Acknowledgement

Tranquilizer Free

Panic Attacks Treatment

Get Instant Access

We thank Monika Simon for her assistance with editing and proofreading.

278 I 7 MS Binding Assays - An Alternative to Radioligand Binding References

1 Williams, M., Mehlin, C., Triggle, D. J.: Receptor targets in drug discovery and development, in Burger's Medicinal Chemistry and Drug Discovery, Vol. ii: Drug Development, ed. Abraham, D. J., John Wiley & Sons, New York, 2003, pp 319-355.

2 Jenkinson, D. H.: Classical approaches to the study of drug-receptors interactions, in Textbook of Receptor Pharmacology, ed. Foreman, J.C., Johansen, T., CRC Press, Boca Raton, 2003, pp 3-78.

3 Hofliger, M. M., Beck-Sickinger, A. G.: Receptor-ligand interaction, in Protein-Ligand Interactions. From Molecular Recognition to Drug Design, ed. Böhm, H.-J., Schneider, G., Wiley-VCH, Weinheim, 2003, pp 107-135.

4 Hulme, E. C.: Preface, in Receptor-Ligand Interactions. A Practical Approach, ed. Hulme, E. C., IRL Press, Oxford, 1992.

5 Wang, J.-X., Yamamura, H. I., Wang, W., Roeske, W. R.: The use of the filtration technique in in vitro radioligand binding assays for membrane-bound and solubilized receptors, in Receptor-Ligand Interactions. A Practical Approach, ed. Hulme, E. C., IRL Press, Oxford, 1992, pp 213-234.

6 Sweetnam, P. M., Price, C. H., Ferkany, J. W.: Mass ligand screening as a tool for drug discovery and development, in Burger's Medicinal Chemistry and Drug Discovery. vol. i: Principles and Practice, ed. Wolff,

M. E., John Wiley & Sons, New York, 1995, pp 697-731.

7 Haylett, D. G.: Direct measurement of drug binding to receptors, in Textbook of Receptor Pharmacology, ed. Foreman, J.C., Johansen, T., CRC Press, Boca Raton, 2003, pp 153-180.

8 Vogel, H. G.: Introduction. Strategies in drug discovery and evaluation, in Drug Discovery and Evaluation. Pharmacological Assays, ed. Vogel,

9 Major, J. S.: Challenges of high throughput screening against cell surface receptors. J. Recept. Signal Transduction Res. 1994, 15, 595-607.

10 Pope, A.J., Haupts, U.M., Moore, K.J.: Homogenous fluorescence readouts for miniaturized high-throughput screening: theory and practice. Drug Discov. Today 1999, 4, 350-362.

11 Hovius, R., Vallotton, P., Wohland, T., Vogel, H.: Fluorescence techniques: shedding light on ligand-receptor interactions. Trends Pharmacol. Sci. 2000, 21, 266-273.

12 Hemmlia, I., Mukkala, V.-M.: Timeresolution in fluorometry technologies, labels, and applications in bioanalytical assays. Crit. Rev. Clin. Lab. Sci. 2001, 38, 441-519.

13 Handl, H. L., Gillies, R. J.: Lanthanide-based luminescent assays for ligand-receptor interactions. Life Sci. 2005, 77, 361-671.

14 Tota, M.R., Daniel, S., Serotina, A., Mazina, K.E., Fong, M.F., Longmore, J., Strader, C.D.: Characterization of a fluorescent substance P analog. Biochemistry 1994, 33, 13079-13086.

15 Turcatti, G., Vogel, H., Chollet, A.: Probing the binding domain of the NK2 receptor with fluorescent ligands: evidence that heptapeptide agonists and antagonists bind differently. Biochemistry 1995, 34, 3972-3980.

16 Hulme, E. C., Birdsall, N. J. M.: Strategy and tactics in receptor-binding studies, in Receptor-Ligand Interactions. A Practical Approach, ed. Hulme, E. C., IRL Press, Oxford, 1992, pp 63-176.

17 Bennett, J. P. Jr, Yamamura, H. I.: Neurotransmitter, hormone, or drug receptor binding methods, in Neurotransmitter Receptor Binding, ed. Yamamura, H. I., Enna, S. J., Kuhar, M. J., Raven Press, New York, 1985, pp 61-89.

