FLIPR Calcium Mobilization Assays in GPCR Drug Discovery

Grzegorz Woszczek; Elisabeth Fuerst; Thomas J A Maguire

doi:10.1007/978-1-0716-1221-7_13

FLIPR Calcium Mobilization Assays in GPCR Drug Discovery

Grzegorz Woszczek, Elisabeth Fuerst, Thomas J A Maguire

School of Immunology & Microbial Sciences
1Department of Hepatology, Imperial College London, London, UK. 2Institute of Liver Studies at King's College School of Medicine at King's College Hospital, London, UK. 3Institute of Human Health and Performance, University College London, London, UK. 4Department of Asthma Allergy and Lung Biology, King's College London, London, UK. 5Division of Critical Care Medicine, University of Alberta, Edmonton, Canada.
MRC & Asthma UK Centre for Allergic Mechanisms in Asthma, King’s College London, Johannesburg, South Africa

Research output: Contribution to journal › Article › peer-review

Abstract

Intracellular calcium mobilization can be measured using several methods varying in indicator dyes and devices used. In this chapter, we describe the fluorescence-based method (FLIPR Calcium 4 Assay) developed by Molecular Devices for a FlexStation and routinely used in our laboratory for detecting intracellular calcium changes. The assay is designed to study calcium mobilization induced by majority of GPCRs and calcium channels and allows for simultaneous concentration-dependent analysis of several receptor agonists and antagonists, useful in receptor characterization and drug discovery projects.

Original language	English
Pages (from-to)	193-205
Number of pages	13
Journal	Methods in molecular biology (Clifton, N.J.)
Volume	2268
DOIs	https://doi.org/10.1007/978-1-0716-1221-7_13
Publication status	Published - Jun 2021

Keywords

Biological Assay/methods
Calcium/metabolism
Calcium Channels/metabolism
Cells, Cultured
Drug Discovery/methods
Fluorometry/methods
High-Throughput Screening Assays/methods
Humans
Receptors, G-Protein-Coupled/metabolism
Signal Transduction

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10.1007/978-1-0716-1221-7_13

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title = "FLIPR Calcium Mobilization Assays in GPCR Drug Discovery",

abstract = "Intracellular calcium mobilization can be measured using several methods varying in indicator dyes and devices used. In this chapter, we describe the fluorescence-based method (FLIPR Calcium 4 Assay) developed by Molecular Devices for a FlexStation and routinely used in our laboratory for detecting intracellular calcium changes. The assay is designed to study calcium mobilization induced by majority of GPCRs and calcium channels and allows for simultaneous concentration-dependent analysis of several receptor agonists and antagonists, useful in receptor characterization and drug discovery projects.",

keywords = "Biological Assay/methods, Calcium/metabolism, Calcium Channels/metabolism, Cells, Cultured, Drug Discovery/methods, Fluorometry/methods, High-Throughput Screening Assays/methods, Humans, Receptors, G-Protein-Coupled/metabolism, Signal Transduction",

author = "Grzegorz Woszczek and Elisabeth Fuerst and Maguire, {Thomas J A}",

year = "2021",

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doi = "10.1007/978-1-0716-1221-7_13",

language = "English",

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journal = "Methods in molecular biology (Clifton, N.J.)",

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T1 - FLIPR Calcium Mobilization Assays in GPCR Drug Discovery

AU - Woszczek, Grzegorz

AU - Fuerst, Elisabeth

AU - Maguire, Thomas J A

PY - 2021/6

Y1 - 2021/6

N2 - Intracellular calcium mobilization can be measured using several methods varying in indicator dyes and devices used. In this chapter, we describe the fluorescence-based method (FLIPR Calcium 4 Assay) developed by Molecular Devices for a FlexStation and routinely used in our laboratory for detecting intracellular calcium changes. The assay is designed to study calcium mobilization induced by majority of GPCRs and calcium channels and allows for simultaneous concentration-dependent analysis of several receptor agonists and antagonists, useful in receptor characterization and drug discovery projects.

AB - Intracellular calcium mobilization can be measured using several methods varying in indicator dyes and devices used. In this chapter, we describe the fluorescence-based method (FLIPR Calcium 4 Assay) developed by Molecular Devices for a FlexStation and routinely used in our laboratory for detecting intracellular calcium changes. The assay is designed to study calcium mobilization induced by majority of GPCRs and calcium channels and allows for simultaneous concentration-dependent analysis of several receptor agonists and antagonists, useful in receptor characterization and drug discovery projects.

KW - Biological Assay/methods

KW - Calcium/metabolism

KW - Calcium Channels/metabolism

KW - Cells, Cultured

KW - Drug Discovery/methods

KW - Fluorometry/methods

KW - High-Throughput Screening Assays/methods

KW - Humans

KW - Receptors, G-Protein-Coupled/metabolism

KW - Signal Transduction

U2 - 10.1007/978-1-0716-1221-7_13

DO - 10.1007/978-1-0716-1221-7_13

M3 - Article

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SN - 1064-3745

VL - 2268

SP - 193

EP - 205

JO - Methods in molecular biology (Clifton, N.J.)

JF - Methods in molecular biology (Clifton, N.J.)

ER -

FLIPR Calcium Mobilization Assays in GPCR Drug Discovery

Abstract

Keywords

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