh M.P. Ion fluxes associated with excitatory amino acid transport. Neuron. 15:1995;721-728
10. +-dependent glutamate uptake. J. Neurosci. 18:1998;9620-9628
11. Zerangue N., Kavanaugh M.P. Flux coupling in a neuronal glutamate transporter. Nature. 383:1996;634-637
12. Danbolt N.C. Glutamate uptake. Prog. Neurobiol. 65:2001;1-105
13. O'Shea R.D. Roles and regulation of glutamate transporters in the central nervous system. Clin. Exp. Pharmacol. Physiol. 29:2002;1018-1023
14. Campiani G., Fattorusso C., De Angelis M., Catalanotti B., Butini S., Fattorusso R., et al. Neuronal high-affinity sodium-dependent glutamate transporters (EAATs): targets for the development of novel therapeutics against neurodegenerative diseases. Curr. Pharm. Des. 9:2003;599-625
15. Rossi D.J., Oshima T., Attwell D. Glutamate release in severe brain ischaemia is mainly by reversed uptake. Nature. 403:2000;316-321
16. Rothstein J.D., Van Kammen M., Levey A.I., Martin L.J., Kuncl R.W. Selective loss of glial glutamate transporter GLT-1 in amyotrophic lateral sclerosis. Ann. Neurol. 38:1995;73-84
17. Tanaka K., Watase K., Manabe T., Yamada K., Watanabe M., Takahashi K., et al. Epilepsy and exacerbation of brain injury in mice lacking the glutamate transporter GLT-1. Science. 276:1997;1699-1702
18. Rothstein J.D., Dykes-Hoberg M., Pardo C.A., Bristol L.A., Jin L., Kuncl R.W., et al. Knockout of glutamate transporters reveals a major role for astroglial transport in excitotoxicity and clearance of glutamate. Neuron. 16:1996;675-686
19. Johansen T.N., Janin Y.L., Nielsen B., Frydenvang K., Bräuner-Osborne H., Stensbøl T.B., et al. 2-Amino-3-(3-hydroxy-1, 2, 5-thiadiazol-4-yl)propionic acid: resolution, absolute stereochemistry and enantiopharmacology at glutamate receptors. Bioorg. Med. Chem. 10:2002;2259-2266
20. Bräuner-Osborne H., Hermit M.B., Nielsen B., Krogsgaard-Larsen P., Johansen T.N. A new structural class of subtype-selective inhibitor of cloned excitatory amino acid transporter, EAAT2. Eur. J. Pharmacol. 606:2000;41-44
21. 50) of an enzymatic reaction. Biochem. Pharmacol. 22:1973;3099-3108
22. Dunlop J., Lou Z., Zhang Y., McIlvain H.B. Inducible expression of the human excitatory amino acid transporter 2 subtype of L-glutamate transporter. Br. J. Pharmacol. 128:1999;1485-1490
23. Shimamoto K., Shigeri Y., Yasuda-Kamatani Y., Lebrun B., Yumoto N., Nakajima T. Syntheses of optically pure β-hydroxyaspartate derivatives as glutamate transporter blockers. Bioorg. Med. Chem. Lett. 10:2000;2407-2410
24. Arriza J.L., Fairman W.A., Wadiche J.I., Murdoch G.H., Kavanaugh M.P., Amara S.G. Functional comparison of three glutamate transporter subtypes cloned from human motor cortex. J. Neurosci. 14:1994;5559-5568
25. Kanai Y., Hediger M.A. Primary structure and functional characterization of a high-affinity glutamate transporter. Nature. 360:1992;467-471
26. Vandenberg R.J., Mitrovic A.D., Chebib M., Balcar V.J., Johnston G.A.R. Contrasting modes of action of methylglutamate derivatives on the excitatory amino acid transporters EAAT1 and EAAT2. Mol. Pharmacol. 51:1997;809-815
27. Shimamoto K., Lebrun B., Yasuda-Kamatani Y., Sakaitani M., Shigeri Y., Yumoto N., et al. DL-threo-β-Benzyloxyaspartate, a potent blocker of excitatory amino acid transporters. Mol. Pharmacol. 53:1998;195-201
28. - neurotransmitter transporters. J. Neurochem. 71:1998;1785-1803