18 Williams, M., Sills, M. A.: Quantitative analysis of ligand-receptor interaction, in Comprehensive Medicinal Chemistry, vol. iii:

Membranes & Receptors, ed. Emmett, J. C., Pergamon Press, Oxford, 1990, pp 45-80.

19 Titeler, M.: Binding theory and methodology, in Receptor Pharmacology and Function, ed. Williams, M., Glennon, R. A., Timmermans, P. B. M. W. M., Marcel Dekker, New York, 1989, pp 17-45.

20 Rahman, A., Choudhary, M. I., Thomsen, W. J.: Radioligand binding assays, in Bioassay Techniques for Drug Development, ed. Rahman, A., Choudhary, M. I., Thomsen, W. J., Harwood Academic Publishers, Amsterdam, 2001, pp 179-218.

21 Bylund, D.B., Deupree, J. D., Toews, M.L.: Radioligand-binding methods for membrane preparations and intact cells, in Methods in Molecular Biology, vol. 259: Receptor Signal Transduction Protocols, ed. Willars, G. B., Challiss, R.A.J., Humana Press, Totowa, 2004, pp 1-28.

22 Cheng, Y.-C., Prusoff, W.H.: Relationships between the inhibition constant (Ki) and the concentration of inhibitor which causes 50 per cent inhibition (IC50) of an enzymatic reaction. Biochem. Pharmacol. 1973, 22, 3099-3108.

23 Hulme, E. C., Buckley, N. J.: Receptor preparations for binding studies, in Receptor-Ligand Interactions. A Practical Approach, ed. Hulme,

S. A.: Cell-free ligand binding assays for nuclear receptors. Methods Enzymol. 2003, 364, 53-71.

C. W.: Microplate gel-filtration method for radioligand-binding assays. Anal. Biochem. 2002, 308, 127-133.

D., Melch, M., McConkey, M., Bergeron, J., Wong, S. K.-F.: Fully automated radioligand binding filtration assay for membrane-bound receptors. BioTechniques 2002, 33, 932-937.

27 Bosworth, N., Towers, P.: Scintillation proximity assay. Nature 1989, 341, 167-168.

28 Minor, L.K.: Assays for membrane tyrosine kinase receptors: methods for high-throughput screening and utility for diagnostics. Expert Rev. Mol. Diagn. 2005, 5, 561-571.

29 Brown, B.A., Cain, M., Broadbent, J., Tompkins, S., Henrich, G., Joseph, R., Casto, S., Harney, H., Greene, R., Delmondo, R., Ng, S.: in High Throughput Screening, ed. Devlin, J.P., Dekker, New York, 1997, pp 317-328.

30 Wu, S., Liu, B.: Application of scintillation proximity assay in drug discovery. Biodrugs 2005, 19, 383-392.

31 Van der Hee, R. M., Deurholt, T., Gerhardt, C. C., de Groene, E.: Comparison of 3 AT1 receptor binding assays: filtration assay, ScreenreadyTM target and WGA Flashplate®. J. Biomol. Screening 2005, 10, 118-126.

32 Walters, W. A., Namchuk, M.: Designing screens: how to make your hits a hit. Nat. Rev. Drug Discov. 2003, 2, 259-266.

33 Houston, J. G., Banks, M. N.: High-throughput screening for lead discovery, in Burger's Medicinal Chemistry and Drug Discovery, vol. ii: Drug Development, ed. Abraham, D. J., John Wiley & Sons, New York, 2003, pp 37-69.

34 Griersiefen, H., Hilgenfeld, R., Hillisch, A.: modern methods of drug discovery: an introduction, in Modern Methods of Drug Discovery, ed. Hillisch, A., Hilgenfeld, R., Birkhauser, Basel, 2003, pp 1-18.

35 Noël, F., Mendonca-Silva, D. L., Quintas, L. E. M.: Radioligand binding assays in the drug discovery process: potential pitfalls of high throughput screenings. Arzneim. Forsch./Drug Res. 2001, 51, 169-173.

36 Rovati, G. E.: Ligand-binding studies: old beliefs and new strategies. Trends Pharmacol. Sci. 1998, 19, 365-369.

37 Takeuchi, T., Rechnitz, G.A.: Nonisotopic receptor assay for benzodiazepine receptors for utilizing a fluorophore labelled ligand. Anal. Biochem. 1991, 194, 250-255.

