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Review

FLIPR™ Assays for GPCR and Ion Channel Targets

Michelle R. Arkin  1 , Patrick R. Connor  2 , Renee Emkey  2 , Kim E. Garbison  2 , Beverly A. Heinz  2 , Todd R. Wiernicki  2 , Paul A. Johnston  3 , Ramani A. Kandasamy, Nancy B. Rankl, Sitta Sittampalam  4
Sarine Markossian  1 , Abigail Grossman  1 , Hannah Baskir  1 , Michelle Arkin  2 , Douglas Auld  3 , Christopher Austin  4 , Jonathan Baell  5 , Kyle Brimacombe  1 , Thomas D.Y. Chung  6 , Nathan P. Coussens  7 , Jayme L. Dahlin  8 , Viswanath Devanarayan  9 , Timothy L. Foley  10 , Marcie Glicksman  11 , Kirill Gorshkov  12 , Stefan Grotegut  13 , Matthew D. Hall  1 , Samuel Hoare  14 , James Inglese  1 , Philip W. Iversen  15 , Madhu Lal-Nag  16 , Zhuyin Li  12 , Jason R. Manro  13 , James McGee  17 , Allison Norvil  13 , Mackenzie Pearson  13 , Terry Riss  18 , Peter Saradjian  19 , G. Sitta Sittampalam  20 , Michael A. Tarselli  21 , O. Joseph Trask Jr.  22 , Jeffrey R. Weidner  23 , Mary Jo Wildey  24 , Kelli Wilson  1 , Menghang Xia  1 , Xin Xu  1
, editors.
In: Assay Guidance Manual [Internet]. Bethesda (MD): Eli Lilly & Company and the National Center for Advancing Translational Sciences; 2004.
[updated ].
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Review

FLIPR™ Assays for GPCR and Ion Channel Targets

Michelle R. Arkin et al.
Free Books & Documents

Excerpt

Calcium ions (Ca2+) play a key role in cellular homeostasis involving calcium channel and GPCR function, which plays a critical role in many disease pathologies. Fluorescent Imaging Plate Reader (FLIPRTM ) technology to measure Ca2+ flux in cells was an important development in the early 1990’s and has played a significant role in HTS and lead optimization applications. In this chapter, the basic concepts in using the FLIPR instrument and assay development and optimization to measure Ca2+ flux in cells are described. Although this chapter is devoted to Ca2+ channel based assay development, the FLIPRTM is also useful for measuring potassium and other ion flux in cells with appropriate fluorescent dyes.

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References

Primary Reference

    1. Baxter D. F., et al. A novel membrane potential-sensitive fluorescent dye improves cell-based assays for ion channels. J. Biomolecular Screening. 2002;7:79–85. - PubMed

Additional Reading

    1. Benjamin E. R., et al. Pharmacological characterization of recombinant N-type calcium channel (Cav2.2) mediated calcium mobilization using FLIPR. Biochemical Pharmacology. 2006;72:770–782. - PubMed
    1. Coward P., et al. Chimeric proteins allow a high-throughput signaling assay of GI-coupled receptors. Analytical Biochemistry. 1999;270:242–248. - PubMed
    1. Hodder P., et al. Miniaturization of intracellular calcium functional assays to 1536-well plate format using a fluorometric imaging plate reader. J. Biomolecular Screening. 2004;9:417–426. - PubMed
    1. Jensen A. Functional characterization of human glycine receptors in a fluorescence-based high throughput screening assay. European J. Pharmacology. 2005;521:39–42. - PubMed
    1. Liu A.M.F., et al. G-α16/z chimeras efficiently link a wide range of G protein-coupled receptors to calcium mobilization. J. Biomolecular Screening. 2003;8:39–49. - PubMed

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