29. 2+ signalling exemplified by the NK1 receptor. J. Recept. Signal. Transduct. Res. 22:2002;241-252
30. Whiteaker K.L., Gopalakrishnan S.M., Groebe D., Shieh C.C., Warrior U., Burns D.J., et al. Validation of FLIPR membrane potential dye for high throughput screening of potassium channel modulators. J. Biomol. Screen. 6:2001;305-312
31. Fitch R.W., Xiao Y., Kellar K.J., Daly J.W. Membrane potential fluorescence: a rapid and highly sensitive assay for nicotinic receptor channel function. Proc. Natl. Acad. Sci. U.S.A. 100:2003;4909-4914
32. Jensen A.A., Mikkelsen I., Frølund B., Bräuner-Osborne H., Falch E., Krogsgaard-Larsen P. Carbamoylcholine homologs: novel and potent agonists at neuronal nicotinic acetylcholine receptors. Mol. Pharmacol. 64:2003;865-875
33. A receptors characterized by fluorescence resonance energy transfer-derived measurements of membrane potential. J. Biol. Chem. 276:2001;38934-38939
34. Jensen AA, Kristiansen U. Functional characterisation of the human α1 glycine receptor in a fluorescence-based membrane-potential assay. Biochem Pharmacol (in press).
35. Hallen S., Fryklund J., Sjostrom J.E., Bonge H. Cytostar-T scintillating microplate assay for measurement of sodium-dependent bile acid uptake in transfected HEK-293 cells. Anal. Biochem. 282:2000;94-101
36. --dependent neurotransmitter transporter activity. Anal. Biochem. 321:2003;31-37
37. Graves R., Davies R., Brophy G., O'Beirne G., Cook N. Noninvasive, real-time method for the examination of thymidine uptake events - application of the method to V-79 cell synchrony studies. Anal. Biochem. 248:1997;251-257
38. Esslinger C.S., Koch H.P., Kavanaugh M.P., Philips D.P., Chamberlin A.R., Thompson C.M., et al. Structural determinants of substrates and inhibitors: probing glutamate transporters with 2, 4-methanopyrrolidine-2, 4-dicarboxylate. Bioorg. Med. Chem. Lett. 8:1998;3101-3106
39. Koch H.P., Kavanaugh M.P., Esslinger C.S., Zerangue N., Humphrey J.M., Amara S.G., et al. Differentiation of substrate and nonsubstrate inhibitors of the high-affinity, sodium-dependent glutamate transporters. Mol. Pharmacol. 56:1999;1095-1104
40. Lebrun B., Sakaitani M., Shimamoto K., Yasuda-Kamatani Y., Nakajima T. New β-hydroxyaspartate derivatives are competitive blockers for the bovine glutamate/aspartate transporter. J. Biol. Chem. 272:1997;20336-20339
41. Chamberlin AR, Koch HP, Bridges RJ. Design and synthesis of conformationally constrained inhibitors of high-affinity, sodium-dependent glutamate transporters. In: Amara SG, editor. Methods enzymol, vol. 296. San Diego: Academic Press; 1998. p. 175-89.
42. Mitrovic A.D., Amara S.G., Johnston G.A., Vandenberg R.J. Identification of functional domains of the human glutamate transporters EAAT1 and EAAT2. J. Biol. Chem. 273:1998;14698-14706
43. Eliasof S., McIlvain H.B., Petroski R.E., Foster A.C., Dunlop J. Pharmacological characterization of threo-3-methylglutamic acid with excitatory amino acid transporters in native and recombinant systems. J. Neurochem. 77:2001;550-557
44. Kenakin T. Pharmacological analysis of drug-receptor interaction. Philadelphia, NY: Lippencott-Raven; 1997.
45. Vandenberg RJ, Ryan RM. Allosteric modulation of glutamate transporters. In: Schousboe A, Bräuner-Osborne H, editors. Molecular neuropharmacology. Strategies and methods. Totowa (NJ, USA): Humana Press, 2004. p. 161-74.