G. A.: Development of a nonisotopic acetylcholine receptor assay for the investigation of cholinergic ligands. Anal. Chim. Acta 1992, 267, 55-62.

39 Janssen, M.J., Ensing, K., de Zeeuw, R.A.: A fluorescent receptor assay for benzodiazepines using coumarin-labeled desethylflumazenil as ligand. Anal. Chem. 2001, 73, 3168-3173.

40 Pedersen, S. E., Lurtz, M. M., Papineni, R. V. L.: Ligand-binding methods for analysis of ion channel structure and function. Methods Enzymol. 1999, 294, 117-135.

41 McGrath, J. C., Arrias, S., Daly, C. J.: Fluorescent ligands for the study of receptors. Trends Pharmacol. Sci. 1996, 17, 393-399.

42 Takeuchi, T., Nishikawa, T., Matsukawa, R., Matsui, J.: Nonisotopic receptor assay for benzodiazepine drugs using time-resolved fluorometry. Anal. Chem. 1995, 67, 2655-2658.

43 Inglese, J., Samama, P., Patel, S., Burbaum, J., Stroke, I. L., Appell, K. C.: Chemokine receptor-ligand interactions measured using time-resolved fluorescence. Biochemistry 1998, 37, 2372-2377.

44 Gao, X., Hsu, C.-K., Heinz, L. J., Morin, J., Shi, Y., Shukla, N. K., Smiley, D. L., Xu, J., Zhong, B., Slieker, L. J.: Europium-labeled melanin-concentrating hormone analogues: ligands for measuring binding to melanin-concentrating hormone receptors 1 and 2. Anal. Biochem. 2004, 328, 187-195.

45 Parker, G. J., Law, T. L., Lenoch, F. J., Bolger, R. E.: Development of high throughput screening assays using fluoresence polarization: nuclear receptor-ligand-binding and kinase/ phosphatase assays. J. Biomol. Screen. 2000, 5, 77-88.

46 Pramanik, A.: Ligand-receptor interactions in live cells by fluorescence correlation spectroscopy. Curr. Pharm. Biotechnol. 2004, 5, 205-212.

47 Price, G.W., Riley, G.J., Middlemiss, D.N.: Biological evaluation of novel compounds, in Medicinal Chemistry Principles and Practice, ed. King, F. D., Royal Society of Chemistry, Cambridge, 2002, pp 91-117.

48 Lundqvist, T.: The devil is still in the details - driving early drug discovery forward with biophysical experimental methods. Curr. Opin. Drug Discov. Dev. 2005, 8, 513-519.

49 Cooper, M.A.: Advances in membrane receptor screening and analysis.

50 Siegel, M. M.: Mass-spectromety-based drug screening assays for early phases in drug discovery, in Integrated Strategies for Drug Discovery Using Mass Spectrometry, ed. Lee, M. S., John Wiley & Sons, New York, 2005, pp 27-70.

51 Daniel, J.M., Friess, S.D., Rajagopalan, S., Wendt, S., Zenobi, R.: Quantitative determination of noncovalent binding interactions using soft ionisation mass spectrometry. Int. J. Mass Spectrom. 2002, 216, 1-27.

52 Van Breemen, R. B.: Mass spectrometry and drug discovery, in Burger's Medicinal Chemistry and Drug Discovery, vol. i: Drug Discovery, ed. Abraham, D. J., John Wiley & Sons, New York, 2003, pp 583-610.

53 Ganem, B., Li, Y.-T., Henion, J.: Detection of noncovalent receptor-ligand complexes by mass spectrometry. J. Am. Chem. Soc. 1991, 113, 6294-6296.

54 Lim, H.-K., Hsieh, Y.L., Ganem, B., Henion, J.: Recognition of cell-wall peptide ligands by vancomycin group antibiotics: studies using ion spray mass spectrometry. J. Mass Spectrom. 1995, 30, 708-714.

55 Schermann, S., Simmons, D.A., Konermann, L.: Mass spectrometry-based approaches to protein-ligand Interactions. Expert Rev. Proteomics 2005, 2, 475-485.

