A high-throughput assay for modulators of ligand-gated chloride channels

Assay and Drug Development Technologies

Volumn 3, Issue 1, 2005, Pages 59-64

  Hamelin, Michel ^a   Meng, Xin ^a   Cuddy, Michael ^a   Korsun, Keith ^a   Ondeyka, John ^a   Simpson, Peter B ^a   Cully, Doris F ^a   Priest, Birgit T ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CHLORIDE CHANNEL; COUMARIN; DYE; GLUTAMIC ACID; IVERMECTIN; NATURAL PRODUCT;

ARTICLE; CAENORHABDITIS ELEGANS; CELL MEMBRANE DEPOLARIZATION; CELL STRAIN HEK293; CONTROLLED STUDY; FLUORESCENCE RESONANCE ENERGY TRANSFER; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; MEMBRANE POTENTIAL; QUANTITATIVE ANALYSIS; VOLTAGE CLAMP;

ANIMALS; BIOLOGICAL ASSAY; CAENORHABDITIS ELEGANS; CELLS, CULTURED; CHLORIDE CHANNELS; DOSE-RESPONSE RELATIONSHIP, DRUG; GLUTAMIC ACID; ION CHANNEL GATING; KIDNEY; PATCH-CLAMP TECHNIQUES; RECOMBINANT PROTEINS; ROBOTICS; SPECTROMETRY, FLUORESCENCE;

EID: 17344372340     PISSN: 1540658X     EISSN: None     Source Type: Journal    
DOI: 10.1089/adt.2005.3.59     Document Type: Article

References (13)

1. Cully DF, Vassilatis DK, Liu KK, Paress PS, Van der Ploeg LH, Schaeffer JM, Arena JP: Cloning of an avermectin-sensitive glutamate-gated chloride channel from Caenorhabditis elegans. Nature 1994;371:707-711.
2. Dent JA, Smith MM, Vassilatis DK, Avery L: The genetics of ivermectin resistance in Caenorhabditis elegans. Proc. Natl. Acad. Sci. U S A 2000;97:2674-2679.
3. Vassilatis DK, Arena JP, Plasterk RH, Wilkinson HA, Schaeffer JM, Cully DF, Van-der-Ploeg LH: Genetic and biochemical evidence for a novel avermectin-sensitive chloride channel in Caenorhabditis elegans Isolation and characterization. J Biol Chem 1997;272:33167-33174.
4. Dent JA, Davis MW, Avery L: avr-15 encodes a chloride channel subunit that mediates inhibitory glutamatergic neurotransmission and ivermectin sensitivity in Caenorhabditis elegans. EMBO J 1997;16:5867-5879.
5. Laughton DL, Lunt GG, Wolstenholme AJ: Reporter gene constructs suggest that the Caenorhabditis elegans avermectin receptor beta-subunit is expressed solely in the pharynx. J Exp Biol 1997;200:1509-1514.
6. Pemberton DJ, Franks CJ, Walker RJ, Holden-Dye L: Characterization of glutamate-gated chloride channels in the pharynx of wild-type and mutant Caenorhabditis elegans delineates the role of the subunit GluCl-alpha2 in the function of the native receptor. Mol Pharmacol 2001;59: 1037-1043.
7. Burg RW, Miller BM, Baker EE, Birnbaum J, Currie JA, Harman R, Kong VL, Monaghan RL, Olson G, Putter I, Tunac JP, Wallick H, Stapley EO, Oiwa R, Omura S: Avermectins, a new family of potent anthelmintic agents: producing organism and fermentation. Antimicrob Agents Chemother 1979;15:361-367.
8. Hamill OP, Marty A, Neher E, Sakmann B, Sigworth FJ: Improved patch-clamp techniques for high-resolution current recording from cells and cell-free membrane patches. Pflugers Arch 1981;391:85-100.
9. Zhang JH, Chung TDY, Oldenburg KR: A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J Biomol Screen 1999;4: 67-73.
10. Gonzalez JE, Oades K, Leychkis Y, Harootunian A, Negulescu PA: Cell-based assays and instrumentation for screening ion-channel targets. Drug Discov Today 1999;4:431-439.
11. Gonzalez JE, Maher MP: Cellular fluorescent indicators and voltage/ion probe reader (VIPR) tools for ion channel and receptor drug discovery. Receptors Channels 2002;8:283-295.
12. Adkins CE, Pillai GV, Kerby J, Bonnert TP, Haldon C, McKernan RM, Gonzalez JE, Oades K, Whiting PJ, Simpson PB: Alpha4beta3delta GABA(A) receptors characterized by fluorescence resonance energy transfer-derived measurements of membrane potential. J Biol Chem 2001;276:38934-38939.
13. Takiguchi Y, Mishima H, Okuda M, Terao M, Aoki A, Fukuda R: Milbemycins, a new family of macrolide antibiotics: fermentation, isolation and physico-chemical properties. J Antibiot (Tokyo) 1980;33:1120-1127.