56 Geoghegan, K.F., Kelly, M.A.: Biochemical applications of mass spectrometry in pharmaceutical drug discovery. Mass Spectrom. Rev. 2005, 24, 347-366.

57 Muckenschnabel, I., Falchetto, R., Mayr, L.M., Filipuzzi, I.: SpeedScreen: label-free liquid chromatography-mass spectrometry-based high-throughput screening for the discovery of orphan protein ligands. Anal. Biochem. 2004, 324, 241-249.

58 Missale, C., Nash, R., Robinson, S.W., Jaber, M., Caron, M.D.: Dopamine receptors: from structure to function. Physiol. Rev. 1998, 78, 189-225.

59 Bleicher, K. H., Böhm, H.-J., Müller, K., Alanine, A. I.: Hit and lead generation: beyond high throughput screening. Nat. Rev. 2003, 2, 369-378.

60 Billard, W., Ruperto, V., Crosby, G., Iorio, L.C., Barnett, A.: Characterization of the binding of 3H-SCH 23390. A selective D-1 receptor antagonist ligand, in rat striatum. Life Sci. 1984, 35, 18851893.

61 Hofner, G., Wanner, K.T.: Competitive binding assays simply done with a native marker and mass spectrometric quantification. Angew. Chem. Int. Ed. 2003, 42, 5235-5237; Angew. Chem. 2003, 115, 5393-5395.

62 Niessen, K.V., Hofner, G., Wanner, K.T.: Competitve MS binding assays for dopamine D2 receptors employing spiperone as anative marker, ChemBioChem 2005, 6, 1769-1775.

63 Rees, C., Hunter, J. C.: Opioid receptors, in Comprehensive Medicinal Chemistry, vol. iii: Membranes & Receptors, ed. Emmett, J. C., Pergamon Press, Oxford, 1990, pp 45-80.

64 Aldrich, J.V., Virgil-Cruz, S.C.: Narcotic analgetics, in Burger's Medicinal Chemistry and Drug Discovery, vol. vi: Nervous System Agents, ed. Abraham, D. J., John Wiley & Sons, New York, 2003, pp 329-481.

65 Wanner, K., Hofner, G., Bertling, W.: Method for determining the binding behaviour of ligands which specifically bind to target molecules. US patent US 20040232077 A1.

66 Raynor, K., Kong, H., Mestek, A., Bye, L.S., Tian, M., Liu, J., Yu, L., Reisine, T.: Characterization of the cloned human mu opioid receptor. J. Pharmacol. Exp. Ther. 1995, 272, 423-428.

67 Goldstein, A., Barrett, R. W.: Ligand dissociation constants from competition binding assays: errors associated with ligand depletion. Mol. Pharmacol. 1987, 13, 603-609.

68 Bylund, D. B., Murrin, L. C.: Radioligand saturation binding experiments over large concentration ranges. Life Sci. 2000, 67, 287-2911.

69 Tate, C. G., Grisshammer, R.: Heterologous expression of G proteincoupled receptors. Trends Biotechnol. 1996, 14, 426-430.

70 Turner, G. J., Reusch, R., Winter-Vann, A. M., Martinez, L., Betlach, M. C.: Heterologous gene expression in a membrane-protein-specific system. Protein Express. Purif. 1999, 17, 312-323.

71 Kalipatnapu, S., Pucadyil, T. J., Harikumar, K. G., Chattopadhyay, A.: Ligand binding characteristics of the human serotonin1A receptor hetero-logously expressed in CHO cells. Biosci. Receptors 2004, 24, 101-115.

72 Janssen, M.J., Ensing, K., de Zeeuw, R.A.: Improved benzodiazepine radioreceptor assay using the MultiScreen® assay system.

73 Zhang, H., Pan, Y.: Affinity ultrafiltration of DNA topoisomerases-targeted compounds determined with HPLC/ESI-MS for drug candidate screening. J. Zhejiang Univ. Sci. 2004, 5, 900-905.

74 Sun, Y., Gu, C., Liu, X., Liang, W., Yao, P., Bolton, J. L., van Breemen, R. B.: Ultrafiltration tandem mass spectrometry of estrogens for characterization of structure and affinity for human estrogen receptors. J. Am. Soc. Mass Spectrom. 2005, 16, 271-279.

75 Liu, J., Carr, S., Rinaldi, K., Chandler, W.: Screening estrogenic oxidized byproducts by combining ER binding and ultrafiltration. Environ. Toxicol. Pharmacol. 2005, 20, 269-278.

76 Biddlecombe, R. A., Pleasance, S.: Automated protein precipitation by filtration in the 96-well format.

77 Janssen, M.J., Ensing, K., de Zeeuw, R.A.: Improved benzodiazepine radioreceptor assay using the MultiScreen® assay system. J. Pharm. Biomed. Anal. 1999, 20, 753-761.

78 Hopfgartner, G., Bourgogne, E.: Quantitative high-throughput analysis of drugs in biological matrices by mass spectrometry. Mass Spectrom. Rev. 2003, 22, 195-214.

79 Mei, H., Hsieh, Y., Nardo, C., Xu, X., Wang, S., Ng, K., Korfmacher, W. A.: Investigation of matrix effects in bioanalytical high-performance liquid chromatography/tandem mass spectrometric assays: application to drug discovery. Rapid Commun. Mass Spectrom. 2003, 17, 97-103.

80 Zepperitz, C., Hofner, G., Wanner, K. T.: MS-binding assays: kinetic, saturation, and competitive experiments based on quantitation of bound marker as exemplified by the GABA transporter mGAT1. ChemMedChem 2006, 1, 208-217.

81 Beleboni, R. O., Gomes Carolino,

R. O., Baldocchi Pizzo, A., Castellan-Baldan, L., Coutinho-Netto, J., Ferreira dos Santos, W., Cysne Coimbra, N.: Pharmacological and biochemical aspects of GABAergic neurotransmission: pathological and neuropsychobiological relationships. Cell. Mol. Neurobiol. 2004, 24, 707-728.

82 Iversen, L.: Neurotransmitter transporters: fruitful targets for CNS drug discovery. Mol. Psychiatry 2000, 5, 357-362.

83 Dalby, N. O.: Inhibition of gamma-aminobutyric acid uptake: anatomy, physiology and effects against epileptic seizures. Eur. J. Pharmacol. 2003, 479, 127-137.

84 Chen, N.-H., Reith, M. E. A., Quick, M. W.: Synaptic uptake and beyond: the sodium- and chloride-dependent neurotransmitter transporter family

SLC6. Pflugers Arch Eur. J. Physiol. 2004, 447, 519-531.

85 Conti, F., Minelliy, A., Melone, M.: GABA transporters in the mammalian cerebral cortex: localization, development and pathological implications. Brain Res. Rev. 2004, 45, 196-212.

86 Czuczwar, S. J., Patsalos, P. N.: The new generation of GABA enhancers potential in the treatment of epilepsy. CNS Drugs 2001, 15, 339-350.

87 Laughlin, T. M., Tram, K. V., Wilcox, G. L., Birnbaum, A. K.: Comparison of antiepileptic drugs tiagabine, lamotrigine, and gabapentin in mouse models of acute, prolonged, and chronic nociception. J. Pharmacol. Exp. Ther. 2002, 302, 1168-1175.

88 Genton, P., Guerrini, R., Perucca, E.: Tiagabine in clinical practice. Epilepsia 2001, 42, 42-45.

89 Iversen, L. L., Neal, M. J.: The uptake of [3 H]GABA by slices of rat cerebral cortex. J. Neurochem. 1968, 15, 11411149.

90 Iversen, L. L., Kelly, J. S.: Uptake and metabolism of g aminobutyric acid by neurones and glial cells. Biochem. Pharmacol. 1975, 24, 933-938.

91 Sutch, R. J., Davies, C. C., Bowery, N. G.: GABA release and uptake measured in crude synaptosomes from genetic absence epilepsy rats from Strasbourg (GAERS). Neurochem. Int. 1999, 34, 415-425.

92 Clausen, R. P., Moltzen, E. K., Perregaard, J., Lenz, S. M., Sanchez, C., Falch, E., Fr0lund, B., Bolvig, T., Sarup, A., Larsson, O. M., Schousboe, A., Krogsgaard-Larsen, P.: Selective inhibitors of GABA uptake: synthesis and molecular pharmacology of 4-N-methylamino-4,5,6,7-tetrahydrobenzo[ D]isoxazol-3-ol analogues. Bioorg. Med. Chem. 2005, 13, 895-908.

93 Bylund, D. B., Toews, M. L.: Radioligand binding methods: practical guide and tips. Am. J. Physiol. Lung Cell. Mol. Physiol. 1993, 265, L421-L429.

94 Bylund, D. B., Deupree, J. D., Toews, M. L.: Radioligand-binding methods for membrane preparations and intact cells. Methods Mol. Biol. 259, 1-28.

95 Braestrup, C., Nielsen, E. B., Sonnewald, U., Knutsen, J. S., Andersen, K. E., Jansen, J. A., Frederiksen, K., Andersen, P. H., Mortnesen, A., Suzdak, P.D.: (R)-N-[4,4-bis(3-methyl-2-thienyl)but-3-en-1-yl]nipecotic acid binds with high affinity to the brain g-aminobutyric acid uptake carrier. J. Neurochem. 1990, 54, 639-647.

96 Suzdak, P. D., Frederiksen, K., Andersen, K. E., Sorensen, P. O., Knutsen, L. J. S., Nielsen, E. B.: NNC-711, a novel potent and selective g-aminobutyric acid uptake inhibitor: pharmacological characterization. Eur. J. Pharmacol. 1992, 223, 189-198.

97 Suzdak, P. D., Foged, C., Andersen, K. E.: Quantitative autoradiographic characterization of the binding of [3H]tiagabine (NNC 05-328) to the GABA uptake carrier. Brain Res. 1994, 647, 231-241.

98 Soudijn, W., van Wijngaarden, I.: The GABA transporter and its inhibitors. Curr. Med. Chem. 2000, 7, 1063-1079.

99 Kragler, A., Hofner, G., Wanner, K. T.: Novel parent structures for inhibitors of the murine GABA transporters mGAT3 and mGAT4. Eur. J. Pharmacol. 2005, 519, 43-47.

100 Knutsen, L. J. S., Andersen, K. E., Lau, J., Lundt, B. F., Henry, R. F., Morton, H. E., Nœrum, L., Petersen,

H., Stephensen, H., Suzdak, P. D., Swedberg, M. D. B., Thomsen, C., Sorensen, P. O.: Synthesis of novel GABA uptake inhibitors. 3. diaryloxime and diarylvinyl ether derivatives of nipecotic acid and guvacine as anticonvulsant agents. J. Med. Chem. 1999, 42, 3447-3462.

101 Barakat, L., Bordey, A.: GAT-1 and reversible GABA transport in bergmann glia in slices.

J. Neurophysiol. 2002, 88, 1407-1419.

102 Ackerman, B.L., Berna, M.J., Murphy, A.T.: Recent advances in use of LC/ MS/MS for quantitative high-throughput bioanalytical support of drug discovery. Curr. Top. Med. Chem. 2002, 2, 53-66.

103 Niessen, W.M.A.: Progress in liquid chromatography-mass spectrometry instrumentation and its impact on high-throughput screening.

J. Chromatogr. A 2003, 1000, 413-426.

104 Hopfgartner, G., Varesio, E.: New approaches for quantitative analysis in biological fluids using mass spectrometric detection. Trends Anal. Chem. 2005, 24, 583-589.

105 Wanner, K., Ftilep, G., Hofner, G.: WO 0014064, 2000 (Chem. Abstr. 2000, 132, 194656).

106 Zhao, X., Hoesl, C. E., Hoefner, G. C., Wanner, K. T.: Synthesis and biological evaluation of new GABA-uptake inhibitors derived from proline and from pyrrolidine-2-acetic acid. Eur. J. Med. Chem. 2005, 40, 231-247.

Was this article helpful?

0 0
Getting to Know Anxiety

Getting to Know Anxiety

Stop Letting Anxiety Rule Your Life And Take Back The Control You Desire Right Now! You don't have to keep letting your anxiety disorder run your life. You can take back your inner power and change your life for the better starting today! In order to have control of a thing, you first must understand it. And that is what this handy little guide will help you do. Understand this illness for what it is. And, what it isn't.

Get My Free Ebook


Post a comment